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Synthesis, crystal and antibacterial studies of diversely functionalized tetrahydropyridin-4-ol.

Abstract：

:In an effort to expand the spectrum of antibacterial activity associated with piperidin-4-one derivatives, we have synthesized two series of 3-carboxyethyl-2,6-diphenyl-4-hydroxy-Delta(3)-tetrahydropyridine derivatives bearing diversified heterocyclic and aromatic systems at the nitrogen atom through acetyl (6-18) and 2-propanoyl (9-31) linkers. Unlike acetyl derivatives, NMR spectral pattern of the propanoyl counterparts revealed the existence of pair of rotational isomers (syn and anti) in solution at room temperature due to the hindered rotation about N-CO bond. X-ray crystal studies of 9 and 24 clearly pointed out that all the compounds existed in only one form particularly, in stable syn form in solid state. Each of the compounds was screened for their in vitro antibacterial activity against nine human pathogenic gram-positive strains including multiple drug resistant organisms and seven problematic gram-negative strains. Among the various heterocycles examined here, imidazole substituted derivatives 12 and 25 exhibited antibacterial activity approaching that of Linezolid and Trovafloxacin drugs particularly against multiple resistant Enterococcus faecium-VanA phenotype strains.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Aridoss G,Amirthaganesan S,Jeong YT

doi

10.1016/j.bmcl.2010.02.015

subject

Has Abstract

pub_date

2010-04-01 00:00:00

pages

2242-9

issue

7

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00205-2

journal_volume

20

pub_type

杂志文章

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