Selective Inhibition of iNOS by Benzyl‐ and Dibenzyl Derivatives of  N ‐(3‐Aminobenzyl)acetamidine | Zendy

Fantacuzzi Marialuigia | Zendy; Maccallini Cristina | Zendy; Lannutti Fabio | Zendy; Patruno Antonia | Zendy; Masella Simona | Zendy; Pesce Mirko | Zendy; Speranza Lorenza | Zendy; Ammazzalorso Alessandra | Zendy; De Filippis Barbara | Zendy; Giampietro Letizia | Zendy; Re Nazzareno | Zendy; Amoroso Rosa | Zendy

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Selective Inhibition of iNOS by Benzyl‐ and Dibenzyl Derivatives of N ‐(3‐Aminobenzyl)acetamidine

Author(s) -

Fantacuzzi Marialuigia,

Maccallini Cristina,

Lannutti Fabio,

Patruno Antonia,

Masella Simona,

Pesce Mirko,

Speranza Lorenza,

Ammazzalorso Alessandra,

De Filippis Barbara,

Giampietro Letizia,

Re Nazzareno,

Amoroso Rosa

Publication year - 2011

Publication title -

chemmedchem

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.817

H-Index - 100

eISSN - 1860-7187

pISSN - 1860-7179

DOI - 10.1002/cmdc.201100125

Subject(s) - enos , amine gas treating , chemistry , docking (animal) , stereochemistry , selectivity , nitro , derivative (finance) , pharmacology , combinatorial chemistry , nitric oxide , biochemistry , nitric oxide synthase , organic chemistry , medicine , business , alkyl , nursing , catalysis , finance

Picking your NOS: The effect of amine substitution at the 3‐aminomethyl group of known iNOS inhibitor W1400 with mono‐ or disubstituted benzylic groups was evaluated. The o ‐nitro‐benzyl derivative was identified as a potent inhibitor of iNOS, with good selectivity over eNOS. Docking simulations were performed to predict the binding mode of these derivatives in the iNOS and eNOS active sites.

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