Nitroaromatic amino acids as inhibitors of neuronal nitric oxide synthase.
J Med Chem
; 41(14): 2636-42, 1998 Jul 02.
Article
de En
| MEDLINE
| ID: mdl-9651169
ABSTRACT
Nitric oxide (NO.) is an important biomodulator of many physiological processes. The inhibition of inappropriate production of NO. by the isoforms of nitric oxide synthase (NOS) has been proposed as a therapeutic approach for the treatment of stroke, inflammation, and other processes. In this study, certain 2-nitroaryl-substituted amino acid analogues were discovered to inhibit NOS. Analogues bearing a 5-methyl substituent on the aromatic ring demonstrated maximal inhibitory potency. For two selected inhibitors, investigation of the kinetics of the enzyme showed the inhibition to be competitive with l-arginine. Additionally, functional NOS inhibition in tissue preparations was demonstrated.
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Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Ornithine
/
Nitric oxide synthase
/
Antienzymes
/
Isoenzymes
/
Neurones
/
Composés nitrés
Limites:
Animals
Langue:
En
Journal:
J Med Chem
Sujet du journal:
QUIMICA
Année:
1998
Type de document:
Article
Pays d'affiliation:
États-Unis d'Amérique