Design, chemical synthesis of 3-(9H-fluoren-9-yl)pyrrolidine-2,5-dione derivatives and biological activity against enoyl-ACP reductase (InhA) and Mycobacterium tuberculosis.

Authors :: Matviiuk T
Rodriguez F
Saffon N
Mallet-Ladeira S
Gorichko M
de Jesus Lopes Ribeiro AL
Pasca MR
Lherbet C
Voitenko Z
Baltas M
Source :: European journal of medicinal chemistry [Eur J Med Chem] 2013; Vol. 70, pp. 37-48. Date of Electronic Publication: 2013 Oct 02.
Publication Year :: 2013
Abstract: We report here the discovery, synthesis and screening results of a series of 3-(9H-fluoren-9-yl)pyrrolidine-2,5-dione derivatives as a novel class of potent inhibitors of Mycobacterium tuberculosis H37Rv strain as well as the enoyl acyl carrier protein reductase (ENR) InhA. Among them, several compounds displayed good activities against InhA which is one of the key enzymes involved in the type II fatty acid biosynthesis pathway of the mycobacteria cell wall. Furthermore, some exhibited promising activities against M. tuberculosis and multi-drug resistant M. tuberculosis strains.<br /> (Copyright © 2013 Elsevier Masson SAS. All rights reserved.)

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