Design, synthesis, and structure-activity relationships of 1,3-dihydrobenzimidazol-2-one analogues as anti-HIV agents.
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) have become very important components in the antiretroviral combination therapies used to treat HIV. Recently, our group identified some 1,3-dihydrobenzimidazol-2-one derivatives and their sulfones as a potent and novel class of NNRTIs. We herein report the synthesis and biological evaluation of the new compounds in which different structural modifications have been introduced in order to investigate their effects on RT inhibition.
Monforte
Anna-Maria
AM
Dipartimento Farmaco-Chimico, Università di Messina, Italy. ammonforte@pharma.unime.it
Logoteta
Patrizia
P
Ferro
Stefania
S
De Luca
Laura
L
Iraci
Nunzio
N
Maga
Giovanni
G
Clercq
Erik De
ED
Pannecouque
Christophe
C
Chimirri
Alba
A
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D015195:Drug Design; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D019380:Anti-HIV Agents; D001562:Benzimidazoles; D018894:Reverse Transcriptase Inhibitors; C014353:benzimidazolone; D054303:HIV Reverse Transcriptase