M. Cowart

发表

Novel heterocyclic-substituted benzofuran histamine H3 receptor antagonists: in vitro properties, drug-likeness, and behavioral activity.

K. Browman, Jill M. Wetter, G. Diaz, 2007, Biochemical pharmacology.

An Expedient and Multikilogram Synthesis of a Naphthalenoid H3 Antagonist

A. Bhatia, Y. Ku, M. Cowart, 2007 .

D‐Amino Acid Homopiperazine Amides: Discovery of A‐320436, a Potent and Selective Non‐Imidazole Histamine H3‐Receptor Antagonist

G. Fox, A. Hancock, T. Pagano, 2004 .

Structure-activity relationships of arylbenzofuran H3 receptor antagonists.

A. Hancock, T. Esbenshade, M. Cowart, 2005, Bioorganic & medicinal chemistry letters.

Distinctions and contradistinctions between antiobesity histamine H3 receptor (H3R) antagonists compared to cognition-enhancing H3 receptor antagonists

E. Bush, A. Hancock, R. Bitner, 2006, Inflammation Research.

A robust and high-capacity [(35)S]GTPgammaS binding assay for determining antagonist and inverse agonist pharmacological parameters of histamine H(3) receptor ligands.

J. Brioni, T. Esbenshade, M. Cowart, 2008, Assay and drug development technologies.

Histamine H3 receptor antagonists: preclinical promise for treating obesity and cognitive disorders.

G. Fox, T. Esbenshade, M. Cowart, 2006, Molecular interventions.

5-(3-Bromophenyl)-7-(6-morpholin-4-ylpyridin-3-yl)pyrido[2,3-d]pyrimidin-4-ylamine: structure-activity relationships of 7-substituted heteroaryl analogs as non-nucleoside adenosine kinase inhibitors.

A. Gomtsyan, R. Snyder, Chih-Hung Lee, 2005, Bioorganic & medicinal chemistry.

Discovery of histamine H 3 antagonists for the treatment of cognitive disorders and Alzheimer ’ s disease

J. Brioni, T. Esbenshade, M. Cowart, 2010 .

Pharmacological characterization of A-960656, a histamine H₃ receptor antagonist with efficacy in animal models of osteoarthritis and neuropathic pain.

Jill M. Wetter, G. Diaz, J. Brioni, 2012, European journal of pharmacology.

JPET Miniseries : H 3 Receptors Discovery of Histamine H 3 Antagonists for the Treatment of Cognitive Disorders and Alzheimer ’ s Disease

J. Brioni, T. Esbenshade, M. Cowart, 2010 .

Efficacy in Cognition and Schizophrenia of a Potent and Selective Histamine H 3 Receptor Antagonist

Min Zhang, K. Browman, Jill M. Wetter, 2005 .

A-134974: a novel adenosine kinase inhibitor, relieves tactile allodynia via spinal sites of action in peripheral nerve injured rats

M. Jarvis, J. Mikusa, S. McGaraughty, 2001, Brain Research.

Cloning and expression of the adenosine kinase gene from rat and human tissues.

R. Simmer, D. Halbert, S. Dorwin, 1997, Biochemical and biophysical research communications.

Molecular recognition in aqueous media. Conformationally restricted water-soluble cyclophanes derived from 6H,12H-5,11-methanodibenzo[b,f][1,5]diazocine.

C. Wilcox, M. Cowart, I. Sucholeiki, 1988, Journal of the American Chemical Society.

New approaches to synthetic receptors. Studies on the synthesis and properties of macrocyclic C-glycosyl compounds as chiral, water-soluble cyclophanes.

C. Wilcox, M. Cowart, 1987, Carbohydrate research.

Minimization of potential hERG liability in histamine H3 receptor antagonists

K. Browman, G. Diaz, J. Brioni, 2008, Inflammation Research.

2-[4-(3,4-Dimethylphenyl)piperazin-1-ylmethyl]-1H benzoimidazole (A-381393), a selective dopamine D4 receptor antagonist

D. Donnelly-roberts, Jill M. Wetter, M. Nakane, 2005, Neuropharmacology.

In vitro studies on a class of quinoline containing histamine H3 antagonists.

G. Diaz, J. Brioni, Ruth L. Martin, 2010, Bioorganic & medicinal chemistry letters.

Pharmacological properties and pro-cognitive effects of ABT-288, a potent and selective histamine H 3 receptor antagonist

K. Browman, J. Sullivan, J. Brioni, 2012 .

New approaches to synthetic receptors. Synthesis and host properties of a water soluble macrocyclic analog of Tröger's base

C. Wilcox, M. Cowart, 1986 .

Behavior of a cross-linked attachment site: testing the role of branch migration in site-specific recombination.

