A meta-analysis of the efficacy and safety of the traditional Chinese medicine formula Kaixinsan decoction for depression.

BACKGROUND: Kaixinsan (KXS) decoction is a traditional Chinese herbal formulation commonly used to treat depression. This study aimed to evaluate the efficacy and safety of KXS, which is widely used, alone and in combination with other therapies, for the treatment of depression. The main objective was to assess the efficacy and safety of KXS in the treatment of depression as a single agent or in combination with other methods. METHODS: Randomized controlled trials of KXS in the treatment of depression were systematically searched from several Chinese and English databases with no language restriction. Patients in these studies met the relevant diagnostic criteria for depression. Data on HAMD, SDS, practical situations, and occurrence of side effects in the studies were extracted. Finally, the methodological quality and risk of bias of the included studies were assessed using the Jadad scale and Cochrane bias evaluation tool. RESULTS: Twelve studies with 1034 patients were included after screening. The Jadad scale and Cochrane bias evaluation tool indicated that the quality of the studies ranged from fair to good, with 41.7% categorized as good and 58.3% as poor. Egger test and funnel plots showed that the publication bias remain low. CONCLUSION: The results showed that the frequency of side effects in the control group was higher than that in the treatment group, and there was a statistically significant difference. KXS was comparable or superior to antidepressants in treating depression and has fewer side effects. The data analysis showed that effectiveness and other indicators differed significantly by geographic area and dosage form, which has implications for future clinical work.

Tongue texture may contribute to the assessment of malignant risk of thyroid nodules.

In the present study, it was aimed to evaluate whether there is an objective tongue image indicator that could be used to evaluate malignant risk of thyroid nodules through a cross sectional study. From December 2018 to December 2020, the TFDA-1 digital tongue-face diagnostic instrument was used to collect the tongue images. TDAS 2.0 software was used for tongue image analysis. A standardized database was constructed by combining patient physical examination results and tongue image analysis results. The relationship between tongue image index and TI-RADS classification of thyroid nodules was tested. A total of 5,900 cases were collected and 4,615 cases were included in the present study after excluding 154 cases due to incomplete information, 1,221 cases with thyroid nodules were separated into 417 cases TI-RADS 2 group, 693 cases in TI-RADS 3 group and 111 cases in TI-RADS 4 group. Without considering confounding factors, tongue image indexes zhiCon, zhiASM, zhiENT, zhiMEAN, zhiClrB, zhiClrR, zhiClrG, zhiClrI, zhiClrL and zhiClrY were significantly different among the three groups (P<0.05). Excluding the influence of age, sex, body mass index, smoking and drinking, the results of one-way variance linear trend analysis showed that the values of zhiCon, zhiENT and zhiMEAN increased with the increasing TI-RADS category, while the values of zhiASM decreased with the increase of TI-RADS category. Tongue texture index may be helpful for differentiating the benign and malignant of thyroid nodules.

Midterm Outcomes of Kissing Covered Self-Expanding Stents for Reconstruction of Complex Aortoiliac Occlusive Disease.

