Open AccessThe design and synthesis of a pyrrole-carbaldehyde hit family as HIV-1 integrase inhibitors
Author(s) -
Telisha Traut,
Raymond Hewer,
Judy Coates,
D. Bradley G. Williams
Publication year - 2011
Publication title -
suid-afrikaanse tydskrif vir natuurwetenskap en tegnologie/die suid-afrikaanse tydskrif vir natuurwetenskap en tegnologie
Language(s) - English
Resource type - Journals
eISSN - 2222-4173
pISSN - 0254-3486
DOI - 10.4102/satnt.v30i1.268
Subject(s) - integrase , in silico , integrase inhibitor , human immunodeficiency virus (hiv) , combinatorial chemistry , chemistry , pyrrole , chemical synthesis , computational biology , chemical toxicity , toxicity , biochemistry , virology , biology , organic chemistry , antiretroviral therapy , in vitro , gene , viral load
Menslike immuniteitsgebreksvirus tipe 1 (MIV-1) en die geassosiëerde verworwe
immuniteitsgebreksindroom (VIGS) toon alreeds ’n ernstige effek op wêreldsgesondheidsvlakke, asook op die wêreldekonomie.
Screening of an HIV-1 IN model against database-derived chemical structures identified pyrrole-carbaldehydes as targets for further development. Chemical synthesis using a facile one-pot reaction resulted in the generation of a compound library. Preliminary toxicity and efficacy assays of the water-soluble HCl-salt derivatives of each compound support the in silico predictions