Machine learning-based classification of structured light modes under turbulence and eavesdropping effects.

This paper considers the classification of multiplexed structured light modes, aiming to bolster communication reliability and data transfer rates, particularly in challenging scenarios marked by turbulence and potential eavesdropping. An experimental free-space optic (FSO) system is established to transmit 16 modes [8-ary Laguerre Gaussian (LG) and 8-ary superposition LG (Mux-LG) mode patterns] over a 3-m FSO channel, accounting for interception threats and turbulence effects. To the best of authors' knowledge, this paper is the first to consider both factors concurrently. We propose four machine/deep learning algorithms-artificial neural network, support vector machine, 1D convolutional neural network, and 2D convolutional neural network-for classification purposes. By fusing the outputs of these methods, we achieve promising classification results exceeding 92%, 81%, and 69% in cases of weak, moderate, and strong turbulence, respectively. Structured light modes exhibit significant potential for a variety of real-world applications where reliable and high-capacity data transmission is crucial.

Sonophoresis-assisted transdermal delivery of antimigraine-loaded nanolipomers: Radio-tracking, histopathological assessment and in-vivo biodistribution study.

Migraine is a disabling neurovascular polygenic disorder affecting life quality with escorted socioeconomic encumbrances. Herein, we investigated the consolidated amalgamation of passive lipomer approach alongside active sonophoresis assisted transdermal delivery of zolmitriptan (ZT) using high frequency ultrasound pre-treatment protocol to mitigate migraine attacks. A modified nanoprecipitation technique was utilized to prepare zolmitriptan loaded lipomers (ZTL) adopting 23 factorial design. Three factors were scrutinized namely lipid type, ZT: lipid ratio and ZT: Gantrez® ratio. The prepared systems were characterized regarding particle size, zeta potential, polydispersity index, entrapment efficiency and in-vitro release studies. The best achieved ZTL system was evaluated for ZT- Gantrez® intermolecular interactions, drug crystallinity, morphology, ex-vivo permeation and histopathological examination. Finally, a comparative in-vivo biodistribution study through radiotracking technique using Technetium-99 m was adopted. L2 was the best-achieved ZTL system with respect to spherical particle size (390.7 nm), zeta-potential (-30.8 mV), PDI (0.2), entrapment efficiency (86.2%), controlled release profile, flux (147.13 µg/cm2/hr) and enhancement ratio (5.67). Histopathological studies proved the safety of L2 system upon application on skin. L2 revealed higher brain Cmax (12.21 %ID/g), prolonged brain MRT (8.67 hr), prolonged brain 0.23 hr), significantly high relative bioavailability (2929.36%) and similar brain Tmax (0.5 hr) compared to I.V. route with higher brain/blood ratio. Thus, sonophoresis assisted transdermal delivery of ZTL offers a propitious alterative to alleviate migraine symptoms.

In vitro biological activity of cobalt(II) complexes with salicylaldimine ligands in microbial and cancer cells.

Background: More studies using cobalt complexes as drugs are needed. Results: The drug action of two cobalt salicylaldimines was determined. The complexes and amphotericin B (20 mg/ml) inhibited Candida albicans at 9-15 and 21 mm. This concentration of both ligands inhibited Staphylococcus aureus at 10 mm and one ligand inhibited Escherichia coli at 9 mm, but the complexes and ampicillin inhibited four bacteria at 9-20 and 21-26 mm. The ligands were inactive against cancer and normal cells, but the complexes and doxorubicin provided IC50 values of 28.18-54.19 and 9.66 µM against MCF-7 cells and 15.76-20.49 and 36.42 µM against BHK cells. Conclusion: The ligands' activity was much improved by complexation, although they remained substandard.

Real-Time Detection of Intruders Using an Acoustic Sensor and Internet-of-Things Computing.

