Search Results - "Annedi, Subhash C."
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Cell-Permeable Inhibitors of Neuronal Nitric Oxide Synthase Open New Prospects for the Treatment of Neurological Disorders
Published in Journal of medicinal chemistry (12-02-2015)“…The disubstituted pyrimidines based SAR study by Silverman et al. ( J. Med. Chem. 2014, DOI: 10.1021/jm501719e) was focused on improving bioavailability and…”
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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
Published in Journal of medicinal chemistry (26-01-2012)“…A series of 1,6-disubstituted indoline derivatives were synthesized and evaluated as inhibitors of human nitric oxide synthase (NOS) designed to mitigate the…”
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1,5-Disubstituted indole derivatives as selective human neuronal nitric oxide synthase inhibitors
Published in Bioorganic & medicinal chemistry letters (15-09-2011)“…A series of 1,5-disubstituted indole derivatives was designed, synthesized and evaluated as inhibitors of human nitric oxide synthase. A variety of flexible…”
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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
Published in Journal of medicinal chemistry (12-04-2012)“…A family of different 3,5-disubstituted indole derivatives having 6-membered rings were designed, synthesized, and demonstrated inhibition of human nitric…”
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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
Published in Journal of medicinal chemistry (11-08-2011)“…Neuronal nitric oxide synthase (nNOS) inhibitors are effective in preclinical models of many neurological disorders. In this study, two related series of…”
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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
Published in Journal of medicinal chemistry (27-10-2011)“…3,6-Disubstituted indole derivatives were designed, synthesized, and evaluated as inhibitors of human nitric oxide synthase (NOS). Bulky amine containing…”
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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
Published in European journal of medicinal chemistry (01-09-2012)“…We recently reported a series of 1,6-disubstituted indoline-based thiophene amidine compounds (5) as selective neuronal nitric oxide synthase (nNOS) inhibitors…”
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1,6-Disubstituted indole derivatives as selective human neuronal nitric oxide synthase inhibitors
Published in Bioorganic & medicinal chemistry letters (15-09-2011)“…A series of 1,6-disubstituted indole derivatives was designed, synthesized and evaluated as inhibitors of human nitric oxide synthase (NOS). By varying the…”
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Novel, druglike 1,7-disubstituted 2,3,4,5-tetrahydro-1H-benzo[b]azepine-based selective inhibitors of human neuronal nitric oxide synthase (nNOS)
Published in Bioorganic & medicinal chemistry letters (01-04-2012)“…R=various cyclic and acyclic basic amine side chains. Selective inhibitors of human neuronal nitric oxide synthase (nNOS). A novel class of 1,7-disubstituted…”
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3,5-Disubstituted indole derivatives as selective human neuronal nitric oxide synthase (nNOS) inhibitors
Published in Bioorganic & medicinal chemistry letters (01-03-2012)“…A series of 3,5-disubstituted indole derivatives was designed, synthesized and evaluated as inhibitors of human nitric oxide synthase (NOS). Various guanidine…”
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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
Published in Journal of medicinal chemistry (22-03-2012)“…Numerous studies have shown that selective nNOS inhibitors could be therapeutic in many neurological disorders. Previously, we reported a series of…”
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Novel 2-aminobenzothiazoles as selective neuronal nitric oxide synthase inhibitors
Published in Bioorganic & medicinal chemistry letters (01-05-2007)“…A novel series of 2-aminobenzothiazoles were synthesized and shown to be selective inhibitors of neuronal nitric oxide synthase (nNOS). A series of substituted…”
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An Unprecedented Twist to ODCase Catalytic Activity
Published in Journal of the American Chemical Society (02-11-2005)“…Orotidine-5‘-monophosphate decarboxylase (ODCase) has evolved to catalyze a decarboxylation reaction, most probably via a carbanion species at the C6 position…”
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Design and Synthesis of Novel Fluoropeptidomimetics as Potential Mimics of the Transition State during Peptide Hydrolysis
Published in Journal of organic chemistry (07-02-2003)“…α-Fluoroamino acids were targeted in our ongoing efforts to design novel fluoropeptidomimetics (1) as potential protease inhibitors. α-Fluoroglycine derivative…”
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Engineering D-amino acid containing novel protease inhibitors using catalytic site architecture
Published in Bioorganic & medicinal chemistry (2006)“…The mechanism of proteolysis by serine proteases is a reasonably well-understood process. Typically, a histidine residue acting as a general base deprotonates…”
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Novel fluoropeptidomimetics: synthesis, stability studies and protease inhibition
Published in Bioorganic & medicinal chemistry (15-04-2005)“…[Display omitted] Designer fluoropeptidomimetics as protease inhibitors are revealed. The key peptidomimetic region in the inhibitors contains a ‘–CHF–S–’…”
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Design and Synthesis of Novel Fluoropeptidomimetics as Potential Mimics of the Transition State during Peptide Hydrolysis
Published in Journal of organic chemistry (29-10-2004)Get full text
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Chapter 2 Advancements in the Development of Nitric Oxide Synthase Inhibitors
Published in Annual Reports in Medicinal Chemistry (2009)“…This chapter focuses on recent advances in the design of the selective inhibitors of nitric oxide synthase (NOS) and some of the emerging preclinical and…”
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