Tricyclic HIV integrase inhibitors V. SAR studies on the benzyl moiety.
SAR studies on the para-fluorobenzyl moiety of tricyclic HIV integrase inhibitors are discussed and lead compounds with potency and PK properties comparable to raltegravir were identified.
Jin
Haolun
H
Gilead Sciences, Inc, Foster City, CA 94404, USA. hjin@gilead.com
Metobo
Sammy
S
Jabri
Salman
S
Mish
Michael
M
Lansdown
Rachael
R
Chen
Xiaowu
X
Tsiang
Manuel
M
Wright
Matthew
M
Kim
Choung U
CU
D000818:Animals; D019380:Anti-HIV Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D001667:Binding, Competitive / Q000502:physiology; D001682:Biological Availability; D002460:Cell Line; D004285:Dogs; D005464:Fluorobenzenes / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D019428:HIV Integrase Inhibitors / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D051381:Rats; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D019380:Anti-HIV Agents; D005464:Fluorobenzenes; D019428:HIV Integrase Inhibitors