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  • Title: Synthesis, pharmacological study and modeling of 7-methoxyindazole and related substituted indazoles as neuronal nitric oxide synthase inhibitors.
    Author: Collot V, Sopkova-de Oliveira Santos J, Schumann-Bard P, Colloc'h N, Mackenzie ET, Rault S.
    Journal: J Enzyme Inhib Med Chem; 2003 Apr; 18(2):195-9. PubMed ID: 12943204.
    Abstract:
    The synthesis, pharmacological evaluation and modelisation of 7-methoxyindazole (7-MI) and related alkoxyindazoles as novel inhibitors of neuronal nitric oxide synthase are presented. 7-MI remains the most active compound of this series in an in vitro enzymatic assay of neuronal nitric oxide synthase activity. Modeling studies of the interaction of 7-substituted indazole derivatives complexed with nNOS and the relationship with their respective biological activities suggest that a bulky substitution on position-7 is responsible for a steric hindrance effect which does not allow these compounds to interact with nNOS in the same way as 7-NI and 7-MI.
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