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1.
PLoS One ; 15(3): e0229598, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32130248

RESUMO

BACKGROUND AND AIM: Coronary heart disease (CHD) is a chronic complex disease caused by a combination of factors such as lifestyle behaviors and environmental and genetic factors. We conducted this study to evaluate the risk factors affecting the development of CHD in Xinjiang, and to obtain valuable information for formulating appropriate local public health policies. METHOD: We conducted a nested case-control study with 277 confirmed CHD cases and 554 matched controls. The association of the risk factors with the risk of CHD was assessed using the multivariate Cox proportional hazard model. Multiplicative interactions were evaluated by entering interaction terms in the Cox proportional hazard model. The additive interactions among the risk factors were assessed by the index of additive interaction. RESULTS: The risk of CHD increased with frequent high-fat food consumption, dyslipidemia, obesity, and family history of CHD after adjustment for drinking, smoking status, hypertension, diabetes, family history of hypertension, and family history of diabetes. We noted consistent interactions between family history of CHD and frequent high-fat food consumption, family history of CHD and obesity, frequent high-fat food consumption and obesity, frequent high-fat food consumption and dyslipidemia, and obesity and dyslipidemia. The risk of CHD events increased with the presence of the aforementioned interactions. CONCLUSIONS: Frequent high-fat food consumption, family history of CHD, dyslipidemia and obesity were independent risk factors for CHD, and their interactions are important for public health interventions in patients with CHD in Xinjiang.

2.
Orthop Surg ; 2020 Mar 11.
Artigo em Inglês | MEDLINE | ID: mdl-32159285

RESUMO

OBJECTIVES: To investigate the contact stress and the contact area o tibial inserts and bushings with respect to different congruency designs in a spherical center axis and rotating bearing hinge knee prosthesis under gait cycle loading conditions using finite element analysis. METHODS: Nine prostheses with different congruency (different degrees of tibiofemoral conformity and different distances between the spherical center and the bushing) designs were developed with the same femoral and tibial components. The models were transferred to finite element software. The peak contact stresses and contact areas on tibial inserts and bushings under the gait cycle loading conditions were investigated and compared. RESULTS: For tibial insert, the peak contact stress was the highest in the low conformity-long group (61.4486 MPa), and it was 1.88 times higher than that in the group with the lowest stress (moderate conformity-short group, 32.754 MPa). The contact area was the largest in the low conformity-long group (420.485 mm2 ), and it was 1.19 times larger than that in the group with the smallest area (moderate conformity-middle group, 352.332 mm2 ). For bushing, the peak contact stress was the highest in the high conformity-long group (72.8093 MPa), and it was 3.21 times higher than that in the group with the lowest stress (high conformity-short group, 22.6928 MPa). The contact area was the largest in the low conformity-short group (2.41 mm2 ), and it was 2.27 times larger than that in the group with the smallest area (high conformity-middle group, 1.063 mm2 ). CONCLUSION: The results of our study showed that the congruency of the tibiofemoral surface and bushing surface should be considered carefully in the design of the spherical center axis and rotating bearing hinge knee prosthesis. Different levels of contact performance were observed with different congruency designs. In addition, the influence of contact stress and contact area on the polyethylene wear of rotating hinge knee prostheses should be confirmed with additional laboratory tests.

3.
Br J Haematol ; 2020 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-32037523

RESUMO

The serine synthesis pathway (SSP) is active in multiple cancers. Previous study has shown that bortezomib (BTZ) resistance is associated with an increase in the SSP in multiple myeloma (MM) cells; however, the underlying mechanisms of SSP-induced BTZ resistance remain unclear. In this study, we found that phosphoglycerate dehydrogenase (PHGDH), the first rate-limiting enzyme in the SSP, was significantly elevated in CD138+ cells derived from patients with relapsed MM. Moreover, high PHGDH conferred inferior survival in MM. We also found that overexpression of PHDGH in MM cells led to increased cell growth, tumour formation, and resistance to BTZ in vitro and in vivo, while inhibition of PHGDH by short hairpin RNA or NCT-503, a specific inhibitor of PHGDH, inhibited cell growth and BTZ resistance in MM cells. Subsequent mechanistic studies demonstrated PHGDH decreased reactive oxygen species (ROS) through increasing reduced glutathione (GSH) synthesis, thereby promoting cell growth and BTZ resistance in MM cells. Furthermore, adding GSH to PHGDH silenced MM cells reversed S phase arrest and BTZ-induced cell death. These findings support a mechanism in which PHGDH promotes proliferation and BTZ resistance through increasing GSH synthesis in MM cells. Therefore, targeting PHGDH is a promising strategy for MM therapy.