BACKGROUND: We sought to investigate the midterm results of kissing self-expanding covered stents (SECSs) for the reconstruction of aortic bifurcation in complex aortoiliac occlusive disease. METHODS: Data of consecutive patients who had undergone endovascular treatment for aortoiliac occlusive disease were screened. Only patients with TransAtlantic Inter-Society Consensus (TASC) class C and D lesions treated by bilateral iliac kissing stents (KSs) were included. Midterm primary patency, risk factors, and limb salvage rates were analyzed. Follow-up results were analyzed using the Kaplan-Meier curves. Cox proportional hazards models were used to identify the predictors of primary patency. RESULTS: A total of 48 patients (95.8% men; mean age, 65.3 ± 10.2 years) were treated with kissing SECSs. Of them, 17 patients had TASC-II class C lesions and 31 had class D lesions. There were 38 total occlusive lesions, with a mean occlusive lesion length of 108.2 ± 57.3 mm. The overall mean lesion length was 140.3 ± 60.5 mm, and the mean length of implanted stents in the aortoiliac arteries was 141.9 ± 59.9 mm. The mean diameter of the deployed SECSs was 7.8 ± 0.5 mm. The mean follow-up time was 36.5 ± 15.8 months, and the follow-up rate was 95.8%. At 36 months, the overall primary patency, assisted primary patency, secondary patency, and limb salvage rates were 92.2%, 95.7%, 97.8%, and 100%, respectively. Univariate Cox regression analysis revealed that stent diameter ≤7 mm (hazard ratio [HR]: 9.53; 95% confidence interval [CI] 1.56-57.94, P = 0.014) and severe calcification (HR: 12.66; 95% CI 2.04-78.45, P = 0.006) were significantly associated with restenosis. Multivariate analysis showed severe calcification to be the only significant determinant of restenosis (HR: 12.66; 95% CI 2.04-78.45, P = 0.006). CONCLUSIONS: Kissing SECSs provide good midterm results for the treatment of aortoiliac occlusive disease. A stent diameter >7 mm is a potent protective factor against restenosis. Because severe calcification appears to be the only significant determinant of restenosis, patients with severe calcification require close follow-up.

Chromosome-level de novo genome assembly of two conifer-parasitic wasps, Megastigmus duclouxiana and Megastigmus sabinae, reveals genomic imprints of adaptation to hosts.

Conifers make up about one third of global forests but are threatened by seed parasitoid wasp species. Many of these wasps belong to the genus Megastigmus, yet little is known about their genomic background. In this study, we provide chromosome-level genome assemblies for two oligophagous conifer parasitoid species of Megastigmus, which represent the first two chromosome-level genomes of the genus. The assembled genomes of Megastigmus duclouxiana and M. sabinae are 878.48 Mb (scaffold N50 of 215.60 Mb) and 812.98 Mb (scaffold N50 of 139.16 Mb), respectively, which are larger than the genome size of most hymenopterans due to the expansion of transposable elements. Expanded gene families highlight the difference in sensory-related genes between the two species, reflecting the difference in their hosts. We further found that these two species have fewer family members but more single-gene duplications than polyphagous congeners in the gene families of ATP-binding cassette transporter (ABC), cytochrome P450 (P450) and olfactory receptors (OR). These findings shed light on the pattern of adaptation to a narrow spectrum of hosts in oligophagous parasitoids. Our findings suggest potential drivers underlying genome evolution and parasitism adaptation, and provide valuable resources for understanding the ecology, genetics and evolution of Megastigmus, as well as for the research and biological control of global conifer forest pests.

Reproduction and genetic diversity of Juniperus squamata along an elevational gradient in the Hengduan Mountains.

Elevation plays a crucial factor in the distribution of plants, as environmental conditions become increasingly harsh at higher elevations. Previous studies have mainly focused on the effects of large-scale elevational gradients on plants, with little attention on the impact of smaller-scale gradients. In this study we used 14 microsatellite loci to survey the genetic structure of 332 Juniperus squamata plants along elevation gradient from two sites in the Hengduan Mountains. We found that the genetic structure (single, clonal, mosaic) of J. squamata shrubs is affected by differences in elevational gradients of only 150 m. Shrubs in the mid-elevation plots rarely have a clonal or mosaic structure compared to shrubs in lower- or higher-elevation plots. Human activity can significantly affect genetic structure, as well as reproductive strategy and genetic diversity. Sub-populations at mid-elevations had the highest yield of seed cones, lower levels of asexual reproduction and higher levels of genetic diversity. This may be due to the trade-off between elevational stress and anthropogenic disturbance at mid-elevation since there is greater elevational stress at higher-elevations and greater intensity of anthropogenic disturbance at lower-elevations. Our findings provide new insights into the finer scale genetic structure of alpine shrubs, which may improve the conservation and management of shrublands, a major vegetation type on the Hengduan Mountains and the Qinghai-Tibet Plateau.

