Tricyclic HIV integrase inhibitors: potent and orally bioavailable C5-aza analogs.
A series of C5-aza tricyclic HIV integrase inhibitors was prepared. A highly potent and orally bioavailable compound (compound 9) was identified and selected for development.
Jin
Haolun
H
Department of Medicinal Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
Wright
Matthew
M
Pastor
Richard
R
Mish
Michael
M
Metobo
Sammy
S
Jabri
Salman
S
Lansdown
Rachael
R
Cai
Ruby
R
Pyun
Peter
P
Tsiang
Manuel
M
Chen
Xiaowu
X
Kim
Choung U
CU
D000284:Administration, Oral; D000818:Animals; D001374:Azacitidine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D001682:Biological Availability; D018360:Crystallography, X-Ray; D004285:Dogs; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans; D009930:Organic Chemicals / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D011760:Pyrrolidinones; D000068898:Raltegravir Potassium; D051381:Rats
D019428:HIV Integrase Inhibitors; D009930:Organic Chemicals; D011760:Pyrrolidinones; D000068898:Raltegravir Potassium; D001374:Azacitidine