4.
Hum Cell ; 33(2): 386-396, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32065361

RESUMO

Long non-coding RNAs (lncRNAs) play key roles in tumorigenesis. It has been reported that the lncRNA nuclear-enriched abundant transcript 1 (NEAT1) may act as an oncogenic regulator in several cancers. However, the biological mechanism of action of NEAT1, particularly the miRNA sponge role in colorectal cancer (CRC), has not been fully elucidated. In our study, the expression of NEAT1, miR-205-5p, and vascular endothelial growth factor A (VEGFA) in CRC cell lines were assessed by reverse transcription-quantitative polymerase chain reaction (RT-qPCR) analysis. Cell proliferation was detected by Cell Counting Kit-8 (CCK-8) assay. Cell migration and invasion were examined by wound healing and transwell assays, respectively. RNA-binding protein immunoprecipitation (RIP), and dual-luciferase and RNA pull-down assays were conducted to determine the correlation between miR-205-5p and NEAT1 or VEGFA. VEGFA, matrix metalloproteinase (MMP)2, and MMP9 protein and mRNA expression were measured by western blotting and RT-qPCR analysis, respectively. Our results demonstrated high expression of NEAT1 and VEGFA and low expression of miR-205-5p in CRC cell lines. The RIP and dual-luciferase assays confirmed miR-205-5p as a target of NEAT1. In addition, VEGFA was identified as a direct target of miR-205-5p. Inhibition of NEAT1 or overexpression of miR-205-5p was able to repress VEGFA expression. Moreover, downregulation of NEAT1 and VEGFA inhibited cell proliferation, migration, and invasion. NEAT1 overexpression facilitated tumor growth by modulating miR-205-5p. Taken together, lncRNA NEAT1 was found to be upregulated in CRC cell lines, promoting CRC cell proliferation, migration, and invasion through regulating the miR-205-5p/VEGFA signaling pathway. These findings suggest that NEAT1 may be a promising biomarker in CRC diagnosis and treatment.

5.
Zhongguo Shi Yan Xue Ye Xue Za Zhi ; 28(1): 82-87, 2020 Feb.
Artigo em Chinês | MEDLINE | ID: mdl-32027257

RESUMO

OBJECTIVE: To provide clinical basis for the diagnosis and treatment of chronic neutrophilic leukemia (CNL) and to provide possible molecular targets for the treatment. METHODS: By summarizing the clinical data of 14 patients with CNL, the clinical characteristics, gene mutation types and possible prognostic factors were analyzed. RESULTS: Among the 14 patients with CNL, males (9 cases) were more than females (5 cases), with a median age of 57 years old. The detection rate of CSF3R mutation was 92.86% (13/14), including 12 cases (85.71%) with T318I mutation and 1 case of Y799X mutation, and only 1 case was not detected for mutation of CSF3R. The ASXL1 mutation was detected in 42.86% (6/14) of the patients, all of which were nonsense mutations, including 4 cases with R693X and 2 cases with E705X, and 14.29% (2/14) of the patients was detected for SETBP1 mutation, all of which were with D868N mutation. No patients with simultaneous ASXL1 and SETBP1 mutations were found, and JAK2 and CALR mutations were not detected. All of the patients had normal karyotypes. These patients' median survival time was 30 months (95%CI 13.19-46.80), and the influence of age over 60 years old was statistically significant (21.83 months vs 35.35 months) (P<0.05). CONCLUSION: It is difficult to diagnose CNL. CSF3R T618I mutation is its specific mutation, and ASXL1 mutation and SETBP1 mutation have auxiliary diagnostic significance for CNL. The age>60 years old at diagnosis is a factor of unfavourable prognosis.