The Efficacy and Safety of Acupuncture for Treating Osteoporotic Vertebral Compression Fracture- (OVCF-) Induced Pain: A Systematic Review and Meta-Analysis of Randomized Clinical Trials.

BACKGROUND: Osteoporotic vertebral compression fractures (OVCFs) are common health issues in the elderly that cause chronic pain in over one-third of patients. This study was sought to evaluate the efficacy and safety of acupuncture for alleviating pain caused by OVCFs. METHODS: We performed a search of 8 electronic databases for publications from the inception to 30th March 2021. Eligible studies were randomized clinical trials (RCTs) that evaluated the effect of acupuncture for the treatment of OVCFs. Two investigators evaluated literature quality and extracted data independently. RevMan V.5.4.1 was used for data analyses, with pooled risk estimates presented as mean difference (MD) or relative risk (RR) along with corresponding 95% confidence intervals (CIs), as appropriate. RESULTS: Fourteen RCTs involving 1,130 patients were included in this meta-analysis. Compared with the control group, acupuncture showed a greater benefit on pain reduction caused by OVCFs (1 week: MD = -1.26, 95% CI: (-1.82,-0.70); 1 month: MD = -1.63, 95% CI: (-1.82,-1.43); 6 months: MD = -1.13, 95% CI: (-1.55, -0.70)). Acupuncture treatment was also associated with fewer adverse events, lower ODI index, and higher bone density than the control group (safety: (RR: 0.30, 95% CI: 0.12-0.75); ODI: MD = -3.19, 95% CI: (-5.20, -1.19); bone density: MD = 0.15, 95% CI: (0.05, 0.26)). The GRADE quality of these results was assessed as low or very low. CONCLUSIONS: Compared with the control treatment, acupuncture was more effective and safer in relieving the pain caused by OVCF and made a greater improvement on patient's ODI score and bone density. Given the low level of our study evidence, future high-quality studies are needed to verify our study findings.

Diffuse reduction of spleen density is a novel prognostic marker for intrahepatic cholangiocarcinoma after curative resection.

BACKGROUND: Diffuse reduction of spleen density (DROSD) is related to cancer prognosis; however, its role in intrahepatic cholangiocarcinoma (ICC) remains unclear. AIM: To assess the predictive value of DROSD in the prognosis of ICC after curative resection. METHODS: In this multicenter retrospective cohort study, we enrolled patients with ICC who underwent curative hepatectomy between 2012 and 2019. Preoperative spleen density was measured using computed tomography. Overall survival (OS) and recurrence-free survival (RFS) rates were calculated and compared utilizing the Kaplan-Meier method. Univariable and multivariable Cox regression analyses were applied to identify independent factors for OS and RFS. A nomogram was created with independent risk factors to predict prognosis of patients with ICC. RESULTS: One hundred and sixty-seven ICC patients were enrolled. Based on the diagnostic cut-off values (spleen density ≤ 45.5 Hounsfield units), 55 (32.9%) patients had DROSD. Kaplan-Meier analysis indicated that patients with DROSD had worse OS and RFS than those without DROSD (P < 0.05). Cox regression analysis revealed that DROSD, carcinoembryonic antigen level, carbohydrate antigen 19-9 level, length of hospital stay, lymph node metastasis, and postoperative complications were independent predictors for OS (P < 0.05). The nomogram created with these factors was able to predict the prognosis of patients with ICC with good reliability (OS C-index = 0.733). The area under the curve for OS was 0.79. CONCLUSION: ICC patients with DROSD have worse OS and RFS. The nomogram is a simple and practical method to identify high-risk ICC patients with poor prognosis.

[Advances on the study of movable artificial vertebral body].

