1.
Bioorg Med Chem Lett
; 13(4): 697-700, 2003 Feb 24.
Article
in English
| MEDLINE
| ID: mdl-12639561
ABSTRACT
A novel series of benzamidines was synthesized and shown to exhibit NR2B-subtype selective NMDA antagonist activity. Compound 31 is orally active in a carrageenan-induced rat hyperalgesia model of pain and shows no motor coordination side effects.
Subject(s)
Benzamidines/pharmacology , Receptors, N-Methyl-D-Aspartate/antagonists & inhibitors , Administration, Oral , Animals , Benzamidines/chemical synthesis , Carrageenan , Drug Evaluation, Preclinical , Hyperalgesia/drug therapy , Pain/drug therapy , Psychomotor Performance/drug effects , Rats , Structure-Activity Relationship
2.
J Med Chem
; 46(4): 453-6, 2003 Feb 13.
Article
in English
| MEDLINE
| ID: mdl-12570367
ABSTRACT
Naphthyridine 7 inhibits the strand transfer of the integration process catalyzed by integrase with an IC50 of 10 nM and inhibits 95% of the spread of HIV-1 infection in cell culture at 0.39 microM. It does not exhibit cytotoxicity in cell culture at < or =12.5 microM and shows a good pharmacokinetic profile when dosed orally to rats. The antiviral activity of 7 and its effect on integration were confirmed using viruses with specific integrase mutations.