Assuntos
Leucemia , Neutrófilos , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Mutação , Prognóstico , Receptores de Fator Estimulador de Colônias
6.
Appl Microbiol Biotechnol ; 104(4): 1533-1543, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31894364

RESUMO

Marine microorganisms live in dramatically different environments and have attracted much attention for their structurally unique natural products with potential strong biological activity. Based on the one strain-many compounds (OSMAC) strategy and liquid chromatography mass spectrometry (LC-MS) methods, our continuing efforts on the investigation of novel active compounds from marine Verrucosispora sp. MS100137 has led to the identification of a new polycyclic metabolite, abyssomicin Y (1), together with six known abyssomicin and proximicin analogs (2-7). Abyssomicin Y is a type I abyssomicin with an epoxide group at C-8 and C-9. Compounds 1-3 showed potent inhibitory effects against the influenza A virus; their observed inhibition rates were 97.9%, 98.3%, and 95.9%, respectively, at a concentration of 10 µM, and they displayed lower cytotoxicity than 4. The structures were determined by different NMR techniques and HRMS experiments. This investigation revealed that OSMAC could serve as a useful method for enabling the activation of the silent genes in the microorganism and for the formation of previously unreported active secondary metabolites.

7.
Mol Oncol ; 2020 Jan 19.
Artigo em Inglês | MEDLINE | ID: mdl-31955515

RESUMO

NEK2 is associated with drug resistance in multiple cancers. Our previous studies indicated that high NEK2 confers inferior survival in multiple myeloma (MM); thus, a better understanding of the mechanisms by which NEK2 induces drug resistance in MM is required. In this study, we discovered that NEK2 enhances MM cell autophagy, and a combination of autophagy inhibitor chloroquine (CQ) and chemotherapeutic bortezomib (BTZ) significantly prevents NEK2-induced drug resistance in MM cells. Interestingly, NEK2 was found to bind and stabilize Beclin-1 protein but did not affect its mRNA expression and phosphorylation. Moreover, autophagy enhanced by NEK2 was significantly prevented by knockdown of Beclin-1 in MM cells, suggesting that Beclin-1 mediates NEK2-induced autophagy. Further studies demonstrated that Beclin-1 ubiquitination is decreased through NEK2 interaction with USP7. Importantly, knockdown of Beclin-1 sensitized NEK2-overexpressing MM cells to BTZ in vitro and in vivo. In conclusion, we identify a novel mechanism whereby autophagy is activated by the complex of NEK2/USP7/Beclin-1 in MM cells. Targeting the autophagy signaling pathway may provide a promising therapeutic strategy to overcome NEK2-induced drug resistance in MM.

8.
Clin Exp Pharmacol Physiol ; 47(3): 459-465, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31663629

RESUMO

Cholangiocarcinoma is an aggressive malignancy with rapid invasion, metastasis and poor prognosis, however, the mechanism mediating its cholangiocarcinoma development needs further investigation. Here, we demonstrate that decreased miR-138 in tumor tissues is related to the poor prognosis in patients, and that miR-138 mediates sorafenib-induced cell survival in cholangiocarcinoma cells. Moreover, miR-138 negatively regulates SOX4 expression by specifically targeting its 3' untranslated region (3' UTR). As per our results, overexpression of SOX4 reversed sorafenib-induced changes in cell viability and apoptosis. Furthermore, the elevated levels of SOX4 in the tumor tissues that correlated with poor prognosis. Overall, the present study reveals that miR-138/SOX4 is involved in sorafinib-mediated cell survival in cholangiocarcinoma cells, and is associated with poor prognosis.

9.
Nat Biotechnol ; 38(1): 76-83, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31819261

RESUMO

Pharmaceutically important polyketides such as avermectin are mainly produced as secondary metabolites during the stationary phase of growth of Streptomyces species in fermenters. The source of intracellular metabolites that are funneled into polyketide biosynthesis has proven elusive. We applied multi-omics to reveal that intracellular triacylglycerols (TAGs), which accumulates in primary metabolism, are degraded during stationary phase. This process could channel carbon flux from both intracellular TAGs and extracellular substrates into polyketide biosynthesis. We devised a strategy named 'dynamic degradation of TAG' (ddTAG) to mobilize the TAG pool and increase polyketide biosynthesis. Using ddTAG we increased the titers of actinorhodin, jadomycin B, oxytetracycline and avermectin B1a in Streptomyces coelicolor, Streptomyces venezuelae, Streptomyces rimosus and Streptomyces avermitilis. Application of ddTAG increased the titer of avermectin B1a by 50% to 9.31 g l-1 in a 180-m3 industrial-scale fermentation, which is the highest titer ever reported. Our strategy could improve polyketide titers for pharmaceutical production.

