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

• Graham R. Lawton,
• Haitao Ji,
• Pavel Martásek,
• Linda J. Roman and
• Richard B. Silverman

Beilstein J. Org. Chem. 2009, 5, No. 28, doi:10.3762/bjoc.5.28

• of Texas Health Science Center, San Antonio, Texas (USA) Department of Pediatrics and Center for Applied Genomics, 1st School of Medicine, Charles University, Prague, Czech Republic 10.3762/bjoc.5.28 Abstract Highly potent and selective inhibitors of neuronal nitric oxide synthase (nNOS) possessing

• potent than the 2-aminopyridine-based analogue. 4-Aminothiazoles were unstable in water, undergoing tautomerization and hydrolysis to give inactive thiazolones. Keywords: 2-aminothiazole; 4-aminothiazole; nitric oxide synthase inhibitor; nNOS; Introduction Neuronal nitric oxide synthase (nNOS) is the

• constitutive isoform of nitric oxide synthase (NOS) found in the CNS. It is believed to play a role in many neurological diseases, including Parkinson’s disease [1], Alzheimer’s disease [2], damage due to stroke [3], and cerebral palsy caused by pre-natal hypoxia [4]. To fully explore the role nNOS plays in