A dipyrido [2,3-b:3',2'-f]azepine analog of the HIV-1 reverse transcriptase inhibitor nevirapine.
The syntheses of 11-ethyl and 11-cyclopropyldipyrido[2,3-b:3',2'-f]azepines, analogs of the HIV-1 reverse transcriptase inhibitor nevirapine 1, are described. These compounds exhibit potency equivalent to nevirapine in the inhibition of wild-type and some mutant RT enzymes.
Dyatkin
A B
AB
Department of Chemical Development, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, CT 06877, USA.
Brickwood
J R
JR
Proudfoot
J R
JR
D019943:Amino Acid Substitution; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D054303:HIV Reverse Transcriptase / Q000737:chemistry / Q000378:metabolism*; D006801:Humans; D007700:Kinetics; D015394:Molecular Structure; D016297:Mutagenesis, Site-Directed; D019829:Nevirapine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011994:Recombinant Proteins / Q000737:chemistry / Q000378:metabolism; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D019380:Anti-HIV Agents; D011725:Pyridines; D011994:Recombinant Proteins; D018894:Reverse Transcriptase Inhibitors; D019829:Nevirapine; D054303:HIV Reverse Transcriptase