At present, artificial vertebral implants have proven to be effective in the treatment of spinal tumors, infections, fractures and other diseases. However, the fusion artificial vertebral body can cause adjacent intervertebral joint degeneration and loss of original physiological curvature and activity. The movable artificial vertebral body can, to some extent, restore the normal physiological movement and reduce biomechanical changes of the spine, reducing the occurrence of complication. The design of movable artificial vertebral body is to equip movable device when the basis of reliable stability is obtained. According to its principle it can be divided into ball socket joint or elastic deformation. However the overall design of movable artificial vertebral body needs further improvement. Traditional mechanical processing methods are difficult to process complex prostheses and the agreement rate between traditional produced prostheses and lesions was low. While the emerging 3D printing technology can achieve individualized improvement of prosthesis, its slow rate and high cost need to be improved. The materials of movable artificial vertebral body includes metal, ceramics, biomaterials, high polymer materials and so on. Titanium alloy is the main material in metal materials, which is widely used, but its modulus of elasticity is still far from that of human bone and it lacks ideal bone fusion. Ceramic materials are rich in variety but fragile and poor in wear resistance. Biomaterials include autogenous bone, allogeneic bone, etc., with limited source and complicated operation. There are many kinds of polymer and biodegradable materials which obtain excellent and ideal properties. But their properties and applications need to be further studied. The movable artificial vertebral body still needs to be promoted and developed. The clinical experimental data is still insufficient, and long-term curative effect needs to be further observed and studied. This paper reviews the development, advantages, design, processing and materials of movable artificial vertebral bodies and provides useful reference for optimization design, processing and clinical application of movable artificial vertebral bodies.

Alarm Value of Somatosensory Evoked Potential in Idiopathic Scoliosis Surgery.

BACKGROUND: Somatosensory evoked potential (SSEP) monitoring is performed to examine postoperative clinical findings when a monitoring event was noted intraoperatively and to ascertain the alarm threshold for intraoperative neural damage. METHODS: The tibial SSEP of both lower limbs was recorded intraoperatively in patients with idiopathic scoliosis. Change of SSEP amplitude as opposed to the baseline was categorized into 4 levels: decrease <40%, decrease of 40%-50%, decrease of 50%-60%, and decrease >60%. Postoperative neurologic function of patients was examined and compared with SSEP data. RESULTS: The baseline amplitude before incision was significantly different from the amplitude after spine exposure. An amplitude reduction of >60% during scoliosis correction procedures was observed in 6 legs, and 4 of them had postoperative deterioration in motor status. As the measure of threshold for alarm, an amplitude reduction of >50% compared with baseline resulted in more false-positive outcomes compared with amplitude attenuation of >60%. CONCLUSIONS: Compared with the traditional SSEP baseline before skin incision, the baseline acquired after spine exposure results in more accurate monitoring. A >60% decrease in SSEP amplitude could be a more suitable alarm threshold.

Girdin expression in cervical carcinoma and its role in the malignant properties of HeLa cells.

Cervical cancer is a major cause of mortality in females worldwide, with the majority of cases reported in developing countries. The molecular mechanisms of this disease are unclear. However, increasing evidence indicates that the expression or overexpression of Girdin is associated with a poor prognosis in a variety of cancer types. Therefore, the aim of the current study was to evaluate the potential association between Girdin expression, and malignant properties of cervical cancer lesions and HeLa cells. Girdin protein expression was examined in 87 samples of cervical squamous cell lesions, including intraepithelial neoplasia (grades I and III) and invasive carcinoma, using immunohistochemical (IHC) staining. A short-hairpin RNA (shRNA) approach was employed to specifically suppress the expression of Girdin mRNA in HeLa cells in vitro, allowing the role of Girdin in a number of malignant properties to be evaluated. Girdin protein was observed in the cytoplasm of 79/87 (90.8%) cervical cancer lesion specimens. However, no positive Girdin signals were identified in healthy cervical squamous epithelium samples. Furthermore, a significant correlation between Girdin expression and lesion grade was identified (Spearman's correlation coefficient, 0.566; P<0.001). When Girdin was suppressed by Girdin shRNA, the rate of HeLa cell growth was significantly reduced in vitro (P<0.05). Additional analysis determined that Girdin was associated with serum-deprived induced HeLa apoptosis. Thus, patients with high-grade cervical cancer tumors exhibited a strong expression for Girdin, and Girdin appears to key in HeLa cell proliferation and serum-deprived induced apoptosis, supporting the hypothesis that Girdin may be important in the process of cervical carcinogenesis.

