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Design, synthesis, and preliminary evaluation of 4-(6-(3-nitroguanidino)hexanamido)pyrrolidine derivatives as potential iNOS inhibitors.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2008 Jan 01; Vol. 16 (1), pp. 578-85. Date of Electronic Publication: 2007 Apr 25. - Publication Year :
- 2008
-
Abstract
- A series of 4-(6-(3-nitroguanidino)hexanamido)pyrrolidine derivatives were synthesized and evaluated for their abilities to inhibit inducible nitric oxide synthase (iNOS) isoform. All target compounds were prepared in 11 steps from commercially trans-4-hydroxy-L-proline. The preliminary pharmacological test showed that three compounds, 17, 21, and 30, have the good potency (IC(50)=2.36, 2.68, 2.5 microM, respectively) which are compared to the NOS inhibitor N(G)-nitroarginine(L-NNA) (IC(50)=14.74 microM), and could be used as lead compounds for exploring new iNOS inhibitors in the future.
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 16
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 17937988
- Full Text :
- https://doi.org/10.1016/j.bmc.2007.04.030