Guillon Christophe D, Wisnoski David D, Saxena Jaya, Heindel Ned D, Heck Diane E, Wolff Donald J, Laskin Jeffrey D
Department of Chemistry, Lehigh University, 6 East Packer Avenue, Bethlehem, PA, USA.
Department of Environmental Health Science, New York Medical College, Valhalla, NY, USA.
Mod Res Inflamm. 2014 May;3(2):48-58. doi: 10.4236/mri.2014.32006.
A series of N-nitro-N-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.
已经制备了一系列N-硝基-N-取代胍作为人一氧化氮合酶（NOS）亚型的潜在抑制剂。氨基胍和硝基精氨酸在抑制诱导型一氧化氮合酶（iNOS）方面的报道效用表明硝基胍类似物可能具有类似的效用。该化合物库针对一氧化氮合酶的三种亚型（内皮型一氧化氮合酶（eNOS）、诱导型一氧化氮合酶（iNOS）和神经型一氧化氮合酶（nNOS））进行了测试。几种候选物对神经型一氧化氮合酶（nNOS）表现出优异的活性和良好的选择性。一种特定的化合物甚至对诱导型一氧化氮合酶（iNOS）表现出良好的选择性。讨论了此类选择性抑制剂的潜在用途。