Phagocytosis of platelets enhances endothelial cell survival under serum deprivation.

Platelets are key players in fundamental processes of vascular biology, such as angiogenesis, tissue regeneration, and tumor metastasis. However, the underlying mechanisms remain unclear. In this study, some tumor vascular endothelial cells were positively stained by antiplatelet antibodies. Further investigation revealed that platelets were taken up by endothelial cells in vitro and in vivo. Human umbilical vascular endothelial cells were rendered apoptotic under conditions of serum deprivation. However, endothelial apoptosis was suppressed and cell viability was enhanced when platelets were added to the cultures. Endothelial survival was paralleled by an upregulation of phosphorylated Akt and p70 S6K. In conclusion, this study demonstrated that platelets can be phagocytosed by endothelial cells, and the phagocytosed platelets could suppress endothelial apoptosis and promote cell viability level. The mechanism underlying this process involves the activation of Akt signaling.

Assessment of muscle mass and its association with protein intake in a multi-ethnic Asian population: relevance in chronic kidney disease.

BACKGROUND: Clinical practice guidelines recommend objective nutritional assessments in managing chronic kidney disease (CKD) patients but were developed while referencing to a North-American population. Specific recommendations for assessing muscle mass were suggested (mid-arm circumference, MAC; corrected mid-arm muscle area, cAMA; mid-arm muscle circumference, MAMC). This study aimed to assess correlation and association of these assessments with dietary protein intake in a multi-ethnic Asian population of healthy and CKD patients. METHODS: We analyzed 24-hour urine collections of selected participants to estimate total protein intake (TPI; g/day). Ideal body weight (IDW; kg) was calculated and muscle assessments conducted. Analyses involved correlation and linear regression, taking significance at p<0.05. RESULTS: There were 232 stable CKD patients and 103 healthy participants comprising of 51.0% male, 38.5% Chinese, 29.6% Malay, 23.6% Indian, and 8.4% others. The mean TPI was 58.9 ± 18.4 g/day in healthy participants and 53.6 ± 19.4 g/day in CKD patients. When normalized to ideal body weight, TPI-IDW (g/kg/day) was similar in healthy and CKD participants. Overall, TPI was associated with MAC (r=0.372, p<0.001), cAMA (r=0.337, p<0.001), and MAMC (r=0.351, p<0.001). TPI-IDW was also associated with MAC (r=0.304, p<0.001), cAMA (r=0.202, p<0.001), and MAMC (r=0.200, p<0.001) but not for TPI normalized to actual body weight. When examined separately, TPI was associated with MAC, cAMA, and MAMC in both CKD and healthy participants, but was associated with TPI-IDW only in CKD patients. CONCLUSION: Total protein intake was associated with muscle assessments in all participants. TPI normalized to IDW should only be used in CKD patients.

Percutaneous Cryoablation for Liver Cancer.