10.
Accid Anal Prev ; 134: 105334, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31689573

RESUMO

It has been widely agreed that it is risky for patients with diabetes to drive during hypoglycemia. However, driving during non-hypoglycemia may also bring certain safety hazards for some patients with diabetes. Based on previous studies on diabetes-related to early aging effect, as well as gender differences in health belief and driving behavior, we have hypothesized that middle-aged male drivers with type 2 diabetes, compared with the control healthy ones, may experience a decline in driving performance without awareness. And the decline is caused by impaired perceptual and cognitive driving-related functions. To verify these hypotheses, we recruited 56 non-professional male drivers aged between 40 and 60 (27 patients with type 2 diabetes and 29 healthy controls) to perform a simulated car-following task and finish behavioral tests of proprioception, visual search, and working memory abilities during non-hypoglycemia. They also reported their hypoglycemia experience and perceived driving skills. We found that the patients had equal confidence in their driving skills but worse driving performance as shown in larger centerline deviation (t = 2.83, p = .006), longer brake reaction time (t = 3.77, p = .001) and shorter minimum time-to-collision (t = -3.27, p = .002). Such between-group differences in driving performance could be fully mediated by proprioception, visual search ability, and working memory capacity but not by hypoglycemia experience. Regarding the effect sizes of the mediation, the visual search ability played the most important role, and then followed the working memory and the proprioception. This initial study provides original and first-hand evidence demonstrating that the middle-aged male drivers with type 2 diabetes have deteriorated driving performance, but they are unaware of it. We will also discuss the possible measures to identify people of the highest risk and improve their safety awareness by using the findings of the current study.


Assuntos
Condução de Veículo/psicologia , Cognição/fisiologia , Diabetes Mellitus Tipo 2/complicações , Autoimagem , Estudos de Casos e Controles , Simulação por Computador , Humanos , Masculino , Memória de Curto Prazo/fisiologia , Pessoa de Meia-Idade , Tempo de Reação/fisiologia
11.
Anal Chim Acta ; 1094: 99-105, 2020 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-31761052

RESUMO

An ultrasensitive fluorescence method for early diagnosis of lung cancer via Nafion-initiated atom transfer radical polymerization (ATRP) is reported, in this paper. In the proposed method, thiolated peptide nucleic acid (PNA) is modified to amino magnetic beads (MBs) via a cross-linking agent to specifically capture target DNA (tDNA), and the initiator (Nafion) of ATRP is attached to PNA/DNA heteroduplexes based on the phosphate groups of the tDNA and sulfonate groups of Nafion via phosphate-Zr4+-sulfonate chemistry. Nafion as a macroinitiator of ATRP possesses multiple C-F active sites to initiate polymerization, and numerous polymeric chains that significantly amplify the fluorescent signal are formed. Under optimal conditions, a good linear relationship is obtained in the range of 0.1 nM-0.1 fM with correlation coefficients of 0.9975, and the detection limit is as low as 35.5 aM (∼214 molecules). The proposed strategy has several advantages of simplicity, cost-effectiveness, selectivity and sensitivity. More importantly, the anti-interference results demonstrate that the proposed Nafion-initiated ATRP strategy has great potential in bioanalytical applications.

