PMID: 7525961Nov 11, 1994Paper

L-N6-(1-iminoethyl)lysine: a selective inhibitor of inducible nitric oxide synthase

Journal of Medicinal Chemistry
W M MooreM G Currie

Abstract

L-N6-(1-Iminoethyl)lysine (L-NIL) has been synthesized and is shown to be both a potent and selective inhibitor of mouse inducible nitric oxide synthase (miNOS). L-NIL has an IC50 of 3.3 microM for miNOS compared to an IC50 of 92 microM for rat brain constitutive NOS indicating that L-NIL is 28-fold more selective for inducible NOS. L-N5-(1-Iminoethyl)ornithine (L-NIO), which differs from L-NIL by having one less methylene group, has very similar potency for inducible NOS, but lacks selectivity. DL-N7-(1-Iminoethyl)homolysine was also synthesized and found to be substantially less potent than L-NIL or L-NIO, with intermediate selectivity for inducible NOS. These data suggest that L-NIL may be useful as a selective inhibitor of inducible NOS for determining the role of this enzyme in disease models.

Citations

Jul 12, 2002·Medicinal Research Reviews·Christos A Kontogiorgis, Dimitra Hadjipavlou-Litina
Dec 18, 2010·Bulletin of Experimental Biology and Medicine·M I RemizovaN I Kochetygov
May 15, 1996·European Journal of Pharmacology·D SalveminiP T Manning
Oct 14, 2003·Bioorganic & Medicinal Chemistry Letters·Claire L M GoodyerMichael D Threadgill
May 1, 1997·Disease-a-month : DM·R G KilbournC Szabó
Aug 12, 1999·European Journal of Pharmacology·J C StocletA L Kleschyov
Jun 20, 2002·Journal of Immunological Methods·James F CurtinThomas G Cotter
Dec 18, 2001·Pharmacology & Therapeutics·F FeihlL Liaudet
Sep 24, 2002·Pharmacology & Therapeutics·B J Nevin, K J Broadley
Nov 22, 2000·Brain Research. Brain Research Reviews·V PrevotJ Beauvillain
Dec 29, 2000·Journal of Chromatography. B, Biomedical Sciences and Applications·U WernerH Guehring
May 3, 2003·Free Radical Biology & Medicine·Salvatore CuzzocreaGiovanni Musci
Aug 17, 2002·Bioorganic & Medicinal Chemistry Letters·Stefan JarochFiona M McDonald
Jun 5, 2003·Bioorganic & Medicinal Chemistry Letters·Stefan JarochFiona M McDonald
Oct 26, 1999·Bioorganic & Medicinal Chemistry·Y LeeR B Silverman
Dec 24, 2003·European Journal of Cardio-thoracic Surgery : Official Journal of the European Association for Cardio-thoracic Surgery·Jürgen H FischerFerdinand Kuhn-Régnier
Sep 16, 1998·Current Opinion in Chemical Biology·B R Babu, O W Griffith
Jul 30, 2002·Autonomic Neuroscience : Basic & Clinical·Christine Vayssettes-CourchayTony J Verbeuren
May 8, 2000·The Journal of Peptide Research : Official Journal of the American Peptide Society·K J KennedyT A Dix
Dec 4, 2002·Nature Reviews. Drug Discovery·Patrick Vallance, James Leiper

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.