Development of nitric oxide synthase inhibitors for neurodegeneration and neuropathic pain

Potent and Selective Double-Headed Thiophene-2-carboximidamide Inhibitors of Neuronal Nitric Oxide Synthase for the Treatment of Melanoma

(2014) He Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Simplified 2-Aminoquinoline-Based Scaffold for Potent and Selective Neuronal Nitric Oxide Synthase Inhibition

(2014) Maris A. Cinelli et al.   JOURNAL OF MEDICINAL CHEMISTRY

In search of potent and selective inhibitors of neuronal nitric oxide synthase with more simple structures

(2013) Qing Jing et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Chiral linkers to improve selectivity of double-headed neuronal nitric oxide synthase inhibitors

(2013) Qing Jing et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Microglial CD14 activated by iNOS contributes to neuroinflammation in cerebral ischemia

(2013) Mian Zhou et al.   BRAIN RESEARCH

Structure-Guided Design of Selective Inhibitors of Neuronal Nitric Oxide Synthase

(2013) He Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Target- and Mechanism-Based Therapeutics for Neurodegenerative Diseases: Strength in Numbers

(2013) Paul C. Trippier et al.   JOURNAL OF MEDICINAL CHEMISTRY

Nitric oxide synthase domain interfaces regulate electron transfer and calmodulin activation

(2013) B. C. Smith et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Accessible Chiral Linker to Enhance Potency and Selectivity of Neuronal Nitric Oxide Synthase Inhibitors

(2013) Qing Jing et al.   ACS Medicinal Chemistry Letters

NADPH–cytochrome P450 oxidoreductase: Prototypic member of the diflavin reductase family

(2012) Takashi Iyanagi et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

Intramolecular hydrogen bonding: A potential strategy for more bioavailable inhibitors of neuronal nitric oxide synthase

(2012) Kristin Jansen Labby et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Cyclopropyl- and methyl-containing inhibitors of neuronal nitric oxide synthase

(2012) Huiying Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY

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

(2012) Subhash C. Annedi et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

(2012) Subhash C. Annedi et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

NXN-188, a selective nNOS inhibitor and a 5-HT1B/1D receptor agonist, inhibits CGRP release in preclinical migraine models

(2012) Deepak K Bhatt et al.   CEPHALALGIA

Nitric Oxide: State of the Art in Drug Design

(2012) R.A.M. Serafim et al.   CURRENT MEDICINAL CHEMISTRY

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

(2012) Subhash C. Annedi et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

(2012) Gabriela Mladenova et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2012) Jailall Ramnauth et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selective Monocationic Inhibitors of Neuronal Nitric Oxide Synthase. Binding Mode Insights from Molecular Dynamics Simulations

(2012) He Huang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Arginine-Based Inhibitors of Nitric Oxide Synthase: Therapeutic Potential and Challenges

(2012) Jan Víteček et al.   MEDIATORS OF INFLAMMATION

Nitric Oxide-Mediated Oxidative Damage and the Progressive Demise of Motor Neurons in ALS

(2012) Derek A. Drechsel et al.   NEUROTOXICITY RESEARCH

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

(2012) Paul Renton et al.   ACS Medicinal Chemistry Letters

Voltage-gated calcium channels and disease

(2011) Stuart M. Cain et al.   BIOFACTORS

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

(2011) Shawn Maddaford et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

(2011) Paul Renton et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Symmetric Double-Headed Aminopyridines, a Novel Strategy for Potent and Membrane-Permeable Inhibitors of Neuronal Nitric Oxide Synthase

(2011) Fengtian Xue et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2011) Jailall Ramnauth et al.   JOURNAL OF MEDICINAL CHEMISTRY

Improved Synthesis of Chiral Pyrrolidine Inhibitors and Their Binding Properties to Neuronal Nitric Oxide Synthase

(2011) Fengtian Xue et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery ofN-(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

(2011) Subhash C. Annedi et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2011) Subhash C. Annedi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-based design, synthesis, and profiling of potent and selective neuronal nitric oxide synthase (nNOS) inhibitors with an amidinothiophene hydroxypiperidine scaffold

(2011) Guyan Liang et al.   MedChemComm

Role of Zinc in Isoform-Selective Inhibitor Binding to Neuronal Nitric Oxide Synthase,

(2010) Silvia L. Delker et al.   BIOCHEMISTRY

Structure-based design, synthesis, and biological evaluation of lipophilic-tailed monocationic inhibitors of neuronal nitric oxide synthase

(2010) Fengtian Xue et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Peripheral but crucial: A hydrophobic pocket (Tyr706, Leu337, and Met336) for potent and selective inhibition of neuronal nitric oxide synthase

(2010) Fengtian Xue et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Safety and pharmacokinetics of NXN-188 after single and multiple doses in five phase I, randomized, double-blind, parallel studies in healthy adult volunteers

(2010) David Vaughan et al.   CLINICAL THERAPEUTICS

Exploration of the Active Site of Neuronal Nitric Oxide Synthase by the Design and Synthesis of Pyrrolidinomethyl 2-Aminopyridine Derivatives

(2010) Haitao Ji et al.   JOURNAL OF MEDICINAL CHEMISTRY

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/nNOS Dimerization Inhibitors That Are Orally Active in Pain Models