Based on the primary tumor site, liver cancer can be divided into two categories: (1) primary liver cancer and (2) metastatic cancer to the liver from a distant primary site. Guided cryoablation via many imaging methods induces iceball formation and tumor necrosisand is an attractive option for treating unresectable hepatocellular carcinoma (HCC) and metastatic liver cancer. There are several advantages to using cryoablation for the treatment of liver cancer: it can be performed percutaneously, intraoperatively, and laparoscopically; iceball formation can be monitored; it has little impact on nearby large blood vessels; and it induces a cryo-immunological response in situ. Clinically, primary research has shown that percutaneous cryoablation of liver cancer is relatively safe and efficient, and it can be combined with other methods, such as radiation therapy, chemotherapy, and immunology, to control disease. Although research is preliminary, cryosurgery is fast becoming an alternative treatment method for HCC or liver tumors. Here, we review the mechanisms of liver tumor cryoablation, cryoablation program selection, clinical efficiency, and complications following treatment.

Combination treatment with comprehensive cryoablation and immunotherapy in metastatic hepatocellular cancer.

AIM: To retrospectively assess the effect of comprehensive cryosurgery (ablation of intra- and extra-hepatic tumors) plus dendritic cell-cytokine-induced killer cell immunotherapy in metastatic hepatocellular cancer. METHODS: We divided 45 patients into cryo-immunotherapy (21 patients), cryotherapy (n = 12), immunotherapy (n = 5) and untreated (n = 7) groups. Overall survival (OS) after diagnosis of metastatic hepatocellular cancer was assessed after an 8-year follow-up. RESULTS: Median OS was higher following cryo-immunotherapy (32 mo) or cryotherapy (17.5 mo; P < 0.05) than in the untreated group (3 mo) and was higher in the cryo-immunotherapy group than in the cryotherapy group (P < 0.05). In the cryo-immunotherapy group, median OS was higher after multiple treatments (36.5 mo) than after a single treatment (21 mo; P < 0.05). CONCLUSION: Cryotherapy and, especially, cryo-immunotherapy significantly increased OS in metastatic hepatocellular cancer patients. Multiple cryo-immunotherapy was associated with a better prognosis than single cryo-immunotherapy.

Classification algorithms enhance the discrimination of glaucoma from normal eyes using high-definition optical coherence tomography.

PURPOSE: To evaluate the diagnostic performance of classification algorithms based on Linear Discriminant Analysis (LDA) and Classification And Regression Tree (CART) methods, compared with optic nerve head (ONH) and retinal nerve fiber layer (RNFL) parameters measured by high-definition optical coherence tomography (Cirrus HD-OCT) for discriminating glaucoma subjects. METHODS: Consecutive glaucoma subjects (Training data = 184; Validation data = 102) were recruited from an eye center and normal subjects (n = 508) from an ongoing Singaporean Chinese population-based study. ONH and RNFL parameters were measured using a 200 × 200 scan protocol. LDA and CART were computed and areas under the receiver operating characteristic curve (AUC) compared. RESULTS: Average RNFL thickness (AUC 0.92, 95% confidence interval [CI] 0.91, 0.93), inferior RNFL thickness (AUC 0.92, 95% CI 0.91, 0.93), vertical cup-disc ratio (AUC 0.91, 95% CI 0.90, 0.92) and rim area/disc area ratio (AUC 0.90, 95% CI 0.86, 0.93) discriminated glaucoma better than other parameters (P ≤ 0.033). LDA (AUC 0.96, 95% CI 0.95, 0.96) and CART (0.98, 95% CI 0.98, 0.99) outperformed all parameters for diagnostic accuracy (P ≤ 0.005). Misclassification rates in LDA (8%) and CART (5.6%) were found to be low. The AUC of LDA for the validation data was 0.98 (0.95, 0.99) and CART was 0.99 (0.99, 0.994). CART discriminated mild glaucoma from normal better than LDA (AUC 0.94 vs. 0.99, P < 0.0001). CONCLUSIONS: Classification algorithms based on LDA and CART can be used in HD-OCT analysis for glaucoma discrimination. The CART method was found to be superior to individual ONH and RNFL parameters for early glaucoma discrimination.

Goodness-of-fit tests for correlated paired binary data.