13.
Oncol Lett ; 18(6): 6108-6116, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31788085

RESUMO

Intra-tumor heterogeneity (ITH) is one of the most important causes of therapy resistance, which eventually leads to the poor outcomes observed in patients with glioma. Mutant-allele tumor heterogeneity (MATH) values are based on whole-exon sequencing and precisely reflect genetic ITH. However, the significance of MATH values in predicting glioma recurrence remains unclear. Information of patients with glioma was obtained from The Cancer Genome Atlas database. The present study calculated the MATH value for each patient, analyzed the distributions of MATH values in different subtypes and investigated the rates of clinical recurrence in patients with different MATH values. Gene enrichment and Cox regression analyses were performed to determine which factors influenced recurrence. A nomogram table was established to predict 1-, 2- and 5-year recurrence probabilities. MATH values were increased in patients with glioma with the wild-type isocitrate dehydrogenase (NADP(+)) (IDH)1/2 (IDH-wt) gene (P=0.001) and glioblastoma (GBM; P=0.001). MATH values were negatively associated with the 2- and 5-year recurrence-free survival (RFS) rates in patients with glioma, particularly in the IDH1/2-wt and GBM cohorts (P=0.001 and P=0.017, respectively). Furthermore, glioma cases with different MATH levels had distinct patterns of gene mutation frequencies and gene expression enrichment. Finally, a nomogram table that contained MATH values could be used to accurately predict the probabilities of the 1-, 2- and 5-year RFS of patients with glioma. In conclusion, the MATH value of a patient may be an independent predictor that influences glioma recurrence. The nomogram model presented in the current study was an appropriate method to predict 1-, 2- and 5-year RFS probabilities in patients with glioma.

14.
Synth Syst Biotechnol ; 4(4): 173-179, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31667367

RESUMO

Microbes serve as the most important resource for drug discovery. During our screening for bioactive compounds from our natural products library, a pathogenic fungus, Microdochium majus strain 99049, from wheat was selected for further investigation. A new alkaloid named brocaeloid D (1), together with six previously characterized compounds (2-7) were identified. Compound 1 belongs to 4-oxoquinoline with C-2 reversed prenylation and a succinimide substructure. All the structures of these newly isolated compounds were determined by different means in spectroscopic experiments. The absolute configurations of 1 was further deduced from comparison of its CD spectrum with that of known compound 2. The bioactivities of these identified compounds were evaluated against several pathogenic microorganisms and cancer cell lines. Compounds 1-5 showed activity against HUH-7 human hepatoma cells with IC50 values of 80 µg/mL. Compound 6 showed mild activity against HeLa cells (IC50 = 51.9 µg/mL), weak anti-MTB activity (MIC = 80  µg/mL), and moderate anti-MRSA activity (MIC = 25 µg/mL), and compound 7 showed weak anti-MRSA activity (MIC = 100 µg/mL).

15.
Org Lett ; 21(24): 9852-9855, 2019 Dec 20.
Artigo em Inglês | MEDLINE | ID: mdl-31774293

RESUMO

The development of new methods to achieve the direct synthesis of bioactive organic molecules is always an important topic in organic synthesis. We hereby demonstrate that N-methoxyamide is an excellent amino source in the iridium-catalyzed intermolecular C-H amination reaction. The linkage of two bioactive organic molecules can be well achieved with this new protocol. More than 20 examples of decorated bioactive compounds were reported, which can facilitate the discovery of new bioactive molecules.

16.
J Inflamm (Lond) ; 16: 21, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31632200

RESUMO

Qihong Que and colleagues found that liraglutide exhibited anti-inflammatory activity through the activation of the PKA/CREB pathway in an OA rat model. We believe there was a flaw in this research. In their first experiment, the sacrifice time of the 10 rats in the control group has not been stated. And when the rats in the OA-1, OA-5, OA-10, OA-20 and OA-28 groups were sacrificed, they were in different weeks of age. If the rats in the control group were compared to the rats in the OA-1, OA-5, OA-10, OA-20 and OA-28 groups respectively, the results may be biased due to differences in the week age of the rats. We believe that addressing this issue could further increase the value of their study.

