Synthesis of 3-heteryl substituted pyrrolidine-2,5-diones via catalytic Michael reaction and evaluation of their inhibitory activity against InhA and Mycobacterium tuberculosis.

Authors :: Matviiuk T
Mori G
Lherbet C
Rodriguez F
Pasca MR
Gorichko M
Guidetti B
Voitenko Z
Baltas M
Source :: European journal of medicinal chemistry [Eur J Med Chem] 2014 Jan; Vol. 71, pp. 46-52. Date of Electronic Publication: 2013 Nov 04.
Publication Year :: 2014
Abstract: In the present paper, we report the synthesis via catalytic Michael reaction and biological results of a series of 3-heteryl substituted pyrrolidine-2,5-dione derivatives as moderate inhibitors against Mycobacterium tuberculosis H37Rv growth. Some of them present also inhibition activities against InhA.<br /> (Copyright © 2013 Elsevier Masson SAS. All rights reserved.)

Subjects :: Antitubercular Agents chemical synthesis
Bacterial Proteins metabolism
Humans
Microbial Sensitivity Tests
Models, Molecular
Mycobacterium tuberculosis growth & development
Oxidoreductases metabolism
Pyrrolidines chemical synthesis
Structure-Activity Relationship
Tuberculosis drug therapy
Antitubercular Agents chemistry
Antitubercular Agents pharmacology
Bacterial Proteins antagonists & inhibitors
Mycobacterium tuberculosis drug effects
Oxidoreductases antagonists & inhibitors
Pyrrolidines chemistry
Pyrrolidines pharmacology

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