- Click chemistry approach: Regioselective one-pot synthesis of some new 8-trifluoromethylquinoline based 1,2,3-triazoles as potent antimicrobial agents
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Three series of 8-trifluoromethylquinoline based 1,2,3-triazoles derivatives (5a-c, 6a-d and 7a-c) were synthesized by multi-step reactions by click chemistry approach. Synthesized compounds were characterized by spectral studies and X-ray analysis. The final compounds were screened for their in-vitro antimicrobial activity by well plate method (zone of inhibition). Compounds 5c, 6b, 8b, 11 and 12 were found to be active against tested microbial strains. The results are summarized in Tables 5 and 6.
- Garudachari,Isloor, Arun M.,Satyanarayana,Fun, Hoong-Kun,Hegde, Gurumurthy
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p. 324 - 332
(2014/02/14)
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- Further modification on phenyl acetic acid based quinolines as liver X receptor modulators
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A series of phenyl acetic acid based quinolines was prepared as LXR modulators. An SAR study in which the C-3 and C-8 positions of the quinoline core were varied led to the identification of two potent LXR agonists 23 and 27. Both compounds displayed good binding affinity for LXRβ and LXRα, and increased expression of ABCA1 in THP-1 cells. These two compounds also had desirable pharmacokinetic profiles in mice and displayed in vivo efficacy in a 12-week Apo E knockout mouse lesion model.
- Hu, Baihua,Jetter, James,Kaufman, David,Singhaus, Robert,Bernotas, Ronald,Unwalla, Rayomand,Quinet, Elaine,Savio, Dawn,Halpern, Anita,Basso, Michael,Keith, James,Clerin, Valerie,Chen, Liang,Liu, Qiang-Yuan,Feingold, Irene,Huselton, Christine,Azam, Farooq,Goos-Nilsson, Annika,Wilhelmsson, Anna,Nambi, Ponnal,Wrobel, Jay
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p. 3321 - 3333
(2008/02/07)
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