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

[ Vol. 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   Pages 533 - 542 ( 10 )

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

Affiliation:

Departamento de Pesquisa e Desenvolvimento de Farmacos, Instituto de Tecnologia em Farmacos, Farmanguinhos/FIOCRUZ, Rua Sizenando Nabuco, 100 Manguinhos, Rio de Janeiro 21041-250 Brazil.



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