Modern home automation systems include features that enhance security, such as cameras and radars. This paper proposes an innovative home security system that can detect burglars by analyzing acoustic signals and instantly notifying the authorized person(s). The system architecture incorporates the concept of the Internet of Things (IoT), resulting in a network and a user-friendly system. The proposed system uses an adaptive detection algorithm, namely the "short-time-average through long-time-average" algorithm. The proposed algorithm is implemented by an IoT device (Arduino Duo) to detect people's acoustical activities for the purpose of home/office security. The performance of the proposed system is evaluated using 10 acoustic signals representing actual events and background noise. The acoustic signals were generated by the sounds of keys shaking, the falling of a small object, the shrinking of a plastic bag, speaking, footsteps, etc. The effects of different algorithms' parameters on the performance of the proposed system have been thoroughly investigated.

Strain FBG-Based Sensor for Detecting Fence Intruders Using Machine Learning and Adaptive Thresholding.

This paper demonstrates an intruder detection system using a strain-based optical fiber Bragg grating (FBG), machine learning (ML), and adaptive thresholding to classify the intruder as no intruder, intruder, or wind at low levels of signal-to-noise ratio. We demonstrate the intruder detection system using a portion of a real fence manufactured and installed around one of the engineering college's gardens at King Saud University. The experimental results show that adaptive thresholding can help improve the performance of machine learning classifiers, such as linear discriminant analysis (LDA) or logistic regression algorithms in identifying an intruder's existence at low optical signal-to-noise ratio (OSNR) scenarios. The proposed method can achieve an average accuracy of 99.17% when the OSNR level is <0.5 dB.

Brain targeting of zolmitriptan via transdermal terpesomes: statistical optimization and in vivo biodistribution study by 99mTc radiolabeling technique.

Zolmitriptan (ZT) is a potent second generation triptan, commonly administered to alleviate migraine attacks. ZT suffers various limitations; massive hepatic first pass metabolism, P-gp efflux transporters susceptibility, and limited (≈40%) oral bioavailability. Transdermal route of administration could be explored to enhance its bioavailability. A 23.31 full factorial design was constructed to developed twenty-four ZT loaded terpesomes via thin film hydration technique. The influence of drug: phosphatidylcholine ratio, terpene type, terpene concentration and sodium deoxycholate concentration on the characterization of the developed ZT-loaded terpesomes was assessed. Particle size (PS), zeta potential (ZP), ZT entrapment efficiency (EE%), drug loading (DL%) and drug released percentages after 6 h (Q6h) were the selected dependent variables. Further morphological, crystallinity, and in-vivo histopathological studies were conducted for the optimum terpesomes (T6). 99mTc-ZT and 99mTc-ZT-T6 gel were radio-formulated for in-vivo biodistribution studies in mice following transdermal application of 99mTc-ZT-T6 gel, relative to 99mTc-ZT oral solution. T6 terpesomes [comprising ZT and phosphatidylcholine (1:15), cineole (1% w/v) and sodium deoxycholate (0.1% w/v)] were optimum with respect to spherical PS (290.2 nm), ZP (-48.9 mV), EE% (83%), DL% (3.9%) and Q6h (92.2%) with desirability value of 0.85. The safety of the developed T6 terpesomes was verified by the in-vivo histopathological studies. 99mTc-ZT-T6 gel showed maximum brain concentration (5 ± 0.1%ID/ g) with highest brain to blood ratio of 1.92 ± 0.1 at 4 h post transdermal application. Significant improvement of ZT brain relative bioavailability (529%) and high brain targeting efficiency (315%) were revealed with 99mTc-ZT-T6 gel, which confirmed successful ZT delivery to the brain. Terpesomes could be safe, successful systems capable of improving ZT bioavailability with high brain targeting efficiency.

Self-Assembling Lecithin-Based Mixed Polymeric Micelles for Nose to Brain Delivery of Clozapine: In-vivo Assessment of Drug Efficacy via Radiobiological Evaluation.