17.
Hum Factors ; : 18720819880646, 2019 Oct 16.
Artigo em Inglês | MEDLINE | ID: mdl-31618105

RESUMO

OBJECTIVE: To test the network disentangling model for explaining air traffic controllers' (ATCos) conflict resolution performance. The network rigidity index (NRI), and the steps to break the relational complexity network following a central-available-node-first rule, was hypothesized to explain the overall task demand, whereas marginal-effort-decrease rule was expected to explain the actual operational outcome. BACKGROUND: Understanding the conflict resolution process of ATCos is important for aviation safety and efficiency. However, linear models are insufficient. We proposed a new model that ATCos behavior can be largely considered as a process to break the relational complexity network, in which nodes represent the aircraft while links represent the cognitive complexity to understand the aircraft dyad relationship. METHOD: Twenty-one professional ATCos completed 27 conflict resolution scenarios that varied in the NRI and other control variables. Multilevel regression analyses were performed to understand the influence of the NRI on the number of interventions, mental workload, and unresolved rate. A cross-validation was performed to evaluate the predictive power of the model. RESULTS: NRI influenced ATCos intervention number in a curvilinear manner, which further leads to ATCo's mental workload. The deviance between the number of interventions and the NRI was strongly linked with unresolved rate. Cross-validation suggests that the models predictions are robust. CONCLUSION: The network disentangling model provides a useful theory-driven way to explain controllers' conflict resolution workload and other important performance outcomes such as intervention probability. APPLICATION: The proposed model can potentially be used for workload management, sector design, and intelligent decision support tool development.

18.
Stress ; : 1-9, 2019 Sep 27.
Artigo em Inglês | MEDLINE | ID: mdl-31532278

RESUMO

Academic stress is a common long-term stress among the student population and is known to impact working memory within the frontoparietal attention network. Perceived control is an individual variation that may play a buffering role between stress and overall adjustment. In this study, we addressed the moderating effects of perceived control between academic stress and working memory. Fifty-nine male college students participated in the study. Academic stress and perceived control were assessed before participants completed a working memory (n-back) task. Event-related potentials (ERPs) including P2 and P3 were analyzed to examine the attention and maintenance processes of working memory. A moderating effect of perceived control on the relationship between academic stress and working memory was found. For students with low levels of perceived control, academic stress was negatively associated with P2 amplitudes at the high workload (3-back) task, suggesting a negative impact on attention process of working memory. In contrast, academic stress did not affect students with high and moderate levels of perceived control. The results indicate that perceived control may serve as a buffer to protect the cognitive function from the disruption of academic stress.

19.
ACS Appl Mater Interfaces ; 11(41): 37822-37832, 2019 Oct 16.
Artigo em Inglês | MEDLINE | ID: mdl-31550118

RESUMO

Sphere-like Bi5O7I (BOI) doped with La (L-BOI) samples were prepared by a solvothermal method followed by calcination at 450 °C for 2 h. Au nanoparticles were loaded on 6% La-doped Bi5O7I (2%A-6%L-BOI) microspheres by a room-temperature chemical reduction method. The UV-vis absorption spectra show that the L-BOI and 2%A-6%L-BOI samples have a strong visible-light absorption in comparison with the pure BOI. The electron paramagnetic resonance results indicate that the number of oxygen vacancies in L-BOI samples is increased with an increasing amount of the La dopant. The band structure of the prepared photocatalysts is investigated by confirming the positions of the valence band (VB) measured by XPS-VB and the Fermi level computed by density functional theory, respectively. NO is selected as a target gaseous pollutant to confirm the influence of La doping and the plasmonic effect of Au nanoparticles on the photocatalytic activity of BOI microspheres. The 2%A-6%L-BOI sample exhibits an enhanced photocatalytic performance compared to BOI, L-BOI, and A-BOI photocatalysts under visible-light irradiation. Interestingly, the 2%A-6%L-BOI sample also can reduce the amount of intermediate NO2 during the NO removal process. The enhanced photocatalytic efficiency of the 2%A-6%L-BOI photocatalyst is profited from the synergy of La-ion doping, oxygen vacancy, and the surface plasmon resonance effect of Au nanoparticles. Based on the results of trapping experiments and electron spin resonance spectroscopy tests, h+, e-, and •O2- were involved in the NO oxidative removal.

20.
Org Lett ; 21(18): 7333-7336, 2019 Sep 20.
Artigo em Inglês | MEDLINE | ID: mdl-31502456

RESUMO

The Rh(III)-catalyzed amidation of C(sp2)-H bonds has been reported by employing the N-methoxyamide as a novel amino source. An excellent level of functional group tolerance can be achieved when N-methoxyamide derivatives are used as the amidating reagents. Importantly, several known bioactive compounds such as Aminalon, Pregabalin, Gabapentin, and Probenecid can be transformed to effective amidating reagents, as a way to facilitate the development of new bioactive molecules.

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