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Article Title

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Potent and Selective Human Neuronal Nitric Oxide Synthase Inhibition by Optimization of the 2-Aminopyridine-Based Scaffold with a Pyridine Linker.

Northwestern University

Target- and mechanism-based therapeutics for neurodegenerative diseases: strength in numbers.

Northwestern University

Novel nanomolar imidazo[4,5-b]pyridines as selective nitric oxide synthase (iNOS) inhibitors: SAR and structural insights.

Nycomed

Discovery of a potent, orally bioavailable and highly selective human neuronal nitric oxide synthase (nNOS) inhibitor, N-(1-(piperidin-4-yl)indolin-5-yl)thiophene-2-carboximidamide as a pre-clinical development candidate for the treatment of migraine.

Neuraxon

1,2,3,4-tetrahydroquinoline-based selective human neuronal nitric oxide synthase (nNOS) inhibitors: lead optimization studies resulting in the identification of N-(1-(2-(methylamino)ethyl)-1,2,3,4-tetrahydroquinolin-6-yl)thiophene-2-carboximidamide as a preclinical development candidate.

Neuraxon

Synthesis, biological evaluation and molecular docking studies of 3-(triazolyl)-coumarin derivatives: effect on inducible nitric oxide synthase.

Universidade De S£O Paulo

NOpiates: Novel Dual Action Neuronal Nitric Oxide Synthase Inhibitors with µ-Opioid Agonist Activity.

TBA

First-in-class, dual-action, 3,5-disubstituted indole derivatives having human nitric oxide synthase (nNOS) and norepinephrine reuptake inhibitory (NERI) activity for the treatment of neuropathic pain.

Neuraxon

Novel, druglike 1,7-disubstituted 2,3,4,5-tetrahydro-1H-benzo[b]azepine-based selective inhibitors of human neuronal nitric oxide synthase (nNOS).

Neuraxon

Discovery of N-(3-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-1H-indol-6-yl) thiophene-2-carboximidamide as a selective inhibitor of human neuronal nitric oxide synthase (nNOS) for the treatment of pain.

Neuraxon

N(delta)-Methylated L-arginine derivatives and their effects on the nitric oxide generating system.

Christian-Albrechts-University of Kiel

Discovery of a series of aminopiperidines as novel iNOS inhibitors.

Adolor

Novel 2-aminobenzothiazoles as selective neuronal nitric oxide synthase inhibitors.

Neuraxon

Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase.

Merck Research Laboratory

Substituted 6-phenyl-pyridin-2-ylamines: selective and potent inhibitors of neuronal nitric oxide synthase.

Pfizer

5-Fluorinated L-lysine analogues as selective induced nitric oxide synthase inhibitors.

Pfizer

1,2-Dihydro-4-quinazolinamines: potent, highly selective inhibitors of inducible nitric oxide synthase which show antiinflammatory activity in vivo.

Astrazeneca R&D Charnwood

Synthesis and biological characterization of L-N(6)-(1-iminoethyl)lysine 5-tetrazole-amide, a prodrug of a selective iNOS inhibitor.

Pfizer

2-Iminohomopiperidinium salts as selective inhibitors of inducible nitric oxide synthase (iNOS).

Pfizer

2-Iminopyrrolidines as potent and selective inhibitors of human inducible nitric oxide synthase.

Pfizer

N-Phenylamidines as selective inhibitors of human neuronal nitric oxide synthase: structure-activity studies and demonstration of in vivo activity.

Glaxo Wellcome Research and Development

Substituted N-phenylisothioureas: potent inhibitors of human nitric oxide synthase with neuronal isoform selectivity.

Glaxo Wellcome Research and Development

2-Iminopiperidine and other 2-iminoazaheterocycles as potent inhibitors of human nitric oxide synthase isoforms.

G. D. Searle Research and Development

Dihydroquinolines with amine-containing side chains as potent n-NOS inhibitors.

Schering

Inhibition of inducible nitric oxide synthase by acetamidine derivatives of hetero-substituted lysine and homolysine.

Glaxo Wellcome Research and Development

3,5-Disubstituted indole derivatives as selective human neuronal nitric oxide synthase (nNOS) inhibitors.

Neuraxon

Discovery of cis-N-(1-(4-(methylamino)cyclohexyl)indolin-6-yl)thiophene-2-carboximidamide: a 1,6-disubstituted indoline derivative as a highly selective inhibitor of human neuronal nitric oxide synthase (nNOS) without any cardiovascular liabilities.

Neuraxon

Heteroaromatic-aminomethyl quinolones: potent and selective iNOS inhibitors.

Afraxis

Design, synthesis, and biological evaluation of 3,4-dihydroquinolin-2(1H)-one and 1,2,3,4-tetrahydroquinoline-based selective human neuronal nitric oxide synthase (nNOS) inhibitors.

Neuraxon

Identification and SAR of selective inducible nitric oxide synthase (iNOS) dimerization inhibitors.

Kalypsys

1,6-Disubstituted indole derivatives as selective human neuronal nitric oxide synthase inhibitors.

Neuraxon

1,5-Disubstituted indole derivatives as selective human neuronal nitric oxide synthase inhibitors.

Neuraxon

Discovery of dual inducible/neuronal nitric oxide synthase (iNOS/nNOS) inhibitor development candidate 4-((2-cyclobutyl-1H-imidazo[4,5-b]pyrazin-1-yl)methyl)-7,8-difluoroquinolin-2(1H)-one (KD7332) part 2: identification of a novel, potent, and selective series of benzimidazole-quinolinone iNOS/nNO

Kalypsys

Heteroalicyclic carboxamidines as inhibitors of inducible nitric oxide synthase; the identification of (2R)-2-pyrrolidinecarboxamidine as a potent and selective haem-co-ordinating inhibitor.

