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Identification and SAR of selective inducible nitric oxide synthase (iNOS) dimerization inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Nov 15; Vol. 21 (22), pp. 6888-94. Date of Electronic Publication: 2011 Sep 08. - Publication Year :
- 2011
-
Abstract
- We have identified and synthesized a series of imidazole containing dimerization inhibitors of inducible nitric oxide synthase (iNOS). The necessity of key imidazole and piperonyl functionality was demonstrated and SAR studies led to the identification of compound 35, which showed a dose dependant inhibition in multiple pain models, including tactile allodynia induced by spinal nerve ligation (Chung model).<br /> (Copyright © 2011 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Enzyme Inhibitors pharmacology
Female
Humans
Imidazoles pharmacology
Nitric Oxide Synthase Type II metabolism
Rats
Rats, Inbred Lew
Enzyme Inhibitors chemistry
Enzyme Inhibitors therapeutic use
Hyperalgesia drug therapy
Imidazoles chemistry
Imidazoles therapeutic use
Nitric Oxide Synthase Type II antagonists & inhibitors
Pain drug therapy
Protein Multimerization drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 21
- Issue :
- 22
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21986586
- Full Text :
- https://doi.org/10.1016/j.bmcl.2011.08.112