S. Benkovic, H. Nash, M. Cowart, 1991, Journal of molecular biology.

Fluorescent benzofuran histamine H3 receptor antagonists with sub-nanomolar potency

A. Hancock, T. Esbenshade, M. Cowart, 2006, Inflammation Research.

Pharmacological Properties and Procognitive Effects of ABT-288, a Potent and Selective Histamine H3 Receptor Antagonist

Min Zhang, Min Zhang, K. Browman, 2012, Journal of Pharmacology and Experimental Therapeutics.

Use of the H3 receptor antagonist radioligand [3H]‐A‐349821 to reveal in vivo receptor occupancy of cognition enhancing H3 receptor antagonists

K. Browman, J. Brioni, J. Bauch, 2009, British journal of pharmacology.

Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction.

D. Donnelly-roberts, Jill M. Wetter, G. Gintant, 2006, Journal of medicinal chemistry.

Synthesis, potency, and in vivo profiles of quinoline containing histamine H3 receptor inverse agonists.

K. Browman, Jill M. Wetter, R. Fryer, 2007, Journal of medicinal chemistry.

Uninjured Rats Dynamic Range Neurons in CFA-Treated and Selective TRPV1 Receptor Antagonist, on Wide Systemic and Site-Specific Effects of A-425619, a

J. Brioni, A. Swensen, Lance Lee, 2015 .

An efficient and convergent synthesis of the potent and selective H3 antagonist ABT-239

A. Bhatia, Y. Ku, M. Cowart, 2006 .

A Facile and Scaleable Synthesis of ABT-239, A Benzofuranoid H3 Antagonist

A. Gupta, A. Bhatia, Y. Ku, 2005 .

Synthesis of phosphorus-containing amino acid analogs as inhibitors of nitric oxide synthase

E. Kowaluk, J. Kerwin, M. Cowart, 1996 .

A new class of potent non-imidazole H(3) antagonists: 2-aminoethylbenzofurans.

A. Hancock, A. Stewart, T. Esbenshade, 2004, Bioorganic & medicinal chemistry letters.

In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.

T. Vortherms, A. Hancock, Marlon D Cowart, 2008, Bioorganic & medicinal chemistry letters.

4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.

J. Sullivan, G. Fox, A. Hancock, 2005, Journal of medicinal chemistry.

Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models.

Jill M. Wetter, M. McPherson, J. Sullivan, 2008, Journal of medicinal chemistry.

Discovery of 4-amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin-3-yl)pyrido[2,3-d]pyrimidine, an orally active, non-nucleoside adenosine kinase inhibitor..

M. Williams, S. Bhagwat, M. Jarvis, 2001, Journal of medicinal chemistry.

Analgesic and anti-inflammatory effects of A-286501, a novel orally active adenosine kinase inhibitor

Chih-Hung Lee, M. Jarvis, J. Mikusa, 2002, Pain.

Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists.

Bruce Clapham, Bin Li, A. Gomtsyan, 2016, Journal of medicinal chemistry.

Synthesis of Novel Carbocyclic Adenosine Analogues as Inhibitors of Adenosine Kinase

J. Kerwin, M. Cowart, M. J. Bennett, 1999 .

International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors

Rob Leurs, Holger Stark, H. Haas, 2015, Pharmacological Reviews.

Process for preparing amine type substituted benzofurans

A. Gupta, Y. Ku, M. Cowart, 2003 .

The histamine H3 receptor: an attractive target for the treatment of cognitive disorders

K. Browman, R. Bitner, J D Brioni, 2008, British journal of pharmacology.

Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency.

Jill M. Wetter, A. Hancock, K. Marsh, 2005, Journal of medicinal chemistry.

Pharmacological Properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: II. Neurophysiological Characterization and Broad Preclinical Efficacy in Cognition and Schizophrenia of a Potent and Selective Histamine H3 Receptor Antagonist

Min Zhang, K. Browman, Jill M. Wetter, 2005, Journal of Pharmacology and Experimental Therapeutics.

Pharmacological Properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and Selective Histamine H3 Receptor Antagonist with Drug-Like Properties

Thomas R. Miller, Gerard B. Fox, Jill M. Wetter, 2005, Journal of Pharmacology and Experimental Therapeutics.

A novel combined chemical-enzymatic synthesis of cross-linked DNA using a nucleoside triphosphate analogue.

S. Benkovic, M. Cowart, 1991, Biochemistry.

Anticonvulsant and antinociceptive actions of novel adenosine kinase inhibitors.

M. Jarvis, R. Berman, S. McGaraughty, 2005, Current topics in medicinal chemistry.

DNA substrate structural requirements for the exonuclease and polymerase activities of procaryotic and phage DNA polymerases.

S. Benkovic, K. Gibson, D. Allen, 1989, Biochemistry.

Structure-activity studies on a series of a 2-aminopyrimidine-containing histamine H4 receptor ligands.

