Current Issue : October - December Volume : 2018 Issue Number : 4 Articles : 6 Articles
The preparation of 5-methylene-thiohydantoins using solid-phase synthesis is reported\nin this paper. After sulfonylation of immobilized Ser (t-Bu)-OH with 4-nitrobenzenesulfonyl\nchloride followed by alkylation with various bromoketones, the 4-Nos group was removed and\nthe resulting polymer-supported �±-acylamino ketones reacted with Fmoc-isothiocyanate. Cleavage\nof the Fmoc protecting group was followed by the spontaneous cyclative cleavage releasing the\n5-methylene-thiohydantoin derivatives from the polymer support. Reduction with triethylsilane\n(TES) yielded the corresponding 5-methyl-thiohydantoins. When Fmoc-isothiocyanate was replaced\nwith alkyl isothiocyanates, the trifluoroacetic acid (TFA) mediated cleavage from the polymer support,\nwhich was followed by the cyclization reaction and the imidazo[2,1-b]thiazol-4-iums were obtained.\nTheir conversion in deuterated dimethylsulfoxide led to imidazole-2-thiones....
Herein, we have synthesized and characterized a new benzimidazole-derived ââ?¬Å?BnIââ?¬Â\nligand and its copper(II) complex, [Cu(BnI)2], 1, and zinc(II) complex, [Zn(BnI)2], 2, using elemental\nanalysis and various spectroscopic techniques. Interaction of complexes 1 and 2 with the\nbiomolecules viz. HSA (human serum albumin) and DNA were studied using absorption titration,\nfluorescence techniques, and in silico molecular docking studies. The results exhibited the\nsignificant binding propensity of both complexes 1 and 2, but complex 1 showed more avid\nbinding to HSA and DNA. Also, the nuclease activity of 1 and 2 was analyzed for pBR322 DNA,\nand the results obtained confirmed the potential of the complexes to cleave DNA. Moreover, the\nmechanistic pathway was studied in the presence of various radical scavengers, which revealed\nthat ROS (reactive oxygen species) are responsible for the nuclease activity in complex 1, whereas\nin complex 2, the possibility of hydrolytic cleavage also exists. Furthermore, the cytotoxicity of the\nligand and complexes 1 and 2 were studied on a panel of five different human cancer cells, namely:\nHepG2, SK-MEL-1, HT018, HeLa, and MDA-MB 231, and compared with the standard drug,\ncisplatin. The results are quite promising against MDA-MB 231 (breast cancer cell line of 1), with an\nIC50 value that is nearly the same as the standard drug. Apoptosis was induced by complex 1 on\nMDA-MB 231 cells predominantly as studied by flow cytometry (FACS). The adhesion and\nmigration of cancer cells were also examined upon treatment of complexes 1 and 2. Furthermore,\nthe in vivo chronic toxicity profile of complexes 1 and 2 was also studied on all of the major organs\nof the mice, and found them to be less toxic. Thus, the results warrant further investigations of\ncomplex 1....
Benzal derivatives were synthesized by crossed aldol. Benzalacetone synthesis was done by crossed aldol condensation between benzaldehyde and acetone with 1:1 mol ratio, while dibenzalacetone in 2:1 mol ratio. Benzalacetone derivatives were synthesized by replacing benzaldehyde with its derivatives, i.e. anisaldehyde, salicylacetone, cinnamaldehyde and p- hydroxyl benzalacetone. The mono derivatives and di derivatives were synthesized by changing the concentration of benzaldehyde. The synthesized compounds showed good antibacterial activity. The antibacterial activity was determined by agar well diffusion method against E. coli and Bacillus subtilis for all benzal derivatives and its was found that mono salicylalacetone exhibited highest antibacterial activity against B. subtilis and least activity was produced by p-hydroxyl benzalacetone for both E. coli and B. subtilis....
A series of novel 1-substituted 7-azaisatin derivatives synthesized from 7-azaindole by oxidation with N bromosuccinamide further involves incorporation of isonicotino- hydrazide with 7-aza isatin then treated with various alky halides to give titled compounds and screened for antimicrobial activity. In view of the antimicrobial property of this pharmacophore it was visualized that its combined effect with an active moiety may result in increased antimicrobial activity. All the synthesized titled compounds exhibited excellent to moderate antimicrobial activity against Bacillus subtilis, Staphylococcus aureus, Proteus vulgaris, Escherichia coli and two fungal strains Candida albicans, Aspergillus niger....
The design, synthesis, and development of novel non-steroidal anti-inflammatory drugs (NSAIDs) with better activity and lower\nside effects are respectable area of research. Novel Diclofenac Schiff �s bases (M1, M2, M4, M7, and M8) were designed and\nsynthesized, and their respective chemical structures were deduced using various spectral tools (IR, 1HNMR, 13CNMR, and MS).\nThe compounds were synthesized via Schiff �s condensation reaction and their anti-inflammatory activity was investigated applying\nthe Carrageenan-induced paw edema model against Diclofenac as positive control. Percentage inhibition of edema indicated that\nall compounds were exhibiting a comparable anti-inflammatory activity as Diclofenac. Moreover, the anti-inflammatory activity\nwas supported via virtual screening usingmolecular docking study. Interestingly compound M2 showed the highest in vivo activity\n(61.32% inhibition) when compared to standard Diclofenac (51.36% inhibition) as well as the best binding energy score (-10.765)\nand the virtual screening docking score (-12.142)....
Polycaprolactone (PCL) is drawing increasing attention in the field of medical 3D printing and tissue engineering because of its\nbiodegradability. This study developed polycaprolactone prepolymers that can be cured using visible light.Three PCL acrylateswere\nsynthesized: polycaprolactone-530 diacrylate (PCL530DA), glycerol-3 caprolactone triacrylate (Glycerol-3CL-TA), and glycerol-6\ncaprolactone triacrylate (Glycerol-6CL-TA). PCL530DA has two acrylates, whereas Glycerol-3CL-TA and Glycerol-6CL-TA have\nthree acrylates. The Fourier transform infrared and nuclear magnetic resonance spectra suggested successful synthesis of all PCL\nacrylates. All are liquid at room temperature and can be photopolymerized into a transparent solid after exposure to 470nm\nblue LED light using 1% camphorquinone as photoinitiator and 2% dimethylaminoethyl methacrylate as coinitiator.The degree of\nconversion for all PCL acrylates can reach more than 80% after 1 min of curing.The compressivemodulus of PCL530DA, Glycerol-\n3CL-TA, and Glycerol-6CL-TA is 65.7�±12.7, 80.9�±6.1, and 32.1�±4.1MPa, respectively, and their compressive strength is 5.3�±0.29,\n8.3 �± 0.18, and 3.0 �± 0.53MPa, respectively.Thus, all PCL acrylates synthesized in this study can be photo polymerized and because\nof their solid structure and low viscosity, they are applicable to soft tissue engineering and medical 3D printing....
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