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Isatin thiazoline hybrids as dual inhibitors of HIV-1 reverse transcriptase.

ABSTRACT: A series of 3-3-{2-[2-3-methyl-4-phenyl-2,3-dihydro-1,3-thiazol-2-ylidene]hydrazin-1-ylidene-2,3-dihydro-1H-indol-2-one derivatives has been designed and synthesized to study their activity on both HIV-1 (Human Immunodeficiency Virus type 1) RT (Reverse Transcriptase) associated functions. These derivatives are analogs of previously reported series whose biological activity and mode of action have been investigated. In this work we investigated the influence of the introduction of a methyl group in the position 3 of the dihydrothiazole ring and of a chlorine atom in the position 5 of the isatin nucleus. The new synthesized compounds are active towards both DNA polymerase and ribonuclease H in the µM range. The nature of the aromatic group in the position 4 of the thiazole was relevant in determining the biological activity.

SUBMITTER: Meleddu R

PROVIDER: S-EPMC6010014 | biostudies-literature | 2017 Dec

REPOSITORIES: biostudies-literature

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Isatin thiazoline hybrids as dual inhibitors of HIV-1 reverse transcriptase.

Meleddu Rita R Distinto Simona S Corona Angela A Tramontano Enzo E Bianco Giulia G Melis Claudia C Cottiglia Filippo F Maccioni Elias E

Journal of enzyme inhibition and medicinal chemistry 20161021 1

A series of 3-3-{2-[2-3-methyl-4-phenyl-2,3-dihydro-1,3-thiazol-2-ylidene]hydrazin-1-ylidene-2,3-dihydro-1H-indol-2-one derivatives has been designed and synthesized to study their activity on both HIV-1 (Human Immunodeficiency Virus type 1) RT (Reverse Transcriptase) associated functions. These derivatives are analogs of previously reported series whose biological activity and mode of action have been investigated. In this work we investigated the influence of the introduction of a methyl group ...[more]

PMID: 27766892

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