title: Nω-NITRO-Nω'-SUBSTITUTED GUANIDINES: A SIMPLE CLASS OF NITRIC OXIDE SYNTHASE INHIBITORS.
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.
authors.affiliation: Department of Chemistry, Lehigh University, 6 East Packer Avenue, Bethlehem, PA, USA.
authors.forename: Christophe D
authors.initials: CD
authors.lastname: Guillon
authors.affiliation: Department of Chemistry, Lehigh University, 6 East Packer Avenue, Bethlehem, PA, USA.
authors.forename: David D
authors.initials: DD
authors.lastname: Wisnoski
authors.affiliation: Department of Chemistry, Lehigh University, 6 East Packer Avenue, Bethlehem, PA, USA.
authors.forename: Jaya
authors.initials: J
authors.lastname: Saxena
authors.affiliation: Department of Chemistry, Lehigh University, 6 East Packer Avenue, Bethlehem, PA, USA.
authors.forename: Ned D
authors.initials: ND
authors.lastname: Heindel
authors.affiliation: Department of Environmental Health Science, New York Medical College, Valhalla, NY, USA.
authors.forename: Diane E
authors.initials: DE
authors.lastname: Heck
authors.affiliation: Department of Pharmacology, Rutgers University - Robert Wood Johnson Medical School, Piscataway, NJ, USA.
authors.forename: Donald J
authors.initials: DJ
authors.lastname: Wolff
authors.affiliation: Department of Environmental and Occupational Medicine, Rutgers University-Robert Wood Johnson Medical School, Piscataway, NJ, USA.
authors.forename: Jeffrey D
authors.initials: JD
authors.lastname: Laskin
keywords: Nitric Oxide Synthase (NOS); Nitro-guanidines; isoforms; selective inhibitors