02140nas a2200313 4500008004100000022001400041245017000055210006900225260000800294300001400302490000700316520107600323653000601399653000601405653001701411653002701428653002801455653001701483653002301500653001501523100002401538700002601562700002601588700002001614700002301634700001901657700002201676856012801698 2019 eng d a1054-252300aSynthesis of new 1,3,4-oxadiazole and benzothiazolylthioether derivatives of 4-arylmethylidene-3-substituted-isoxazol-5(4H)-one as potential antimycobacterial agents0 aSynthesis of new 134oxadiazole and benzothiazolylthioether deriv cNOV a1873-18840 v283 a

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.

10a110a310a4-Oxadiazole10aantibacterial activity10aAntitubercular activity10aBenzothiazol10aIsoxazol-5(4H)-one10aThioeteher1 aChavan, Abhijit, P.1 aDeshpande, Rujuta, R.1 aBorade, Nandkumar, A.1 aShinde, Abhijit1 aMhaske, Pravin, C.1 aSarkar, Dhiman1 aBobade, Vivek, D. uhttps://library.ncl.res.in/content/synthesis-new-134-oxadiazole-and-benzothiazolylthioether-derivatives-4-arylmethylidene-302099nas a2200253 4500008004100000022001400041245010600055210006900161260000800230300001100238490000800249520125600257653001701513653003101530653001301561653002201574100002301596700002001619700001901639700001901658700001901677700002301696856012601719 2021 eng d a0045-206800aSynthesis of new 2-(thiazol-4-yl)thiazolidin-4-one derivatives as potential anti-mycobacterial agents0 aSynthesis of new 2thiazol4ylthiazolidin4one derivatives as poten cOCT a1051920 v1153 aTo search for potent antimycobacterial lead compounds, a new series of 3-substituted phenyl-2-(2-(substituted phenyl)thiazol-4-yl) thiazolidin-4-one (5a-t) derivatives have been synthesized by the condensation of 2 substituted phenyl thiazole-4-carbaldehyde with aromatic amine followed by cyclocondensation with thioglycolic acid. The structure of the newly synthesized 2-(thiazol-4-yl)thiazolidin-4-one derivatives were characterized by the spectroscopic analysis. The synthesized compounds were screened for antimycobacterial activity against Mycobacterium tuberculosis H37Ra (MTB) (ATCC 25177) and Mycobacterium bovis BCG (BCG, ATCC 35743). Most of the 2-(thiazol-4-yl)thiazolidin-4-one derivatives showed good to excellent antimycobacterial activity against both the Mtb strains. Nine derivatives 5c, 5g, 5j, 5m, 5n, 5o, 5p, 5s, and 5t showed excellent activity against M. bovis BCG with MIC 4.43 to 24.04 mu M were further evaluated for the cytotoxicity activity against HeLa A549, and HCT-116 cell lines and showed no significant cytotoxic activity at the maximum concentration evaluated. The potential antimycobacterial activities enforced that the thiazolyl-thiazolidin-4-one derivatives could lead to compounds that could treat tuberculosis.10aCytotoxicity10aMycobacterium tuberculosis10aThiazole10aThiazolidin-4-one1 aAbhale, Yogita, K.1 aShinde, Abhijit1 aShelke, Monika1 aNawale, Laxman1 aSarkar, Dhiman1 aMhaske, Pravin, C. uhttps://library.ncl.res.in/content/synthesis-new-2-thiazol-4-ylthiazolidin-4-one-derivatives-potential-anti-mycobacterial02255nas a2200289 4500008004100000022001400041245013300055210006900188260000800257300001400265490000700279520128400286653001701570653002701587653003101614653001301645653001301658100002601671700002301697700002001720700002001740700002201760700002401782700001901806700002301825856011701848 2022 eng d a1040-663800aSynthesis of new thiazole and pyrazole clubbed 1,2,3-triazol derivatives as potential antimycobacterial and antibacterial agents0 aSynthesis of new thiazole and pyrazole clubbed 123triazol deriva cJUL a3216-32370 v423 a

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.

10a123-Triazole10aantibacterial activity10aantimycobacterial activity10aPyrazole10aThiazole1 aJagadale, Shivaji, M.1 aAbhale, Yogita, K.1 aPawar, Hari, R.1 aShinde, Abhijit1 aBobade, Vivek, D.1 aChavan, Abhijit, P.1 aSarkar, Dhiman1 aMhaske, Pravin, C. uhttps://library.ncl.res.in/content/synthesis-new-thiazole-and-pyrazole-clubbed-123-triazol-derivatives-potential02258nas a2200265 4500008004100000022001400041245016900055210006900224260000900293300001200302490000700314520130000321653002001621653002701641653002401668653002201692100002301714700002001737700002301757700002201780700002201802700001901824700002301843856012601866 2024 eng d a1040-663800aSynthesis and antimicrobial evaluation of novel 2'-aryl-4-aryl-2,4'-Bisthiazole and 2'-aryl-4-Pyridyl-2,4'-bisthiazole derivatives as potential antibacterial agents0 aSynthesis and antimicrobial evaluation of novel 2aryl4aryl24Bist cFEB  a773-7870 v443 a

In continuation of our research work to explore bisthiazole derivatives as potential antimicrobial agents, herein we reported the synthesis of a series of novel 2'-aryl-4-aryl-2,4'-bisthiazole (7a-t) and 2'-aryl-4-pyridyl-2,4'-bisthiazole (9a-l) by cyclocondensation of 2-aryl thiazole-4-carbothioamide 5a-d with 2-bromo-1-arylethanone (6a-e) and bromo-1-(pyridin-2/3/4-yl)ethanone (8a-c), respectively. These novel candidates were evaluated in vitro for their antibacterial potential against four pathogenic bacteria, Escherichia coli (NCIM 2576), Pseudomonas flurescence (NCIM 2059), Staphylococcus aureus (NCIM 2602), and Bacillus subtilis (NCIM 2162). The synthesized compounds were also screened for their in vitro antifungal activity against Candida albicans (NCIM 3100). Among them, compounds 7b, 9d, 9 g, 9i, and 9 l exhibited excellent antibacterial activity with MIC 2.1 to 12.3 mu g/mL against all tested strains. Most of the compounds reported moderate antifungal activity. The pyridine ring-substituted bisthiazole reported good to excellent antibacterial activity as compared to phenyl ring-substituted bisthiazole. The potential antibacterial activity suggested that bisthiazole derivatives could assist in the development of lead compounds to treat microbial infections.

10a24'-bisthiazole10aantibacterial activity10aAntifungal activity10acyclocondensation1 aNalawade, Jitendra1 aShinde, Abhijit1 aAbhale, Yogita, K.1 aNandurkar, Yogesh1 aBobade, Vivek, D.1 aSarkar, Dhiman1 aMhaske, Pravin, C. uhttps://library.ncl.res.in/content/synthesis-and-antimicrobial-evaluation-novel-2-aryl-4-aryl-24-bisthiazole-and-2-aryl-4