3,4-Dihydro-1-isoquinolinamines: a novel class of nitric oxide synthase inhibitors with a range of isoform selectivity and potency

H Beaton; P Hamley; D J Nicholls; A C Tinker; A V Wallace

doi:10.1016/s0960-894x(01)00119-6

3,4-Dihydro-1-isoquinolinamines: a novel class of nitric oxide synthase inhibitors with a range of isoform selectivity and potency

Bioorg Med Chem Lett. 2001 Apr 23;11(8):1023-6. doi: 10.1016/s0960-894x(01)00119-6.

Authors

H Beaton¹, P Hamley, D J Nicholls, A C Tinker, A V Wallace

Affiliation

¹ Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Loughborough, UK.

PMID: 11327580
DOI: 10.1016/s0960-894x(01)00119-6

Abstract

3-Phenyl-3.4-dihydro-1-isoquinolinamine is a weak inhibitor of iNOS and nNOS. Structural variation of 5a results in inhibitors with a range of potency and selectivity for the NOS enzymes, including a potent and very selective iNOS inhibitor 5j.

MeSH terms

Animals
Cells, Cultured
Cerebellum / cytology
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Humans
Inhibitory Concentration 50
Isoquinolines / chemistry
Isoquinolines / pharmacology*
Nitric Oxide Synthase / antagonists & inhibitors*
Nitric Oxide Synthase Type I
Nitric Oxide Synthase Type II
Protein Isoforms / antagonists & inhibitors
Rats
Sensitivity and Specificity

Substances

Enzyme Inhibitors
Isoquinolines
Protein Isoforms
NOS1 protein, human
NOS2 protein, human
Nitric Oxide Synthase
Nitric Oxide Synthase Type I
Nitric Oxide Synthase Type II
Nos1 protein, rat
Nos2 protein, rat