Purpose: The research objective is to design intranasal brain targeted CLZ loaded lecithin based polymeric micelles (CLZ- LbPM) aiming to improve central systemic CLZ bioavailability. Methods: In our study, intranasal CLZ loaded lecithin based polymeric micelles (CLZ- LbPM) were formulated using soya phosphatidyl choline (SPC) and sodium deoxycholate (SDC) with different CLZ:SPC:SDC ratios via thin film hydration technique aiming to enhance drug solubility, bioavailability and nose to brain targeting efficiency. Optimization of the prepared CLZ-LbPM using Design-Expert® software was achieved showing that M6 which composed of (CLZ:SPC: SDC) in respective ratios of 1:3:10 was selected as the optimized formula. The optimized formula was subjected to further evaluation tests as, Differential Scanning Calorimetry (DSC), TEM, in vitro release profile, ex vivo intranasal permeation and in vivo biodistribution. Results: The optimized formula with the highest desirability exhibiting (0.845), small particle size (12.23±4.76 nm), Zeta potential of (-38 mV), percent entrapment efficiency of > 90% and percent drug loading of 6.47%. Ex vivo permeation test showed flux value of 27 µg/cm².h and the enhancement ratio was about 3 when compared to the drug suspension, without any histological alteration. The radioiodinated clozapine ([131I] iodo-CLZ) and radioiodinated optimized formula ([131I] iodo-CLZ-LbPM) were formulated in an excellent radioiodination yield more than 95%. In vivo biodistribution studies of [131I] iodo-CLZ-LbPM showed higher brain uptake (7.8%± 0.1%ID/g) for intranasal administration with rapid onset of action (at 0.25 h) than the intravenous formula. Its pharmacokinetic behavior showed relative bioavailability, direct transport percentage from nose to brain and drug targeting efficiency of 170.59%, 83.42% and 117% respectively. Conclusion: The intranasal self-assembling lecithin based mixed polymeric micelles could be an encouraging way for CLZ brain targeting.

Effect of Ramadan fasting on chronic inflammation markers and gut bacterial endotoxins among Egyptian hemodialysis patients.

BACKGROUND: Chronic kidney disease (CKD) is associated with a state of chronic inflammation. This study aimed to investigate effects of Ramadan fasting on the markers of chronic inflammation and gut bacterial endotoxin levels in maintenance hemodialysis. METHOD: A prospective self-controlled observational study included 45 patients. Serum levels of High Sensitive CRP (hsCRP), indoxyl sulfate, and trimethylamine-n-levels were measured within a week before and a week after Ramadan fasting. RESULTS: Twenty-seven patients have fasted more than 15 days (29 ± 2.2 days). The levels of high sensitive C-reactive protein (hsCRP) (median of 62 mg/L vs. 91 mg/L), trimethylamine-n-oxide (TMAO) (median of 4.5 µmoL/L vs. 17 µmoL/L), platelet-to-lymphocyte ratio (PLR) (mean of 98.9 mg/L vs. 111.8 mg/L) and neutrophil-to-lymphocyte ratio (NLR) (median of 1.56 vs. 1.59) were significantly lower after Ramadan fasting with p < 0.001, p < 0.001, p < 0.001, and p = 0.04, respectively. CONCLUSION: A beneficial effect of Ramadan fasting on levels of bacterial endotoxins and markers of chronic inflammation in hemodialysis patients was observed.

Cod liver oil nano-structured lipid carriers (Cod-NLCs) as a promising platform for nose to brain delivery: Preparation, in vitro optimization, ex vivo cytotoxicity & in vivo biodistribution utilizing radioiodinated zopiclone.

Nano-structured lipid carriers containing zopiclone were prepared as a targeted drug delivery system to convey zopiclone directly to brain via nasal route. Nano-structured lipid carriers were constructed adopting hot emulsification-ultrasonication method using palmitic acid in place of the solid lipid, cod liver oil as liquid lipid, and poloxamer 407 as a surfactant. A three-factor three-level central composite face-centered design was used to optimize the formulated nano-structured lipid carriers. The independent factors were lipid amount (X1), surfactant amount (X2), and sonication time (X3). The examined responses were entrapment efficiency (EE,Y1,%), particle size (PS,Y2,nm), zeta potential(mV), polydispersity index(PDI,Y3), in vitro release(Q8h,Y4,%) and dissolution efficiency (DE,Y5,%). The optimum formula showed high entrapment efficiency of 94.31% ± 2.44, in vitro drug release of 83.89% ± 1.77 with dissolution efficiency equals 88.63% ± 2.01, small particle size of 71.27 nm ± 13.57 and low polydispersity index 0.097 ± 0.15. In vivo biodistribution in mice was evaluated by a radiobiological technique using radioiodinated zopiclone([131I]iodo-ZP). Results revealed the superiority of the intranasal route to deliver zopiclone directly to brain faster and higher brain uptake (6.9 ± 1.02%ID/g at 5 min post-administration). The current study confirmed that intranasal administration of nano-structured lipid carriers had great potential as an effective tool for targeted brain zopiclone delivery for insomnia treatment.

