title: 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.
authors: a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
authors: Rita
authors: R
authors: Meleddu
authors: a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
authors: Simona
authors: S
authors: Distinto
authors: b Department of Life and Environmental Sciences , University of Cagliari, Cittadella Universitaria di Monserrato , Cagliari , Italy.
authors: Angela
authors: A
authors: Corona
authors: b Department of Life and Environmental Sciences , University of Cagliari, Cittadella Universitaria di Monserrato , Cagliari , Italy.
authors: Enzo
authors: E
authors: Tramontano
authors: a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
authors: Giulia
authors: G
authors: Bianco
authors: a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
authors: Claudia
authors: C
authors: Melis
authors: a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
authors: Filippo
authors: F
authors: Cottiglia
authors: a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
authors: Elias
authors: E
authors: Maccioni
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D007510:Isatin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D015394:Molecular Structure; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D019380:Anti-HIV Agents; D018894:Reverse Transcriptase Inhibitors; D013844:Thiazoles; D007510:Isatin; C514824:reverse transcriptase, Human immunodeficiency virus 1; D054303:HIV Reverse Transcriptase
keywords: HIV-1 therapeutic agents; Isatin derivatives; RT dual inhibitors