2. Academic Validation
  3. Thienopyridines: nitric oxide synthase inhibitors with potent in vivo activity

Thienopyridines: nitric oxide synthase inhibitors with potent in vivo activity

  • Bioorg Med Chem Lett. 2001 Apr 23;11(8):1027-30. doi: 10.1016/s0960-894x(01)00120-2.
H Beaton 1,  N Boughton-Smith,  P Hamley,  A Ghelani,  D J Nicholls,  A C Tinker,  A V Wallace
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Loughborough, UK.
PMID: 11327581 DOI: 10.1016/s0960-894x(01)00120-2
Abstract

5-Substituted 7-amino-4,5-tetrahydrothieno[2,3-c]pyridines and 6-substituted 4-amino-6,7-dihydrothieno[3,2-c]pyridines were shown to be exceptionally potent inhibitors of inducible and neuronal nitric oxide synthase. Selectivity and potency could be modulated by variation of the 5- or 6-substituent. Compound 3e showed potent in vivo inhibition of iNOS.

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