New iron(III) complexes with 2-formylpyridine thiosemicarbazones: Synthetic aspects, structural and spectral analyses and cytotoxicity screening against MCF-7 human cancer cells.

2-Formylpyridine thiosemicarbazone - iron (III) chelates [ F e L 2 ] C l • 2 H 2 O {L = L1 (C1) [HL 1  = 4-(4-Nitrophenyl)-1-((pyridin-2-yl)methylene)thiosemicarbazide] and L = L2 (C2) [HL 2  = 4-(2,5-Dimethoxyphenyl)-1-((pyridin-2-yl)methylene)thiosemicarbazide]} were prepared. The two ligand anions in each complex resulted in saturation of the iron coordination number and consequently the existence of these complexes as 1:1 electrolytes. As well, the iron in these complexes exhibits low-spin electronic configuration. X-ray crystallography of complex C1 indicated its triclinic crystal system and P 1 ‾ space group. In addition, it proved the ligation through a thiol sulfur atom and two nitrogen atoms of pyridine and azomethine groups. This is while the presence of two water molecules of crystallization in the complex structure was also indicated. The ligand HL 1 was selected for cytotoxicity screening against human MCF-7, A-549, HEPG-2 and HCT-116 cancer cells and the most enhanced activities were detected against the breast cells. Against these cells, the compounds HL 1 , HL 2 , C1 and C2 induced cytotoxicity, respectively, with IC50 values of 52.4, 145.4, 34.3 and 62.0 µM. However, against the healthy BHK cells, HL 1 and HL 2 caused cytotoxicity, respectively, with IC50 values of 54.8 and 110.6 µM and cytotoxicity with percent viabilities of 56.7 and 55.4% of the BHK cells by the complexes (137.4 µM of C1 and 131.9 µM of C2) was determined. These activities against MCF-7 cells are less significant compared with the measured value for doxorubicin. But this standard is more toxic to normal cells than the thiosemicarbazones (IC50 (doxorubicin) = 9.66 µM against MCF-7 cells and 36.42 µM against BHK cells).

Synthesis, Solid State Structure, and Cytotoxic Activity of a Complex Dimer of Yttrium with Anthranilic Acid against Cancer Cells.

This paper presents the synthesis and isolation of a new binuclear complex of yttrium with anthranilic acid (HA). The complex [Y2(HA)6(H2O)4] Cl6.2C2H5OH (C1) was obtained as single crystals that its X-ray analysis revealed its triclinic P-1 space group in addition to anti-prismatic geometry around each of the yttrium ions. In the complex, the anthranilic acid ligands are bidentate, zwitter ionic and neutral, and the yttrium ions' charge is only compensated by six chloride ions. The cytotoxicity of this complex against human breast cancer MDA-MB-231 cells, prostate cancer PC-3 cells, and bladder cancer T-24 cells was evaluated. This yttrium complex displayed more cytotoxic activity against the bladder cancer cells with an IC50 value of 307.7 µg/ml (223 µM). On the other hand, the activities of complex C1 against the MDA-MB-231 and PC-3 cells were less significant respectively with IC50 values of 1097 µg/ml (796 µM) and 921 µg/ml (669 µM).

Synthesis, X-ray structure and anticancer activity evaluation of a binuclear La(III) complex with anthranilic acid.

