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Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Design, Synthesis and Pharmacological Evaluation of HIV-1 Reverse Transcriptase Inhibition of New Indolin-2-Ones

Author(s): Nubia Boechat, W. Bruce Kover, Vera Bongertz, Monica M. Bastos, Nelilma C. Romeiro, Maria L.G. Azevedo and Wagner Wollinger

Volume 3, Issue 6, 2007

Page: [533 - 542] Pages: 10

DOI: 10.2174/157340607782360326

Price: $65

Abstract

The design, synthesis and anti HIV-1 replication inhibition of 3-(cyclopropylethynyl)-3-hydroxy-indolin-2- ones, analogues of efavirenz (Sustiva™), are described. Different substituted isatins were used to generate final products that contain pharmacophoric features for RT inhibition, such as the oxoindole and cyclopropylethynyl groups. The suitability of the indolin-2-one ring in the planned compounds in replacement to the benzoxazinone ring of efavirenz was proven, since compound 15 presented a greater activity than efavirenz against HIV-1 replication and was not significantly cytotoxic.

Keywords: Isatins, molecular modeling, efavirenz


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