title: Structure-activity relationships of some 3-substituted-4-hydroxycoumarins as HIV-1 protease inhibitors.
abstract: The screening of the HIV-1 protease (PR) inhibitory activity (IC-50) of various substituted 3-phenyl-4-hydroxycoumarins, 3-benzyl-4-hydroxycoumarins, 3-phenoxy-4-hydroxy-coumarins, 3-benzenesulfonyl-4-hydroxycoumarins and 3-(7-coumarinyloxy)-4-hydroxycoumarins was performed. The data indicate the importance of substituents at positions 5 and 7 of the coumarin ring on the inhibitory potency of the HIV-1-PR.
authors.affiliation: Laboratoire de Chimie Thérapeutique, Faculté de Pharmacie de Paris-Sud, Chatenay Malabry, France. serge.kirkiacharian@cep.u-psud.fr
authors.forename: Serge
authors.initials: S
authors.lastname: Kirkiacharian
authors.forename: Duong Thanh
authors.initials: DT
authors.lastname: Thuy
authors.forename: Sames
authors.initials: S
authors.lastname: Sicsic
authors.forename: Robert
authors.initials: R
authors.lastname: Bakhchinian
authors.forename: Raffi
authors.initials: R
authors.lastname: Kurkjian
authors.forename: Thierry
authors.initials: T
authors.lastname: Tonnaire
mesh_terms: D015110:4-Hydroxycoumarins / Q000138:chemical synthesis* / Q000494:pharmacology; D001665:Binding Sites; D016333:HIV Protease / Q000187:drug effects; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D006860:Hydrogen Bonding; D020128:Inhibitory Concentration 50; D013329:Structure-Activity Relationship
chemical_list: D015110:4-Hydroxycoumarins; D017320:HIV Protease Inhibitors; D016333:HIV Protease