A binuclear La(III) complex {[La2(HA)4(H2O)4(C2H5OH)2Cl2]Cl4 (C1)} with 2-aminobenzoic acid (HA) was prepared from the ligand and heptahydrated lanthanum chloride. The complex was characterised by X-ray crystallography that revealed anti-prismatic geometry around both of the lanthanum. In the complex, the four 2-aminobenzoic acid ligands are zwitter ionic and the two lanthanum(III) ions net charge is only counterbalanced by chloride ions. The complex cytotoxicity was determined against human breast (MDA-MB-231), prostate (PC-3) and bladder (T-24) cancer cells. This complex afforded cytotoxicity towards the T-24 bladder cancer cells with an IC50 value of 383.5 µg/mL (319 µM). In contrary, activities by the lanthanum complex with IC50 values of 1124 µg/mL (934 µM) and 739 µg/mL (614 µM) were, respectively, shown against the MDA-MB-231 and PC-3 cancer cells. This means the complex is more cytotoxic against the T-24 cells, despite that its activity is less compared with activities shown by classical drugs.

Brain targeting efficiency of intranasal clozapine-loaded mixed micelles following radio labeling with Technetium-99m.

The research objective is to design intranasal (IN) brain targeted CLZ-loaded polymeric nanomicellar systems (PNMS) aiming to improve central systemic CLZ bioavailability. Direct equilibrium method was used to prepare CLZ-PNMS using two hydrophobic poloxamines; Tetronic® 904 (T904) and Tetronic® 701 (T701) and one hydrophilic poloxamer; Synperonic® PE/F127 (F127). Optimization is based on higher percent transmittance, solubilizing efficiency, and in vitro release after 24 h with smaller particle size was achieved using Design-Expert® software. The optimized formula was further evaluated via TEM, ex vivo nasal permeation in addition to in vivo biodistribution using radiolabeling technique of the optimized formula by Technetium-99m (99mTc). The optimized formula M5 has small size (217 nm) with relative high percentage of transmittance (97.72%) and high solubilization efficacy of 60.15-fold following 92.79% of CLZ released after 24 h. Ex vivo nasal permeation showed higher flux of 36.62 µg/cm2.h compared to 7.324 µg/cm2.h for CLZ suspension with no histological irritation. In vivo biodistribution results showed higher values of radioactivity percentage of the labeled optimized formula (99mTc-M5) in brain and brain/blood ratio following IN administration of 99mTc-M5 complex which were greater than their corresponding values following intravenous route. It is obvious that nasal delivery of CLZ-PNMS could be a promising way to improve central systemic CLZ bioavailability.

mmW Rotman Lens-Based Sensing: An Investigation Study.

A Rotman lens is a wideband true-time delay device. Due to its simplistic structure with wave/signal routing capabilities, it has been widely utilized as a beamforming device in numerous communication systems. Since the basic Rotman lens design incorporates multiple input, output, and dummy ports, in this study, and for the first time, we utilized a Rotman lens as a sensor. The main idea was to gather abundant information from available Rotman lens ports to obtain better sensing performance. The realized lens is optimized to work in the millimeter wave (mmW) band from 27 to 29 GHz with a focus on a central frequency of 28 GHz. The design has a footprint of 140 × 103 × 0.8 mm3. The polarity correlator was used to characterize the material under investigation.

Effect of Ramadan fasting on arterial stiffness parameters among Egyptian hypertensive patients with and without chronic kidney disease.

Arterial stiffness (AS) increases progressively in patients with chronic kidney disease (CKD). It is a strong predictor of cardiovascular and all-cause mortality. This study aims at evaluate of the effect of Ramadan fasting on AS parameters, augmentation index (AIx), and pulse wave velocity (PWV) in hypertensive patients with and without CKD. A cohort of 71 patients (mean age = 57.14 ± 14.5 years, 42 females and 29 males) were enrolled in this study; 34 with CKD and 37 without CKD. All patients had hypertension, while 25 patients had diabetes mellitus. Serum creatinine (Cr), serum urea, estimated glomerular filtration rate (eGFR) by CKD-EPI formula, brachial and central systolic blood pressure (BSP and CSP respectively), brachial and central diastolic blood pressure (BDP, CDP, respectively), AIx and PWV (measured by cuff based oscillometric method) were assessed before and after Ramadan fasting. In patients without CKD BSP, BDP, CSP, and CDP significantly decreased (P = 0.0001, 0.0001, 0.0001, and 0.0001, respectively). In patients with CKD BSP and CSP significantly decreased (P = 0.005 and 0.005), while BDP and CDP decreased, but the change was not statistically significant. AIx significantly decreased in patients without CKD (P = 0.0001, mean 36.24 before and 26.22 after Ramadan fasting), but did not significantly change in patients with CKD (P 0.381 mean 25.94 before and 25 after Ramadan fasting). PWV decreased in both groups, but the change was not significant. Serum Cr significantly increased (P = 0.03 mean 1.06 mg/dL before and 1.11 mg/dL after Ramadan fasting), while eGFR did not significantly decrease (P = 0.072, mean 69.73 mL/ min/1.73 m2 before and 67.3 mL/min/1.73 m2 after Ramadan fasting) in patients without CKD. Serum Cr significantly decreased (P 0.028 mean 1.93 mg/dL before and 1.87 mg/dL after Ramadan fasting) and eGFR significantly increased (P 0.006 mean 32.65 mL/min/1.73 m2 before and 34.68 mL/min/1.73 m2 after RF) in patients with CKD. Ramadan fasting is associated with improved peripheral and central blood pressure control in hypertensive patients with and without CKD. It is also associated with improved arterial compliance (decreased AIx) in hypertensive patients without CKD.

