01943nas a2200253   4500008004100000022001200041245016100053210006900214260000900283300000700292490000800299520103300307653004101340653003001381653001701411653001001428100001801438700002101456700002401477700002001501700001901521700001801540856013101558       2018                        eng d  a974362600aSynthesis and biological evaluation of some bicyclic [2-(2,4-dimethylphenylthio)phenyl] aniline and its amide derivatives as potential antitubercular agents0 aSynthesis and biological evaluation of some bicyclic 224dimethyl  cFEB   a220 v1303 a<p>In the present investigation, a series of bicyclic [2-(2,4-dimethylphenylthio)phenyl] aniline analogues were synthesized and characterized by IR, NMR (1H and 13C) and mass spectra. All newly synthesized 15 compounds were inspected for their in vitro antitubercular activity against Mycobacterium tuberculosis (MTB) H37Ra in both active and dormant state using an established XTT Reduction Menadione assay (XRMA). The titled compounds exhibited minimum inhibitory concentration (MIC90) ranging from 0.05 to &gt;30 (μg/mL). The potent four compounds were further evaluated in THP-1 infection model where they demonstrated significant antitubercular activity. All the ex vivo active were further evaluated for cytotoxic activity against THP-1, MCK7 and HeLa cell lines in order to check selectivity index. All compounds were further screened against four different bacteria to assess their selectivity towards MTB. These derivatives could be considered as a precursor structure for further design of antituberculosis agent.</p>10a4-dimethylphenylthio)phenyl] aniline10aantituberculosis activity10aCytotoxicity10a[2-(21 aPatil, Yogesh1 aShingare, Ramesh1 aChakraborty, Shakti1 aBorkute, Rachna1 aSarkar, Dhiman1 aMadje, Balaji  uhttps://library.ncl.res.in/content/synthesis-and-biological-evaluation-some-bicyclic-2-24-dimethylphenylthiophenyl-aniline-and01848nas a2200205   4500008004100000022001400041245011900055210006900174260000900243300001400252490000600266520110100272100002301373700002401396700002401420700001901444700002301463700002601486856013001512       2018                        eng d  a2040-250300aTriazole-diindolylmethane conjugates as new antitubercular agents: synthesis, bioevaluation, and molecular docking0 aTriazolediindolylmethane conjugates as new antitubercular agents  cJUL   a1114-11300 v93 a<p>We describe the synthesis of novel triazole-incorporated diindolylmethanes (DIMs) using a molecular hybridization approach. The in vitro antitubercular activity of the DIMs against Mycobacterium tuberculosis H37Ra (ATCC 25177) was tested in the active and dormant state. Among all the synthesized conjugates, the compounds 6b, 6f, 6l, 6n, 6q, 6r, and 6s displayed good antitubercular activity against both the active and dormant Mtb H37Ra strain. The compound 6l exhibited good antitubercular activity against dormant Mtb H37Ra with an IC50 value of 1 g mL(-1) and IC90 (MIC) value of 3 g mL(-1). The compounds 6b, 6l, and 6r displayed good antitubercular activity against active Mtb H37Ra with IC50 values of 2.19, 1.52, and 0.22 g mL(-1), respectively. The compounds 6b, 6h, 6l, and 6s displayed more than 70% inhibition against the Gram-positive Bacillus subtilus strain at 3 g mL(-1). The molecular docking study showed the binding modes of the titled compounds in the active site of the DprE1 enzyme and assisted with elucidating a structural basis for the inhibition of Mycobacteria.</p>1 aDanne, Ashruba, B.1 aChoudhari, Amit, S.1 aChakraborty, Shakti1 aSarkar, Dhiman1 aKhedkar, Vijay, M.1 aShingate, Bapurao, B.  uhttps://library.ncl.res.in/content/triazole-diindolylmethane-conjugates-new-antitubercular-agents-synthesis-bioevaluation-and02080nas a2200313   4500008004100000022001400041245012500055210006900180260000800249300001200257490000700269520107300276653000601349653000601355653001501361653002801376653002201404653002701426653001301453100001801466700002201484700002301506700002401529700002001553700002201573700002401595700001901619856012801638       2019                        eng d  a1054-252300aSynthesis and antimycobacterial evaluation of new 5-(1-benzyl-1H-1,2,3-triazol-4-yl)-4-methyl-2-arylthiazole derivatives0 aSynthesis and antimycobacterial evaluation of new 51benzyl1H123t  cJUN  a805-8190 v283 a<p>A new series of 5-(1-benzyl-1H-1,2,3-triazol-4-yl)-4-methyl-2-arylthiazole derivatives, 6a-w have been synthesized by click reaction of substituted benzylazide, 5a-d with 5-ethynyl-4-methyl-2-substituted phenylthiazole, 4a-f. The starting compounds 4-ethynyl-2-substituted phenylthiazole (4a-f) were synthesized from the corresponding thiazole aldehyde by using the Ohira-Bestmann reagent. The structure of the synthesized compounds was determined by spectral analysis. All the synthesized compounds were screened for their preliminary antitubercular activity against Mycobacterium tuberculosis H37Ra (MTB, ATCC 25177). Most of the synthesized compounds reported good activity against M. tuberculosis H37Ra strain with IC50 range of 0.58-8.23 mu g/mL. Compounds 6g and 6k reported good antitubercular activity with MIC90 values of 4.71 and 2.22 mu g/mL, respectively. Potential antimycobacterial activity suggested that these compounds could serve as good lead compounds for further optimization and development of a newer antitubercular candidate. [GRAPHICS] .</p>10a110a210a3-Triazole10aAntitubercular activity10aMolecular docking10aOhira-Bestmann reagent10aThiazole1 aShinde, Vikas1 aMahulikar, Pramod1 aMhaske, Pravin, C.1 aChakraborty, Shakti1 aChoudhari, Amit1 aPhalle, Siddharth1 aChoudhari, Prafulla1 aSarkar, Dhiman  uhttps://library.ncl.res.in/content/synthesis-and-antimycobacterial-evaluation-new-5-1-benzyl-1h-123-triazol-4-yl-4-methyl-2