Ontology highlight
ABSTRACT:
SUBMITTER: Jing Q
PROVIDER: S-EPMC3790268 | biostudies-literature | 2013 Oct
REPOSITORIES: biostudies-literature
Jing Qing Q Li Huiying H Chreifi Georges G Roman Linda J LJ Martásek Pavel P Poulos Thomas L TL Silverman Richard B RB
Bioorganic & medicinal chemistry letters 20130814 20
To develop potent and selective nNOS inhibitors, new double-headed molecules with chiral linkers that derive from natural amino acids or their derivatives have been designed. The new structures contain two ether bonds, which greatly simplifies the synthesis and accelerates structure optimization. Inhibitor (R)-6b exhibits a potency of 32nM against nNOS and is 475 and 244 more selective for nNOS over eNOS and iNOS, respectively. Crystal structures show that the additional binding between the amin ...[more]