Jill M. Wetter, U. Warrior, M. McPherson, 2008, Journal of medicinal chemistry.

Recent developments in the discovery of novel adenosine kinase inhibitors: mechanism of action and therapeutic potential.

M. Jarvis, S. McGaraughty, M F Jarvis, 2006, CNS drug reviews.

Adenosine kinase inhibitors: polar 7-substitutent of pyridopyrimidine derivatives improving their locomotor selectivity.

Chih-Hung Lee, Changcheng Zhu, M. Jarvis, 2003, Bioorganic & medicinal chemistry letters.

Structure-activity studies of 5-substituted pyridopyrimidines as adenosine kinase inhibitors.

S. Bhagwat, E. Bayburt, M. Jarvis, 2001, Bioorganic & medicinal chemistry letters.

PII: S0304-3959(01)00435-3

Chih-Hung Lee, M. Jarvis, J. Mikusa, 2002 .

Effects of A-134974, a novel adenosine kinase inhibitor, on carrageenan-induced inflammatory hyperalgesia and locomotor activity in rats: evaluation of the sites of action.

M. Jarvis, J. Mikusa, S. McGaraughty, 2001, The Journal of pharmacology and experimental therapeutics.

A mutant of DNA polymerase I (Klenow fragment) with reduced fidelity.

S. Benkovic, S. Carroll, M. Cowart, 1991, Biochemistry.

In Vitro Preclinical Cardiac Assessment of Tolterodine and Terodiline: Multiple Factors Predict the Clinical Experience

Gary A Gintant, Zhi Su, G. Gintant, 2006, Journal of cardiovascular pharmacology.

Medicinal chemistry and biological properties of non-imidazole histamine H3 antagonists.

A. Hancock, M. Cowart, R. Faghih, 2004, Mini reviews in medicinal chemistry.

Antagonism of Supraspinal Histamine H3 Receptors Modulates Spinal Neuronal Activity in Neuropathic Rats

J. Brioni, S. McGaraughty, K. Chu, 2012, Journal of Pharmacology and Experimental Therapeutics.

H4 receptor antagonism exhibits anti-nociceptive effects in inflammatory and neuropathic pain models in rats

Jill M. Wetter, J. Brioni, S. Baker, 2010, Pharmacology Biochemistry and Behavior.

Antinociceptive effects of histamine H3 receptor antagonist in the preclinical models of pain in rats and the involvement of central noradrenergic systems

Jill M. Wetter, J. Brioni, M. Decker, 2010, Brain Research.

Identification of GLPG/ABBV-2737, a Novel Class of Corrector, Which Exerts Functional Synergy With Other CFTR Modulators

L. Nelles, P. Stouten, Ashvani K. Singh, 2019, Front. Pharmacol..

and Alzheimer's disease

J. Brioni, Jorge D. Brioni, Tim A. Esbenshade, 2010 .

Discovery of GLPG2451, a Novel Once Daily Potentiator for the Treatment of Cystic Fibrosis.

K. Conrath, C. Menet, M. Andrews, 2021, Journal of medicinal chemistry.

Diaryldiamines with dual inhibition of the histamine H(3) receptor and the norepinephrine transporter and the efficacy of 4-(3-(methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in pain.

Jill M. Wetter, J. Brioni, P. Honore, 2010, Journal of medicinal chemistry.

Histamine receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database

H. Haas, J. Schwartz, R. Thurmond, 2019, IUPHAR/BPS Guide to Pharmacology CITE.

An 80-Amino Acid Deletion in the Third Intracellular Loop of a Naturally Occurring Human Histamine H3 Isoform Confers Pharmacological Differences and Constitutive Activity

R. Leurs, G. Bongers, P. van Meer, 2007, Journal of Pharmacology and Experimental Therapeutics.

4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration.

Youssef L Bennani, A. Hancock, K. Marsh, 2007, Bioorganic & medicinal chemistry letters.

Pharmacological Properties of ABT-239: II. Neurophysiological Characterization and Broad Preclinical Efficacy in Cognition and Schizophrenia of a Potent and Selective Histamine H3 Receptor Antagonist

K. Browman, Jill M. Wetter, R. Porsolt, 2004 .

Discovery of Histamine H3 Antagonists for the Treatment of Cognitive Disorders and Alzheimer's Disease

J. Brioni, Tiffany Runyan Garrison, Jorge D Brioni, 2011, Journal of Pharmacology and Experimental Therapeutics.

Activation of dopamine D4 receptors by ABT-724 induces penile erection in rats.

D. Donnelly-roberts, J. Sullivan, M. Nakane, 2004, Proceedings of the National Academy of Sciences of the United States of America.

Kinetic and structural investigations of the replicative fidelity of the Klenow fragment.

