@article {43671, title = {Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives}, journal = {European Journal of Medicinal Chemistry}, volume = {132}, year = {2017}, month = {MAY}, pages = {333-340}, type = {Article}, abstract = {

In the present study a series of 4-methyl-2-aryl-5-(2-aryl/benzyl thiazol-4-yl) oxazole (4a-v) have been synthesized and evaluated for their preliminary antitubercular, antimicrobial and cytotoxicity activity. Among all the synthesized compounds, 4v reported comparable activity against dormant M. tuberculosis H37Ra and M. bovis BCG strains with respect to standard drug rifampicin. The active compounds from the antitubercular study were further tested for anti-proliferative activity against HeLa, A549 and PANC-1 cell lines using MU assay and showed no significant cytotoxic activity at the maximum concentration evaluated. Further, the synthesized compounds were found to have potential antibacterial activities with MIC range of 2.1-26.8 mu g/mL. High potency, lower cytotoxicity and promising antimycobacterial activity suggested that these compounds could serve as good leads for further optimisation and development. (C) 2017 Elsevier Masson SAS. All rights reserved.

}, doi = {10.1016/j.ejmech.2017.03.065}, author = {Abhale, Yogita K. and Sasane, Amit V. and Chavan, Abhijit P. and Shekh, Saddam Husen and Deshmukh, Keshav K. and Bhansali, Sujit and Nawale, Laxman and Sarkar, Dhiman and Mhaske, Pravin C.} } @article {46314, title = {Synthesis of new 1,3,4-oxadiazole and benzothiazolylthioether derivatives of 4-arylmethylidene-3-substituted-isoxazol-5(4H)-one as potential antimycobacterial agents}, journal = {Medicinal Chemistry Research}, volume = {28}, year = {2019}, month = {NOV}, pages = {1873-1884}, type = {Article}, abstract = {

A new series of 4-[(substituted benzylidene)-3-[(5-(pyridine-4-yl)-1,3,4-oxadiazole-2-ylthio)-methyl]i soxazol-5(4H)-one (6a-g) and 4-(substituted benzylidene)-3-((benzo[d]thiazol-2-ylthio)methyl)isoxazol-5(4H)-one (8a-g) was synthesized. All the synthesized compounds were screened for antitubercular activity against Mycobacterium tuberculosis H37Ra (ATCC 25177) and Mycobacterium bovis BCG (ATCC 35743) and antibacterial activity against Escherichia coli (NCIM 2576), Pseudomonas flurescence (NCIM 2059), Staphylococcus aureus (NCIM 2602), Bacillus subtilis (NCIM 2162). Amongst the synthesized 1,3,4-oxadiazole and benzothiazoyl thioether derivatives, compounds 6b and 8b showed excellent antimycobacterial activity and compounds 6b, 8a, 8b, and 8d showed excellent antibacterial activity against all tested antibacterial strains. The synthesized compounds were further evaluated for their cytotoxic activity against the HCT 116 and HeLa cancer cell lines. The 1,3,4-oxadiazole and benzothiazoyl thioether derivatives 6a-g and 8a-g did not show cytotoxicity.

}, keywords = {1, 3, 4-Oxadiazole, antibacterial activity, Antitubercular activity, Benzothiazol, Isoxazol-5(4H)-one, Thioeteher}, issn = {1054-2523}, doi = {10.1007/s00044-019-02420-7}, author = {Chavan, Abhijit P. and Deshpande, Rujuta R. and Borade, Nandkumar A. and Shinde, Abhijit and Mhaske, Pravin C. and Sarkar, Dhiman and Bobade, Vivek D.} } @article {48165, title = {Synthesis and antimycobacterial screening of a novel series of alpha-amino acids containing thiazole linker}, journal = {ARKIVOC}, year = {2022}, type = {Article}, abstract = {

A small focused library of uncommon (S)-2-amino-3-(4-(((4-methyl-2-arylthiazol-5-yl)methyl)amino)phenyl) propanoic acid (5a-e) and (S)-2-amino-3-(4-(((2-arylthiazol-4-yl)methyl)amino)phenyl)propanoic acid (9a-d) derivatives have been efficiently synthesized by employing molecular simplification. The title compounds were screened for inhibitory activity against Mycobacterium tuberculosis H37Ra (MTB) and Mycobacterium bovis (BCG) strains. The cytotoxicity study was conducted against primary Human Umbilical Vein Endothelial Cells (HUVECs), on two different human tumor cells HeLa, and HCT 116 and was observed non-toxic to host cells.

}, keywords = {Amino acid, antibacterial activity, Cytotoxicity, Mycobacterium tuberculosis, synthesis, Thiazole}, issn = {1551-7004}, doi = {10.24820/ark.5550190.p011.831}, author = {Nalawade, Jitendra L. and Mhaske, Pravin C. and Shinde, Abhijit D. and Chavan, Abhijit P. and Abhale, Yogita K. and Sarkar, Dhiman and Bobade, Vivek D.} } @article {46623, title = {Synthesis of new thiazole and pyrazole clubbed 1,2,3-triazol derivatives as potential antimycobacterial and antibacterial agents}, journal = {Polycyclic Aromatic Compounds}, volume = {42}, year = {2022}, month = {JUL}, pages = {3216-3237}, type = {Article}, abstract = {

New series of 4-methyl-2-(4-substituted phenyl)-5-(4-((4-(4-substituted phenyl)-1H-1,2,3-triazol-1-yl)methyl)-1-phenyl-1H-pyrazol-3-yl)thiazole, 6a-t and 4-(1,3-diphenyl-1H-pyrazol-4-yl)-1-((1,3-diphenyl-1H-pyrazol-4-yl)methyl )-1H-1,2,3-triazole, 11a-o derivatives have been synthesized by applying copper-catalyzed [3 + 2] cycloaddition reaction. The newly synthesized 1,3-thiazolyl-pyrazolyl-1,2,3-triazole (6a-t) and bis-pyrazolyl-1,2,3-triazole (11a-o) derivatives were screened for in vitro antimycobacterial activity against M. Tuberculosis H37Ra dormant and active and antibacterial activity against four pathogenic bacteria, E. coli (NCIM 2576), P. flurescence (NCIM 2059), S. aureus (NCIM 2602) and B. subtilis (NCIM 2162). Compounds 6a, 6f, 6j, 11e and 11m showed good activity against M tuberculosis H37Ra Active strain, also compounds 6g, 6h, 11f, 11n and 11o showed good activity against M tuberculosis H37Ra Dormant strain. Compounds 6b, 6i, 6l, 6o, 6r, 11k, 11l and 11m showed good activity against B. subtilis with IC50 1.99-2.96 mu g/mL. The antibacterial activity of thiazolyl-pyrazolyl-1,2,3-triazole and bis-pyrazolyl-1,2,3-triazole derivatives suggested that, these derivatives could lead to new compounds for treatment against bacterial infection.

}, keywords = {123-Triazole, antibacterial activity, antimycobacterial activity, Pyrazole, Thiazole}, issn = {1040-6638}, doi = {10.1080/10406638.2020.1857272}, author = {Jagadale, Shivaji M. and Abhale, Yogita K. and Pawar, Hari R. and Shinde, Abhijit and Bobade, Vivek D. and Chavan, Abhijit P. and Sarkar, Dhiman and Mhaske, Pravin C.} }