Article
A quick diversity-oriented amide-forming reaction to optimize P-subsite residues of HIV protease inhibitors.
Chemistry & biology - 1 Aug 2002
Brik Ashraf, Lin Ying-Chuan, Elder John, Wong Chi-Huey
Abstract excerpt
We report a new simple method that allows rapid preparation in solution of a library of compounds for in situ high-throughput screening to identify new inhibitors of HIV-1 protease. The method is based on the amide-forming reaction of a C(2)-symmetrical diamino diol core with various carboxylic acids, followed by a direct assay of the inhibition activity without product isolation. Sixty-two compounds were made...
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