S. Benkovic, R. Kuchta, D. Allen, 1988, Biochemical Society Transactions.

1H, 15N and 13C resonance assignments, secondary structure, and the conformation of substrate in the binary folate complex of Escherichia coli dihydrofolate reductase

P. Wright, S. Benkovic, A. Palmer, 1994, Journal of biomolecular NMR.

Selective H3 receptor (H3R) blockade: broad efficacy in cognition and schizophrenia.

K. Browman, J. Sullivan, M. E. Ballard, 2005, Inflammation Research.

Synthesis and structure-activity relationships of 5-heteroatom-substituted pyridopyrimidines as adenosine kinase inhibitors.

A. Gomtsyan, Chih-Hung Lee, S. Bhagwat, 2003, European journal of medicinal chemistry.

Synthesis and Structure—Activity Relationships of 5-Heteroatom-Substituted Pyridopyrimidines as Adenosine Kinase Inhibitors.

A. Gomtsyan, Chih-Hung Lee, S. Bhagwat, 2003 .

The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.

K. Browman, Jill M. Wetter, A. Hancock, 2008, Journal of medicinal chemistry.

Discovery of histamine H 3 antagonists for the treatment of cognitive disorders and Alzheimer ’ s disease

J. Brioni, T. Esbenshade, M. Cowart, 2010 .

cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.

Jill M. Wetter, J. Brioni, P. Chandran, 2008, Journal of medicinal chemistry.

Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction.

D. Donnelly-roberts, J. Sullivan, M. Nakane, 2004, Journal of medicinal chemistry.

Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning.

D. Donnelly-roberts, J. Sullivan, M. Nakane, 2004, Journal of medicinal chemistry.

Rigidified 2-aminopyrimidines as histamine H4 receptor antagonists: effects of substitution about the rigidifying ring.

J. Brioni, T. Esbenshade, M. Cowart, 2010, Bioorganic & medicinal chemistry letters.

In vitro and in vivo characterization of A‐940894: a potent histamine H4 receptor antagonist with anti‐inflammatory properties

J. Wetter, B. Yao, C. Cuff, 2009, British journal of pharmacology.

Nitroaromatic amino acids as inhibitors of neuronal nitric oxide synthase.

E. Kowaluk, J. Kerwin, M. Cowart, 1998, Journal of Medicinal Chemistry.

Histamine receptors in GtoPdb v.2021.3

H. Haas, J. Schwartz, R. Thurmond, 2021, IUPHAR/BPS Guide to Pharmacology CITE.

Design of adenosine kinase inhibitors from the NMR-based screening of fragments.

Jean M. Severin, E A Kowaluk, P. Hajduk, 2000, Journal of medicinal chemistry.

Antiobesity evaluation of histamine H3 receptor (H3R) antagonist analogs of A-331440 with improved safety and efficacy

E. Bush, A. Hancock, P. Jacobson, 2005, Inflammation Research.

In vitro optimization of structure activity relationships of analogues of A-331440 combining radioligand receptor binding assays and micronucleus assays of potential antiobesity histamine H3 receptor antagonists.

E. Bush, A. Hancock, P. Jacobson, 2004, Basic & clinical pharmacology & toxicology.

Crystal structures of human adenosine kinase inhibitor complexes reveal two distinct binding modes.

Jean M. Severin, A. Gomtsyan, S. Muchmore, 2006, Journal of Medicinal Chemistry.

Isoform dependent differences in histamine H3 receptor constitutive activity revealed by human H3(445) and H3(365) receptors.

J. Brioni, A. Hancock, T. Esbenshade, 2007 .

Lack of efficacy of melanin-concentrating hormone-1 receptor antagonists in models of depression and anxiety.

A. Vasudevan, A. Souers, G. Fox, 2006, European journal of pharmacology.

Histaminergic mechanisms in the CNS Selective H 3 receptor ( H 3 R ) blockade : broad efficacy in cognition and schizophrenia

K. Browman, J. Sullivan, M. E. Ballard, 2022 .

International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors

H. Haas, R. Thurmond, R. Leurs, 2015, Pharmacological Reviews.

Antinociceptive effects of histamine H3 receptor antagonist in the preclinical models of pain in rats and the involvement of central noradrenergic systems

Jill M. Wetter, J. Brioni, M. Decker, 2010, Brain Research.

Pharmacological characterization of A-960656, a histamine H₃ receptor antagonist with efficacy in animal models of osteoarthritis and neuropathic pain.

Jill M. Wetter, G. Diaz, J. Brioni, 2012, European journal of pharmacology.

Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists.

A. Gomtsyan, J. Segreti, R. Henry, 2016, Journal of medicinal chemistry.

Pharmacological Properties and Procognitive Effects of ABT-288, a Potent and Selective Histamine H3 Receptor Antagonist

Min Zhang, K. Browman, J. Sullivan, 2012, Journal of Pharmacology and Experimental Therapeutics.