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Updated: Jun 10, 2026

Rapid Screening of HIV Reverse Transcriptase and Integrase Inhibitors
Published on: April 10, 2014
Design, synthesis and pharmacological evaluation of HIV-1 reverse transcriptase inhibition of new indolin-2-ones
Núbia Boechat1, W Bruce Kover, Vera Bongertz
1Departamento de Pesquisa e Desenvolvimento de Fármacos, Instituto de Tecnologia em Fármacos, Far-manguinhos/FIOCRUZ, Rua Sizenando Nabuco, 100 Manguinhos, Rio de Janeiro 21041-250, Brazil. boechat@far.fiocruz.br
Abstract:
The design, synthesis and anti HIV-1 replication inhibition of 3-(cyclopropylethynyl)-3-hydroxy-indolin-2-ones, analogues of efavirenz (Sustivatrade mark), 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.
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