We review a few popular statistical models for correlated binary outcomes, present maximum likelihood estimates for the model parameters, and discuss model selection issues using a variety of goodness-of-fit test statistics. We apply bootstrap strategies that are computationally efficient to evaluate the performance of goodness-of-fit statistics and observe that generally the power and the type I error rate of the goodness-of-fit statistics depend on the model under investigation. Our simulation results show that careful choice of goodness-of-fit statistics is an important issue especially when we have a small sample and the outcomes are highly correlated. Two biomedical applications are included.

Radical treatment of stage IV pancreatic cancer by the combination of cryosurgery and iodine-125 seed implantation.

AIM: To investigate the therapeutic effect of radical treatment and palliative treatment in stage IV pancreatic cancer patients. METHODS: 81 patients were enrolled in the study. Radical treatment was performed on 51 patients, while 30 patients were put under palliative treatment. The procedural safety and interval survival for stage IV pancreatic cancer (IS-IV) was assessed by almost 2.5 years of follow-ups. The IS-IV of patients under the two kinds of treatment, and the effects of treatment timing and frequency on IS-IV, were compared. RESULTS: The IS-IV of patients who received radical treatment was significantly longer than those who received palliative treatment (P < 0.001). The IS-IV of patients who received delayed radical or palliative treatment was longer than those who received accordingly timely treatment (P = 0.0034 and 0.0415, respectively). Multiple treatments can play an important role in improving the IS-IV of patients who received radical treatment (P = 0.0389), but not for those who received palliative treatment (P = 0.99). CONCLUSION: The effect of radical treatment was significantly more obvious than that of palliative treatment, and multiple radical treatments may contribute more to patients than a single radical treatment.

3-(2-Chloro-phen-yl)-4-hy-droxy-furan-2(5H)-one.

In the title mol-ecule, C(10)H(7)ClO(3), the butyrolactone core, a furan-2(5H)-one, forms a dihedral angle of 59.21 (5)° with the benzene ring. In the crystal, two types of hydrogen bonds (O-H⋯O and C-H⋯Cl) link mol-ecules into infinite chains along the b axis. π-π contacts [centroid-centroid distances = 3.6359 (10) and 3.8776 (11) Å] link the chains into a three-dimensional network.

Tyrosyl-tRNA synthetase inhibitors as antibacterial agents: synthesis, molecular docking and structure-activity relationship analysis of 3-aryl-4-arylaminofuran-2(5H)-ones.

Thirty-five 3-aryl-4-arylaminofuran-2(5H)-one derivatives were designed, prepared and tested for their inhibitory activity against tyrosyl-tRNA synthetase. Out of these compounds, 3-(3-bromophenyl)-4-(3,5-dichlorophenylamino)furan-2(5H)-one (35) was the most active with IC(50) of 0.09 ± 0.02 µM. The structure-activity relationship revealed that introduction of chlorine atoms at both meta positions of aniline moiety significantly increased the enzyme inhibitory activity. The results of antibacterial assay revealed that the tested compounds showed good activity against Gram-positive bacteria, with 35 being the most potent with MIC(50) of 0.06 µg/mL against Staphylococcus aureus ATCC 25923. Molecular docking of 35 into S. aureus tyrosyl-tRNA synthetase active site was also performed. The inhibitor snugly fitting the active site may well explain its excellent inhibitory activity.

3-(4-Bromo-phen-yl)-4-[2-(4-nitro-phen-yl)hydrazin-yl]furan-2(5H)-one.

In the title compound, C(16)H(12)BrN(3)O(4), the furan-2(5H)-one ring forms a dihedral angle of 33.19 (9)° with the 4-bromo-benzene unit and is nearly perpendicular to the 4-nitro-benzene segment, making a dihedral angle of 89.93 (10)°. In the crystal, N-H⋯O hydrogen bonds link the mol-ecules, generating an infinite chain along [010]. The chains are linked into a three-dimensional network by C-H⋯O, C-H⋯π and π-π contacts [centroid-centroid separation = 3.805 (2) Å].