title: Synthesis of novel cyclic urea based HIV-1 protease inhibitors.
abstract: A series of novel HIV-1 protease inhibitors was prepared in a short stereospecific manner. These compounds have only one P1 substituent interacting with the S1/S1' binding site of HIV-1 protease and only one hydroxyl group interacting with the catalytic aspartic acid domain, X-ray crystallography confirmed the desired R, R configuration of the final products.
authors.affiliation: DuPont Merck Pharmaceutical Company, Wilmington, DE 19880-0353, USA.
authors.forename: D A
authors.initials: DA
authors.lastname: Nugiel
authors.forename: K
authors.initials: K
authors.lastname: Reese
mesh_terms: D018360:Crystallography, X-Ray; D003500:Cyclization; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology*; D007536:Isomerism; D008968:Molecular Conformation; D014508:Urea / Q000031:analogs & derivatives / Q000138:chemical synthesis*
chemical_list: D017320:HIV Protease Inhibitors; D014508:Urea