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

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

Volume: 3 Issue: 6

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

Affiliation:

Keywords: Isatins, molecular modeling, efavirenz

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.

Cite this article as:

Boechat Nubia, Kover Bruce W., Bongertz Vera, Bastos M. Monica, Romeiro C. Nelilma, Azevedo L.G. Maria and Wollinger Wagner, Design, Synthesis and Pharmacological Evaluation of HIV-1 Reverse Transcriptase Inhibition of New Indolin-2-Ones, Medicinal Chemistry 2007; 3 (6) . https://dx.doi.org/10.2174/157340607782360326