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-301984nas a2200205 4500008004100000022001400041245013800055210006900193260000800262300001400270490000700284520122800291100002601519700001901545700002001564700002201584700001901606700002301625856013001648 2020 eng d a0022-152X00aSynthesis and antimycobacterial screening of new 4-(4-(1-benzyl-1H-1,2,3-triazol-4-yl)-1-phenyl-1H-pyrazol-3-yl)quinoline derivatives0 aSynthesis and antimycobacterial screening of new 441benzyl1H123t cNOV a3918-39290 v573 a

A new series of 4-(4-(1-benzyl-1H-1,2,3-triazol-4-yl)-1-phenyl-1H-pyrazol-3-yl)quinoline (6a-t) have been synthesized by a click reaction of 4-(4-ethynyl-1-phenyl-1H-pyrazol-3-yl)quinoline (4a-d) with a substituted benzyl azide (5a-e). The starting alkyne derivatives4a-dare obtained from Bestmann-Ohira reaction of 1-phenyl-3-(quinolin-4-yl)-1H-pyrazole-4-carbaldehyde and dimethyl(1-diazo-2-oxopropyl)phosphonate. The newly synthesized compounds are screened againstM. tuberculosisH37Ra dormant and active,Escherichia coli,Pseudomonas fluorescence,Staphylococcus aureusandBacillus subtilisstrains at 30 mu g/mL concentration. Most of the screened compounds showed good to moderate antibacterial activity againstS. aureus,B. subtilis, andMycobacterium tuberculosisH37Ra strains. The synthesized derivatives of quinolinyl-pyrazole-4-carbaldehyde and quinolinyl-pyrazole-4-ethyne reportd good to moderate activity against both strains ofM. tuberculosisH37Ra. Ten derivatives of quinolinyl-pyrazole presented good activity againstB. subtilis. These results suggested that further optimization and development of quinolinyl-pyrazolyl-1,2,3-triazole moeity could serve as lead compounds for antimycobacterial activity.

1 aThakare, Prashant, P.1 aWalunj, Yogesh1 aChavan, Abhijit1 aBobade, Vivek, D.1 aSarkar, Dhiman1 aMhaske, Pravin, C. uhttps://library.ncl.res.in/content/synthesis-and-antimycobacterial-screening-new-4-4-1-benzyl-1h-123-triazol-4-yl-1-phenyl-1h01555nas a2200253 4500008004100000022001400041245011200055210006900167520065400236653001500890653002700905653001700932653003100949653001400980653001300994100002701007700002301034700002401057700002401081700002301105700001901128700002201147856013201169 2022 eng d a1551-700400aSynthesis and antimycobacterial screening of a novel series of alpha-amino acids containing thiazole linker0 aSynthesis and antimycobacterial screening of a novel series of a3 a

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.

10aAmino acid10aantibacterial activity10aCytotoxicity10aMycobacterium tuberculosis10asynthesis10aThiazole1 aNalawade, Jitendra, L.1 aMhaske, Pravin, C.1 aShinde, Abhijit, D.1 aChavan, Abhijit, P.1 aAbhale, Yogita, K.1 aSarkar, Dhiman1 aBobade, Vivek, D. uhttps://library.ncl.res.in/content/synthesis-and-antimycobacterial-screening-novel-series-alpha-amino-acids-containing-thiazole02255nas 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