Structure-activity relationships of some 3-substituted-4-hydroxycoumarins as HIV-1 protease inhibitors.
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.
Kirkiacharian
Serge
S
Laboratoire de Chimie Thérapeutique, Faculté de Pharmacie de Paris-Sud, Chatenay Malabry, France. serge.kirkiacharian@cep.u-psud.fr
Thuy
Duong Thanh
DT
Sicsic
Sames
S
Bakhchinian
Robert
R
Kurkjian
Raffi
R
Tonnaire
Thierry
T
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
D015110:4-Hydroxycoumarins; D017320:HIV Protease Inhibitors; D016333:HIV Protease