Zn(II) and Cd(II) thiosemicarbazones for stimulation/inhibition of kojic acid biosynthesis from Aspergillus flavus and the fungal defense behavior against the metal complexes' excesses.

The complexes {[ZnL1Cl] C1, [ZnL2Cl].0.5H2O C2, [CdL1Cl] C3, and [CdL2Cl] C4} were prepared from tridentate thiosemicarbazones {HL1 = 4-(3-nitrophenyl)-1-((pyridin-2-yl)methylene) thiosemicarbazide and HL2 = 4-(2,4-dimethoxyphenyl)-1-((pyridin-2-yl)methylene)thiosemicarbazide} and identified by elemental CHNS, spectroscopic {IR and UV-Vis.}, thermal and DMF solution electrical conductivity data. On another hand, kojic acid (KA) which represents important secondary metabolite with numerous hot spot applications was successfully biosynthesized from Aspergillus flavus and structurally analyzed by single crystal analysis. The Zn(II) complexes C1&C2 (0.3 mM) enhanced the KA biosynthesis by 70.87% and 42.26%, while 76.09% of C1 and 72.78% of C2 were absorbed by the fungal cells. The Cd(II) complexes C3&C4 at 0.3 mM inhibited KA production by 87.95% and 97.03% with Cd(II) consumption reaching to 40.09% & 37.3%, while 0.4 mM of C3&C4 resulted in 100% inhibition of kojic acid biosynthesis. Light microscopic analysis showed the fungal structural abnormalities and the cell antioxidant behavior was detected. These complexes could be highly applicable as new stimulators and inhibitors of kojic acid production.

Stabilized oral nanostructured lipid carriers of Adefovir Dipivoxil as a potential liver targeting: Estimation of liver function panel and uptake following intravenous injection of radioiodinated indicator.

PURPOSE: Adefovir dipivoxil (AD), a nucleoside reverse transcriptase inhibitor is effective against Hepatitis B virus. Its poor oral bioavailability leads to frequent administration causing severe adverse effects. Thereby the entrapment of AD within lipid nanoparticulate systems is a way of increasing AD oral bioavailability as a result of improving intestinal permeability with efficient liver-targeted delivery together with higher drug stability during storage. METHODS: AD-loaded nanostructured lipid carriers (AD-NLCs) were prepared via solvent emulsification diffusion technique adopting 24 full factorial design to study the effect of lipid percentage, presence of egg yolk lecithin, surfactant type and percentage on entrapment efficiency (E.E.%), particle size and percent in-vitro drug released after 8 h (Q8hrs). RESULTS: Formula (F12) showed E.E.% of 90.5 ± 0.2%, vesicle size of 240.2 ± 2.5 nm and Q8hrs of 58.55 ± 9.4% was selected as the optimum formula with desirability value of 0.757 based on highest EE%, lowest P.S. and Q8hrs. Further evaluation of the optimized formula using radioiodinated rose bengal (RIRB) in thioacetamide induced liver damage in Swiss Albino mice revealed a higher liver uptake of 22 ± 0.01% ID/g (percent injected dose/g organ) and liver uptake/Blood (T/B) ratio of 2.22 ± 0.067 post 2 h of I.V injection of RIRB compared to 9 ± 0.01% ID/g and 0.64 ± 0.017 in untreated group, respectively. CONCLUSION: NLCs could be successfully used as oral drug delivery carriers of the antiviral drug Adefovir Dipivoxil to the liver with higher stability and oral bioavailability. Graphical abstract.

