Naphthoxazepine inhibitors of HIV-1 integrase: synthesis and biological evaluation.
Two sets of compounds derived from the fusion of a diversely annulated naphthoxazepinedione system with 1,3-thiazole and 1,3-oxazole are described. These compounds are close analogues of previously reported thiazolothiazepine inhibitors of human immunodeficiency virus type 1 integrase (HIV-1 IN). Some of the new derivatives show potency similar to that of the reference compounds, thus gaining further insight into the structure-activity relationship of this class of IN inhibitors.
Garofalo
Antonio
A
Dipartimento di Scienze Farmaceutiche, Università della Calabria, 87036 Arcavacata di Rende, Cs, Italy. garofalo@unical.it
Grande
Fedora
F
Brizzi
Antonella
A
Aiello
Francesca
F
Dayam
Raveendra
R
Neamati
Nouri
N
D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D019427:HIV Integrase / Q000187:drug effects*; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D015394:Molecular Structure; D010077:Oxazepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000998:Antiviral Agents; D019428:HIV Integrase Inhibitors; D010077:Oxazepines; D019427:HIV Integrase; C514801:p31 integrase protein, Human immunodeficiency virus 1