Glaxosmithkline

Symmetric double-headed aminopyridines, a novel strategy for potent and membrane-permeable inhibitors of neuronal nitric oxide synthase.

Northwestern University

Synthesis, biological evaluation, and docking studies of N-substituted acetamidines as selective inhibitors of inducible nitric oxide synthase.

Universita G. D'Annunzio

 

Inhibition of nitric oxide synthase by benzoxazolones

TBA

 

Conformationally restricted arginine analogues as inhibitors of human nitric oxide synthase

TBA

 

1,2-diaminobenzimidazoles : Selective inhibitors of nitric oxide synthase derived from aminoguanidine

TBA

Design and synthesis of 2-amino-4-methylpyridine analogues as inhibitors for inducible nitric oxide synthase and in vivo evaluation of [18F]6-(2-fluoropropyl)-4-methyl-pyridin-2-amine as a potential PET tracer for inducible nitric oxide synthase.

Washington University

Structural analysis of isoform-specific inhibitors targeting the tetrahydrobiopterin binding site of human nitric oxide synthases.

Sanofi-Aventis

Evaluation of 3-substituted arginine analogs as selective inhibitors of human nitric oxide synthase isozymes.

Nagoya City University

2-Aminopyridines with a shortened amino sidechain as potent, selective, and highly permeable human neuronal nitric oxide synthase inhibitors.

Northwestern University

Bicyclic amidine inhibitors of nitric oxide synthase: discovery of perhydro-iminopyrindine and perhydro-iminoquinoline as potent, orally active inhibitors of inducible nitric oxide synthase.

Merck Research Laboratories

Synthesis of analogs of (1,4)-3- and 5-imino oxazepane, thiazepane, and diazepane as inhibitors of nitric oxide synthases.

Merck Research Laboratories

Optimization of

China Pharmaceutical University

2-aminopyridines as highly selective inducible nitric oxide synthase inhibitors. Differential binding modes dependent on nitrogen substitution.

Astrazeneca R&D Charnwood

Structure-activity relationships of potent, selective inhibitors of neuronal nitric oxide synthase based on the 6-phenyl-2-aminopyridine structure.

Pfizer

Fluorinated dihydroquinolines as potent n-NOS inhibitors.

Schering

3-Hydroxy-4-methyl-5-pentyl-2-iminopyrrolidine: a potent and highly selective inducible nitric oxide synthase inhibitor.

Pharmacia

Dihydroquinolines as novel n-NOS inhibitors.

Schering

Design and synthesis of orally bioavailable inhibitors of inducible nitric oxide synthase. Part 1: synthesis and biological evaluation of dihydropyridin-2-imines.

Fukui Research Institute

Selective heterocyclic amidine inhibitors of human inducible nitric oxide synthase.

Pharmacia

Antiglioma Activity of Aryl and Amido-Aryl Acetamidine Derivatives Targeting iNOS: Synthesis and Biological Evaluation.

University "G. D'Annunzio" of Chieti-Pescara

Thienopyridines: nitric oxide synthase inhibitors with potent in vivo activity.

Astrazeneca R&D Charnwood

3,4-Dihydro-1-isoquinolinamines: a novel class of nitric oxide synthase inhibitors with a range of isoform selectivity and potency.

Astrazeneca R&D Charnwood

Substituted 2-aminopyridines as inhibitors of nitric oxide synthases.

Merck Research Laboratories

Optimization of Blood-Brain Barrier Permeability with Potent and Selective Human Neuronal Nitric Oxide Synthase Inhibitors Having a 2-Aminopyridine Scaffold.

Northwestern University

A new class of selective and potent inhibitors of neuronal nitric oxide synthase.

Pfizer

Synthesis and evaluation of new sulfur-containing L-arginine-derived inhibitors of nitric oxide synthase.

Wake Forest University

First Contact: 7-Phenyl-2-Aminoquinolines, Potent and Selective Neuronal Nitric Oxide Synthase Inhibitors That Target an Isoform-Specific Aspartate.

Northwestern University

Acetamidine lysine derivative, N-(5(S)-amino-6,7-dihydroxyheptyl)ethanimidamide dihydrochloride: a highly selective inhibitor of human inducible nitric oxide synthase.

Searle

Substituted 2-iminopiperidines as inhibitors of human nitric oxide synthase isoforms.

G. D. Searle Research and Development

Synthesis and evaluation of two positron-labeled nitric oxide synthase inhibitors, S-[11C]methylisothiourea and S-(2-[18F]fluoroethyl)isothiourea, as potential positron emission tomography tracers.

Washington University

Nitrile in the Hole: Discovery of a Small Auxiliary Pocket in Neuronal Nitric Oxide Synthase Leading to the Development of Potent and Selective 2-Aminoquinoline Inhibitors.

Northwestern University

Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.

Northwestern University

Improvement of Cell Permeability of Human Neuronal Nitric Oxide Synthase Inhibitors Using Potent and Selective 2-Aminopyridine-Based Scaffolds with a Fluorobenzene Linker.

Northwestern University

Affinity map of bromodomain protein 4 (BRD4) interactions with the histone H4 tail and the small molecule inhibitor JQ1.

Bayer Healthcare

Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology.

Case Western Reserve University

Coupling of metabotropic glutamate receptors 2 and 4 to G alpha 15, G alpha 16, and chimeric G alpha q/i proteins: characterization of new antagonists.

Upr Centre

Pharmacologic characterization of CI-996, a new angiotensin receptor antagonist.

Parke-Davis Pharmaceutical Research

Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.

Emory University