Brain-targeting by optimized 99mTc-olanzapine: in vivo and in silico studies.

Purpose: Olanzapine (OLZ) is an atypical antipsychotic agent that is characterized by low brain porousness. The present work aimed to develop radiolabeled olanzapine (OLZ) without colloidal impurities and evaluate its biodistribution following intravenous (I.V.) and intranasal (I.N.) administration as a potential agent for brain diagnosis. Materials and methods: OLZ was radiolabeled with technetium-99m by using sodium dithionite as the reducing agent. Biodistribution of 99mTc-OLZ complex in mice following I.V. and I.N. administrations was examined. Furthermore, a molecular docking study was performed.Results: Sodium dithionite labeling procedure resulted in highest radiochemical yield (96.30 ± 0.09%) and in vitro stability in serum up to 8 h. Biodistribution study of 99mTc-OLZ complex showed high brain uptake following I.N. (6.2 ± 0.12% ID/g) and I.V. (5.5 ± 0.09% ID/g) at 0.5 and 1 h post administration (P.I.), respectively. Docking into two brain targets predicts higher affinity of 99mTc-OLZ than free OLZ. Additionally, docking to P-glycoproteins shows less affinity for the radiolabelled OLZ and hence it is expected to be associated with better brain exposure than free OLZ.Conclusion: These chemical and preliminary biological merits strongly suggest that the 99mTc-OLZ complex with new reducing agent could be used as a potential diagnostic agent for brain.

New acrylamide-sulfisoxazole conjugates as dihydropteroate synthase inhibitors.

New functionalized acrylamide derivatives bearing sulfisoxazole moiety were designed to target bacterial dihydropteroate synthase (DHPS). The in vitro antimicrobial activities of these compounds were assessed. The E-configuration of compound 5b was proved by single crystal X-ray analysis. Compounds 5g and 5h displayed double the activity of ampicillin against B. subtilis. Also, 5h was two times more active than gentamycin against E. coli. Interestingly, compounds 5f-g, 7c, 8a, 8c exhibited two folds the potency of amphotericin B against S. racemosum while 5h displayed three folds the activity of amphotericin B against S. racemosum. Most of the synthesized compounds showed superior activities to the parent sulfisoxazole and were non-toxic to normal cells. DHPS is confirmed to be a putative target for our compounds via antagonizing their antibacterial activity by the folate precursor (p-aminobenzoic acid) and product (methionine) on E. coli ATCC 25922. Docking experiments against DHPS rationalized the observed antibacterial activity. Additionally, compound 5g was evaluated as a selective targeting vector for 99mTc that showed a remarkable uptake and targeting ability towards the infection site that was induced in mice.

Synthesis, structural and antimicrobial studies of binary and ternary complexes of a new tridentate thiosemicarbazone.

A new thiosemicarbazone ligand was synthesized and characterized using spectroscopic techniques (UV-Vis and IR) and synchrotron x-ray powder diffraction. With M2+ = Mn2+, Zn2+ and Cd2+, coordination compounds of the type (M[L]2) were isolated. In the presence of sodium dithiocarbamate salts (NadiEtdtc.3H2O = sodium diethyldithiocarbamate trihydrate and Napipdtc = sodium piperidinedithiocarbamate), Zn2+ and Cd2+ were able to form ternary octahedral complexes where each metal binds a deprotonated (thiosemicarbazone) ligand, a monobasic dithiocarbamate ligand and a water molecule. In vitro biological evaluation tests of the free HL ligand and its metal complexes against selected fungal and bacterial cultures were performed. Compared with HL, the complexes displayed enhanced biological activities and ternary Zn (II) complexes displayed comparable antibacterial activities to the chloramphenicol standard.