01495nas a2200229   4500008004100000022001400041245007200055210006900127260000800196300001400204490000700218520075800225100002200983700002301005700002301028700002101051700002401072700001901096700002601115700002401141856010001165       2018                        eng d  a1756-891900a Rational design of coumarin derivatives as antituberculosis agents0 aRational design of coumarin derivatives as antituberculosis agen  cOCT  a2431-24440 v103 aA series of coumarin derivatives was designed as potential antituberculosis agents. Results: The compounds were screened against active and dormant Mycobacterium tuberculosis (Mtb). Compounds 3k and 3n were found to have the most promising activity against replicating MtbH37Rv exhibiting minimum inhibitory concentration of 4.63 and 9.75 mu M respectively. The compounds were also effective against dormant MtbH37Rv exhibiting more potency than the standard drugs, isoniazid and rifampicin. The compounds were found to be non-cytotoxic against human cell lines. Conclusion: This study provides promising antituberculosis agents that are effective against replicating as well as dormant Mtb and can thus act as potential leads for further development.
1 aMali, Hemlata, M.1 aSabale, Sandip, S.1 aDegani, Mariam, S.1 aBorkute, Rachana1 aChoudhari, Amit, S.1 aSarkar, Dhiman1 aKrishna, Vagolu, Siva1 aSriram, Dharmarajan  uhttps://library.ncl.res.in/content/rational-design-coumarin-derivatives-antituberculosis-agents01775nas a2200277   4500008004100000245014700041210006900188260000800257300001200265490000800277520079400285100002201079700002601101700002001127700002401147700002201171700002301193700002001216700002101236700001701257700001901274700002401293700003001317700002201347856012801369       2019                        eng d00aSynthesis and biological evaluation of 2,4,5-trisubstituted thiazoles as antituberculosis agents effective against drug-resistant tuberculosis0 aSynthesis and biological evaluation of 245trisubstituted thiazol  cSEP  a315-3280 v1783 a<p>The dormant and resistant form of Mycobacterium tuberculosis presents a challenge in developing new anti-tubercular drugs. Herein, we report the synthesis and evaluation of trisubstituted thiazoles as antituberculosis agents. The SAR study has identified a requirement of hydrophobic substituent at C2, ester functionality at C4, and various groups with hydrogen bond acceptor character at C5 of thiazole scaffold. This has led to the identification of 13h and 13p as lead compounds. These compounds inhibited the dormant Mycobacterium tuberculosis H37Ra strain and M. tuberculosis H37Rv selectively. Importantly, 13h and 13p were non-toxic to CHO cells. The 13p showed activity against multidrug-resistant tuberculosis isolates. (C) 2019 Elsevier Masson SAS. All rights reserved.</p>
1 aKarale, Uttam, B.1 aKrishna, Vagolu, Siva1 aKrishna, Vamshi1 aChoudhari, Amit, S.1 aShukla, Manjulika1 aGaikwad, Vikas, R.1 aMahizhaveni, B.1 aChopra, Sidharth1 aMisra, Sunil1 aSarkar, Dhiman1 aSriram, Dharmarajan1 aDusthackeer, V., N. Azger1 aRode, Haridas, B.  uhttps://library.ncl.res.in/content/synthesis-and-biological-evaluation-245-trisubstituted-thiazoles-antituberculosis-agents