Christophe D Guillon1, David D Wisnoski1, Jaya Saxena1, Ned D Heindel1, Diane E Heck2, Donald J Wolff3, Jeffrey D Laskin4. 1. Department of Chemistry, Lehigh University, 6 East Packer Avenue, Bethlehem, PA, USA. 2. Department of Environmental Health Science, New York Medical College, Valhalla, NY, USA. 3. Department of Pharmacology, Rutgers University - Robert Wood Johnson Medical School, Piscataway, NJ, USA. 4. Department of Environmental and Occupational Medicine, Rutgers University-Robert Wood Johnson Medical School, Piscataway, NJ, USA.
Abstract
A series of Nω-nitro-Nω'-substituted guanidines has been prepared as potential inhibitors of the human Nitric Oxide Synthase (NOS) isoforms. The reported utility of aminoguanidine and nitroarginine in iNOS inhibition points to a potential similar utility for analogs of nitro-guanidine. The compound library was tested against the three isoforms of Nitric Oxide Synthase (eNOS, iNOS and nNOS). Several candidates showed excellent activity and good selectivity for nNOS. One particular compound even demonstrated good selectivity for iNOS. The potential usefulness of such selective inhibitors is discussed.
A series of Nω-nitro-n class="Chemical">Nω'-substituted guanidines has been prepared as potential inhibitors of the humanNitric Oxide Synthase (NOS) isoforms. The reported utility of aminoguanidine and nitroarginine in iNOS inhibition points to a potential similar utility for analogs of nitro-guanidine. The compound library was tested against the three isoforms of Nitric Oxide Synthase (eNOS, iNOS and nNOS). Several candidates showed excellent activity and good selectivity for nNOS. One particular compound even demonstrated good selectivity for iNOS. The potential usefulness of such selective inhibitors is discussed.
Authors: Sherri C Young; Karine M Fabio; Mou-Tuan Huang; Jaya Saxena; Meredith P Harman; Christophe D Guillon; Anna M Vetrano; Diane E Heck; Robert A Flowers; Ned D Heindel; Jeffrey D Laskin Journal: J Appl Toxicol Date: 2011-02-11 Impact factor: 3.446
Authors: R P Casillas; R C Kiser; J A Truxall; A W Singer; S M Shumaker; N A Niemuth; K M Ricketts; L W Mitcheltree; L R Castrejon; J A Blank Journal: J Appl Toxicol Date: 2000-12 Impact factor: 3.446