title: Synthesis of 3-heteryl substituted pyrrolidine-2,5-diones via catalytic Michael reaction and evaluation of their inhibitory activity against InhA and Mycobacterium tuberculosis.
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.
authors.affiliation: Université de Toulouse, UPS, Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, LSPCMIB, 118 route de Narbonne, F-31062 Toulouse cedex 9, France; Taras Shevchenko National University of Kyiv, Department of Chemistry, 64 str. Volodymyrska, Kyiv 01601, Ukraine.
authors.forename: Tetiana
authors.initials: T
authors.lastname: Matviiuk
authors.affiliation: University of Pavia, Dipartimento di Biologia e Biotecnologie "Lazzaro Spallanzani", via Ferrata 1, 27100 Pavia, Italy.
authors.forename: Giorgia
authors.initials: G
authors.lastname: Mori
authors.affiliation: Université de Toulouse, UPS, Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, LSPCMIB, 118 route de Narbonne, F-31062 Toulouse cedex 9, France; CNRS, Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, LSPCMIB, UMR-5068, 118 Route de Narbonne, F-31062 Toulouse cedex 9, France. Electronic address: lherbet@chimie.ups-tlse.fr.
authors.forename: Christian
authors.initials: C
authors.lastname: Lherbet
authors.affiliation: Université de Toulouse, UPS, Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, LSPCMIB, 118 route de Narbonne, F-31062 Toulouse cedex 9, France; CNRS, Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, LSPCMIB, UMR-5068, 118 Route de Narbonne, F-31062 Toulouse cedex 9, France.
authors.forename: Frédéric
authors.initials: F
authors.lastname: Rodriguez
authors.affiliation: University of Pavia, Dipartimento di Biologia e Biotecnologie "Lazzaro Spallanzani", via Ferrata 1, 27100 Pavia, Italy.
authors.forename: Maria Rosalia
authors.initials: MR
authors.lastname: Pasca
authors.affiliation: Taras Shevchenko National University of Kyiv, Department of Chemistry, 64 str. Volodymyrska, Kyiv 01601, Ukraine.
authors.forename: Marian
authors.initials: M
authors.lastname: Gorichko
authors.affiliation: Université de Toulouse, UPS, Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, LSPCMIB, 118 route de Narbonne, F-31062 Toulouse cedex 9, France.
authors.forename: Brigitte
authors.initials: B
authors.lastname: Guidetti
authors.affiliation: Taras Shevchenko National University of Kyiv, Department of Chemistry, 64 str. Volodymyrska, Kyiv 01601, Ukraine. Electronic address: z_voitenko@mail.univ.kiev.ua.
authors.forename: Zoia
authors.initials: Z
authors.lastname: Voitenko
authors.affiliation: Université de Toulouse, UPS, Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, LSPCMIB, 118 route de Narbonne, F-31062 Toulouse cedex 9, France; CNRS, Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, LSPCMIB, UMR-5068, 118 Route de Narbonne, F-31062 Toulouse cedex 9, France. Electronic address: baltas@chimie.ups-tlse.fr.
authors.forename: Michel
authors.initials: M
authors.lastname: Baltas
mesh_terms: D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001426:Bacterial Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D009169:Mycobacterium tuberculosis / Q000187:drug effects* / Q000254:growth & development; D010088:Oxidoreductases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011759:Pyrrolidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014376:Tuberculosis / Q000188:drug therapy
chemical_list: D000995:Antitubercular Agents; D001426:Bacterial Proteins; D011759:Pyrrolidines; D010088:Oxidoreductases; C085257:InhA protein, Mycobacterium; C032519:pyrrolidine
keywords: InhA; Michael addition; Succinimide; Tuberculosis