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Design and regioselective synthesis of trifluoromethylquinolone derivatives as potent antimicrobial agents.

Abstract：

:Three series of new trifluoromethyl substituted quinolone derivatives were synthesized (4a-f, 6a-f and 8a-f) from corresponding substituted anilines by multi-step reactions. The regioselective alkylation with different alkyl halides were carried out by approaching two different routes to get the final products in good yield. Newly synthesized compounds were characterized by spectral study and also by C, H, N analyses. Three dimensional structure of 2b and 4b were also confirmed by single crystal X-ray studies. The final compounds (4a-f, 6a-f and 8a-f) were screened for their in-vitro antibacterial and antifungal activity by well plate method (zone of inhibition). The results revealed that, compounds 4a, 6b, 6c and 8e showed significant antibacterial activity as compared to the standard drug Ciprofloxacin. The compound 8a was found to be a potent antifungal agent.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Garudachari B,Isloor AM,Satyanarayana MN,Fun HK,Pavithra N,Kulal A

doi

10.1016/j.ejmech.2013.07.021

subject

Has Abstract

pub_date

2013-10-01 00:00:00

pages

422-32

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(13)00469-8

journal_volume

68

pub_type

杂志文章

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