(2010) Joseph E. Payne et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pharmacological Characterization of KLYP961, a Dual Inhibitor of Inducible and Neuronal Nitric-Oxide Synthases

(2010) K. T. Symons et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Unexpected Binding Modes of Nitric Oxide Synthase Inhibitors Effective in the Prevention of a Cerebral Palsy Phenotype in an Animal Model

(2010) Silvia L Delker et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Pterin-Centered Radical as a Mechanistic Probe of the Second Step of Nitric Oxide Synthase

(2010) Joshua J. Woodward et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Potent, Highly Selective, and Orally BioavailableGem-Difluorinated Monocationic Inhibitors of Neuronal Nitric Oxide Synthase

(2010) Fengtian Xue et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Nitric oxide synthase (NOS) in the trigeminal vascular system and other brain structures related to pain in rats

(2010) Roshni Ramachandran et al.   NEUROSCIENCE LETTERS

Nitric Oxide Signaling in Brain Function, Dysfunction, and Dementia

(2010) Joern R. Steinert et al.   NEUROSCIENTIST

NO synthase: Structures and mechanisms

(2010) Simon Daff   NITRIC OXIDE-BIOLOGY AND CHEMISTRY

Design of Selective Neuronal Nitric Oxide Synthase Inhibitors for the Prevention and Treatment of Neurodegenerative Diseases

(2009) Richard B. Silverman   ACCOUNTS OF CHEMICAL RESEARCH

Selective neuronal nitric oxide synthase inhibitors and the prevention of cerebral palsy

(2009) Haitao Ji et al.   ANNALS OF NEUROLOGY

Synthesis and enzymatic evaluation of 2- and 4-aminothiazole-based inhibitors of neuronal nitric oxide synthase

(2009) Graham R Lawton et al.   Beilstein Journal of Organic Chemistry

Developing Dual and Specific Inhibitors of Dimethylarginine Dimethylaminohydrolase-1 and Nitric Oxide Synthase: Toward a Targeted Polypharmacology To Control Nitric Oxide

(2009) Yun Wang et al.   BIOCHEMISTRY

Analogues of 2-aminopyridine-based selective inhibitors of neuronal nitric oxide synthase with increased bioavailability

(2009) Graham R. Lawton et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Effect of potential amine prodrugs of selective neuronal nitric oxide synthase inhibitors on blood–brain barrier penetration

(2009) Richard B. Silverman et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and in vitro evaluation of pteridine analogues as monoamine oxidase B and nitric oxide synthase inhibitors

(2009) Louis H.A. Prins et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Potent and selective neuronal nitric oxide synthase inhibitors with improved cellular permeability

(2009) Fengtian Xue et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of Highly Potent and Selective Inhibitors of Neuronal Nitric Oxide Synthase by Fragment Hopping

(2009) Haitao Ji et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Inducible Nitric Oxide Synthase (iNOS) Inhibitor Development Candidate KD7332, Part 1: Identification of a Novel, Potent, and Selective Series of Quinolinone iNOS Dimerization Inhibitors that are Orally Active in Rodent Pain Models

(2009) Céline Bonnefous et al.   JOURNAL OF MEDICINAL CHEMISTRY

More than a Retrograde Messenger: Nitric Oxide Needs Two cGMP Pathways to Induce Hippocampal Long-Term Potentiation

(2009) F. Taqatqeh et al.   JOURNAL OF NEUROSCIENCE

Heme-Coordinating Inhibitors of Neuronal Nitric Oxide Synthase. Iron−Thioether Coordination Is Stabilized by Hydrophobic Contacts without Increased Inhibitor Potency

(2009) Jeffrey D. Martell et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Nitric Oxide Activates ATP-Sensitive Potassium Channels in Mammalian Sensory Neurons: Action by Direct S-Nitrosylation

(2009) Takashi Kawano et al.   Molecular Pain

The selective serotonin reuptake inhibitor fluoxetine reduces striatal in vivo levels of voltammetric nitric oxide (NO): A feature of its antidepressant activity?

(2009) Francesco Crespi   NEUROSCIENCE LETTERS

Revisiting Heme Mechanisms. A Perspective on the Mechanisms of Nitric Oxide Synthase (NOS), Heme Oxygenase (HO), and Cytochrome P450s (CYP450s)

(2008) Yaoqiu Zhu et al.   BIOCHEMISTRY

Analogues of 2-phenyl-ethenesulfonic acid phenyl ester have dual functions of inhibiting expression of inducible nitric oxide synthase and activating peroxisome proliferator-activated receptor γ

(2008) Yue-Zhi Lee et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Minimal Pharmacophoric Elements and Fragment Hopping, an Approach Directed at Molecular Diversity and Isozyme Selectivity. Design of Selective Neuronal Nitric Oxide Synthase Inhibitors

(2008) Haitao Ji et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Comparative pharmacological study of free radical scavenger, nitric oxide synthase inhibitor, nitric oxide synthase activator and cyclooxygenase inhibitor against MPTP neurotoxicity in mice

(2008) Hironori Yokoyama et al.   METABOLIC BRAIN DISEASE

Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase

(2008) Elsa D Garcin et al.   Nature Chemical Biology

Modification of Nitric Oxide Synthase Activity and Neuronal Response in Rat Striatum by Melatonin and Kynurenine Derivatives

(2003) Josefa León et al.   JOURNAL OF NEUROENDOCRINOLOGY