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 , Wagner Wollinger .

Journal Name: Medicinal Chemistry

Volume 3 , Issue 6 , 2007

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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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Article Details

VOLUME: 3
ISSUE: 6
Year: 2007
Page: [533 - 542]
Pages: 10
DOI: 10.2174/157340607782360326
Price: $58

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