Applications of Organocatalytic Asymmetric Synthesis to Drug Prototypes—Dual Action and Selective Inhibitors ofn-Nitric Oxide Synthase with Activity Against the 5-HT1D/1BSubreceptors

2011 ◽  
Vol 13 (5) ◽  
pp. 840-843 ◽  
Author(s):  
Stephen Hanessian ◽  
Eli Stoffman ◽  
Xueling Mi ◽  
Paul Renton
Keyword(s):  
Nitric Oxide ◽  
Nitric Oxide Synthase ◽  
Asymmetric Synthesis ◽  
Selective Inhibitors ◽  
Dual Action ◽  
Oxide Synthase

scholarly journals Synthesis and enzymatic evaluation of 2- and 4-aminothiazole-based inhibitors of neuronal nitric oxide synthase

2009 ◽  
Vol 5 ◽  
Author(s):  
Graham R Lawton ◽  
Haitao Ji ◽  
Pavel Martásek ◽  
Linda J Roman ◽  
Richard B Silverman
Keyword(s):  
Nitric Oxide ◽  
Nitric Oxide Synthase ◽  
Blood Brain Barrier ◽  
Neuronal Nitric Oxide Synthase ◽  
Lead Compound ◽  
Selective Inhibitors ◽  
Net Charge ◽  
In Vivo Efficacy ◽  
Oxide Synthase

Highly potent and selective inhibitors of neuronal nitric oxide synthase (nNOS) possessing a 2-aminopyridine group were recently designed and synthesized in our laboratory and were shown to have significant in vivo efficacy. In this work, analogs of our lead compound possessing 2- and 4-aminothiazole rings in place of the aminopyridine were synthesized. The less basic aminothiazole rings will be less protonated at physiological pH than the aminopyridine ring, and so the molecule will carry a lower net charge. This could lead to an increased ability to cross the blood-brain barrier thereby increasing the in vivo potency of these compounds. The 2-aminothiazole-based compound was less potent than the 2-aminopyridine-based analogue. 4-Aminothiazoles were unstable in water, undergoing tautomerization and hydrolysis to give inactive thiazolones.

N-Substituted acetamidines and 2-methylimidazole derivatives as selective inhibitors of neuronal nitric oxide synthase

2010 ◽  
Vol 20 (22) ◽  
pp. 6495-6499 ◽  
Author(s):  
Cristina Maccallini ◽  
Antonia Patruno ◽  
Fabio Lannutti ◽  
Alessandra Ammazzalorso ◽  
Barbara De Filippis ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Nitric Oxide Synthase ◽  
Neuronal Nitric Oxide Synthase ◽  
Selective Inhibitors ◽  
Oxide Synthase

Nω-Nitroarginine-Containing Dipeptide Amides. Potent and Highly Selective Inhibitors of Neuronal Nitric Oxide Synthase

1999 ◽  
Vol 42 (16) ◽  
pp. 3147-3153 ◽  
Author(s):  
Hui Huang ◽  
Pavel Martasek ◽  
Linda J. Roman ◽  
Bettie Sue Siler Masters ◽  
Richard B. Silverman
Keyword(s):  
Nitric Oxide ◽  
Nitric Oxide Synthase ◽  
Neuronal Nitric Oxide Synthase ◽  
Selective Inhibitors ◽  
Oxide Synthase

scholarly journals Effects of Selective Inhibitors of Nitric Oxide Synthase-2 Dimerization on Acute Cardiac Allograft Rejection

Circulation ◽  
2002 ◽  
Vol 106 (18) ◽  
pp. 2392-2396 ◽  
Author(s):  
Matthias J. Szabolcs ◽  
Ji Sun ◽  
Ningsheng Ma ◽  
Arline Albala ◽  
Robert R. Sciacca ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Nitric Oxide Synthase ◽  
Allograft Rejection ◽  
Cardiac Allograft ◽  
Selective Inhibitors ◽  
Cardiac Allograft Rejection ◽  
Nitric Oxide Synthase 2 ◽  
Oxide Synthase

Fluorinated indazoles as novel selective inhibitors of nitric oxide synthase (NOS): Synthesis and biological evaluation

2009 ◽  
Vol 17 (17) ◽  
pp. 6180-6187 ◽  
Author(s):  
Rosa M. Claramunt ◽  
Concepción López ◽  
Carlos Pérez-Medina ◽  
Marta Pérez-Torralba ◽  
José Elguero ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Nitric Oxide Synthase ◽  
Biological Evaluation ◽  
Selective Inhibitors ◽  
Oxide Synthase ◽  
Synthesis And Biological Evaluation
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