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New quinolin-4-yl-1,2,3-triazoles carrying amides, sulphonamides and amidopiperazines as potential antitubercular agents.

Abstract：

:Three new series of quinoline-4-yl-1,2,3-triazoles carrying amides, sulphonamides and amidopiperazines were synthesized through multi-step reactions. The required intermediate, [1-(6-methoxy-2-methylquinolin-4-yl)-1H-1,2,3-triazol-4-yl]methanol (2) was prepared by treating 4-azido-6-methoxy-2-methylquinoline (1) with propargyl alcohol. Three different series of compounds were synthesized from this intermediate. All the newly synthesized compounds were characterized by spectral and elemental analyses. The structure of 2 was confirmed by X-ray crystallographic study. Further, the title compounds were evaluated for their in vitro anti-bacterial activity against five different bacterial strains and antimycobacterial activity against Mycobacterium tuberculosis H37Rv, Mycobacterium smegmatis (ATCC 19420) and Mycobacterium fortuitum (ATCC 19542). Title compounds, 6a, 6d, 6i, 6j, 7e, 10a and 10i were found to be active against Mycobacterium tuberculosis H37Rv strain and could be lead molecules of interest.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Thomas KD,Adhikari AV,Chowdhury IH,Sumesh E,Pal NK

doi

10.1016/j.ejmech.2011.03.039

subject

Has Abstract

pub_date

2011-06-01 00:00:00

pages

2503-12

issue

6

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(11)00254-6

journal_volume

46

pub_type

杂志文章

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