01624nas a2200193   4500008004100000245013100041210006900172260000800241300001300249490000700262520089200269100003001161700002401191700002301215700001901238700002301257700002601280856012401306       2017                        eng d00aQuinolidene based monocarbonyl curcumin analogues as promising antimycobacterial agents: synthesis and molecular docking study0 aQuinolidene based monocarbonyl curcumin analogues as promising a  cFEB  a 922-9280 v273 a<p>A series of quinoline incorporated monocarbonyl curcumin analogues was efficiently synthesized using [HDBU][HSO4] as catalyst via Knoevenagel type condensation and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Ra (MTB) and Mycobacterium bovis BCG in dormant state. The analogues 3e, 3h, 4a and 4e exhibited very good antitubercular activity. The antiproliferative activity of the analogues against MCF-7, A549 and HCT-116 cell lines was evaluated using modified MTT assay and these compounds were found to be non-cytotoxic. Molecular docking study has been carried out against M. tuberculosis pantothenate synthetase (MTB PS) enzyme in an effort to enhance the understanding of their action as antitubercular agents. The potency, low cytotoxicity and selectivity of these analogues support them as valid leads for further optimization.</p>1 aSubhedar, Dnyaneshwar, D.1 aShaikh, Mubarak, H.1 aNawale, Laxman, U.1 aSarkar, Dhiman1 aKhedkar, Vijay, M.1 aShingate, Bapurao, B.  uhttps://library.ncl.res.in/content/quinolidene-based-monocarbonyl-curcumin-analogues-promising-antimycobacterial-agents01956nas a2200217   4500008004100000245008100041210006900122260000800191300001400199490000800213520120400221100003001425700002401455700002601479700001901505700001901524700002301543700002601566700003101592856011501623       2017                        eng d00aQuinolidene-rhodanine conjugates: facile synthesis and biological evaluation0 aQuinolidenerhodanine conjugates facile synthesis and biological   cJAN  a385–3990 v1253 a<p>A series of rhodanine incorporated quinoline derivatives were efficiently synthesized using reusable DBU acetate as ionic liquid and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Ra (MTB) (ATCC 25177) and Mycobacterium bovis BCG (ATCC 35743) both in active and dormant state. Compounds 3e, 3f, 3g, 3h and 3i exhibited very good antitubercular activity. The active compounds were studied for cytotoxicity against HUVEC, THP-1, macrophages, A549, PANC-1 and HeLa cell lines using modified MTT assay and were found to be noncytotoxic. Inactivity of all these compounds against Gram positive and Gram negative bacteria indicates their specificity towards the MTB. Further, the synthesized compounds have been screened for their in vitro antifungal activity. In addition, the molecular docking studies revealed the binding modes of these compounds in active site of Zmp1 enzyme, which in turn helped to establish a structural basis of inhibition of mycobacteria. The results of present study clearly indicate the identification of some novel, selective and specific inhibitors against MTB that can be explored further for potential antitubercular drug.</p>1 aSubhedar, Dnyaneshwar, D.1 aShaikh, Mubarak, H.1 aShingate, Bapurao, B.1 aNawale, Laxman1 aSarkar, Dhiman1 aKhedkar, Vijay, M.1 aKhan, Firoz, A. Kalam1 aSangshetti, Jaiprakash, N.  uhttps://library.ncl.res.in/content/quinolidene-rhodanine-conjugates-facile-synthesis-and-biological-evaluation