Thienopyridone antibacterials .1. A synthesis of some 7-alkyl-2-chloro-1,4-dihydro-4-oxothieno[2,3-b]pyridine-5-carboxylic acids

A selected set of 7-alkyl-4-oxothieno[2,3-b]pyridine-5-carboxylic acids (7) and their methyl esters (6) were prepared by cyclization of the respective 3-N-alkylamino-2-(2,5-dichloro-3-thienoyl)acrylates (5) which, in turn, are accessible via methyl 3-(2,5-dichlorothien-3-yl)-3-oxopropanoate (3). Of...

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Bibliographic Details
Published inHeterocycles Vol. 45; no. 2; pp. 255 - 264
Main Authors ElAbadelah, MM, Sabri, SS, AlAshqar, HA
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier 01.02.1997
Subjects
Chemistry
Chemistry, Organic
Physical Sciences
Science & Technology
5-CARBOXYLIC ACIDS
AGENTS
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Summary:A selected set of 7-alkyl-4-oxothieno[2,3-b]pyridine-5-carboxylic acids (7) and their methyl esters (6) were prepared by cyclization of the respective 3-N-alkylamino-2-(2,5-dichloro-3-thienoyl)acrylates (5) which, in turn, are accessible via methyl 3-(2,5-dichlorothien-3-yl)-3-oxopropanoate (3). Of the present series, the N-cyclopropyl derivative (7b) exhibited the highest potency against Escherichia coli (MIC = 0.5 mu g/ml).
ISSN:0385-5414