Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
This paper reports the synthesis and the antiviral properties of new diarylpyrimidine (DAPY) compounds as nonnucleoside reverse transcriptase inhibitors (NNRTIs). The synthesis program around this new DAPY series was further optimized to produce compounds displaying improved activity against a panel of eight clinically relevant single and double mutant strains of human immunodeficiency virus type 1 (HIV-1).
Guillemont
Jerome
J
Medicinal Chemistry Department, Johnson & Johnson Pharmaceutical Research and Development, Campus de Maigremont BP615, Val de Reuil, France. jguillem@prdfr.jnj.com
Pasquier
Elisabeth
E
Palandjian
Patrice
P
Vernier
Daniel
D
Gaurrand
Sandrine
S
Lewi
Paul J
PJ
Heeres
Jan
J
de Jonge
Marc R
MR
Koymans
Lucien M H
LM
Daeyaert
Frits F D
FF
Vinkers
Maarten H
MH
Arnold
Eddy
E
Das
Kalyan
K
Pauwels
Rudi
R
Andries
Koen
K
de Béthune
Marie-Pierre
MP
Bettens
Eva
E
Hertogs
Kurt
K
Wigerinck
Piet
P
Timmerman
Philip
P
Janssen
Paul A J
PA
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D002460:Cell Line; D024882:Drug Resistance, Viral; D054303:HIV Reverse Transcriptase / Q000235:genetics / Q000378:metabolism*; D015497:HIV-1 / Q000187:drug effects* / Q000235:genetics; D006801:Humans; D009154:Mutation; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D019380:Anti-HIV Agents; D011743:Pyrimidines; D018894:Reverse Transcriptase Inhibitors; D054303:HIV Reverse Transcriptase