Synthesis and activity of new acylated diaminohydroxyalkanes as human immunodeficiency virus protease inhibitors.
A series of HIV-1 protease inhibitors based on the lead compound Pc (IC50 = 165 nmol/l) with structural modifications at P1/P1' substituents or with a lengthening at its core unit were synthesized from amino acid starting materials. All analogues were less active than Pc against the protease.
Marastoni
M
M
Department of Pharmaceutical Sciences, University of Ferrara, Italy.
Bazzaro
M
M
Bortolotti
F
F
Tomatis
R
R
D000473:Alkanes / Q000138:chemical synthesis* / Q000494:pharmacology; D002478:Cells, Cultured; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002851:Chromatography, High Pressure Liquid; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D013058:Mass Spectrometry; D009904:Optical Rotation; D013329:Structure-Activity Relationship
D000473:Alkanes; D017320:HIV Protease Inhibitors