Search Results - "Malley, Mary F."
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Novel Synthesis of the Hexahydroimidazo[1,5b]isoquinoline Scaffold: Application to the Synthesis of Glucocorticoid Receptor Modulators
Published in Journal of medicinal chemistry (11-02-2010)“…The first stereoselective synthesis of the hexahydroimidazo[1,5b]isoquinoline (HHII) scaffold as a surrogate for the steroidal A-B ring system is described…”
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Discovery of Potent, Orally-Active, and Muscle-Selective Androgen Receptor Modulators Based on an N-Aryl-hydroxybicyclohydantoin Scaffold
Published in Journal of medicinal chemistry (28-12-2006)“…A novel, N-aryl-bicyclohydantoin selective androgen receptor modulator scaffold was discovered through structure-guided modifications of androgen receptor…”
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Synthesis, characterization, and crystal structures of M(DO3A) (M = iron, gadolinium) and Na[M(DOTA)] (M = Fe, yttrium, Gd)
Published in Inorganic chemistry (01-08-1993)“…Macrocyclic amino carboxylate (DOTA and DO3A, where DOTA is 1,4,7,10-tetrakis(carboxymethyl)-1,4,7,10-tetraazacyclododecane and DO3A is…”
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Discovery of BMS-753426: A Potent Orally Bioavailable Antagonist of CC Chemokine Receptor 2
Published in ACS medicinal chemistry letters (10-06-2021)“…To improve the metabolic stability profile of BMS-741672 (1a), we undertook a structure–activity relationship study in our trisubstituted cyclohexylamine…”
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Use of a Conformational-Switching Mechanism to Modulate Exposed Polarity: Discovery of CCR2 Antagonist BMS-741672
Published in ACS medicinal chemistry letters (14-03-2019)“…We encountered a dilemma in the course of studying a series of antagonists of the G-protein coupled receptor CC chemokine receptor-2 (CCR2): compounds with…”
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Discovery of potent and selective nonsteroidal indazolyl amide glucocorticoid receptor agonists
Published in Bioorganic & medicinal chemistry letters (01-10-2013)“…Modification of a phenolic lead structure based on lessons learned from increasing the potency of steroidal glucocorticoid agonists lead to the discovery of…”
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Dihydropyrimidine calcium channel blockers: 2-heterosubstituted 4-aryl-1,4-dihydro-6-methyl-5-pyrimidinecarboxylic acid esters as potent mimics of dihydropyridines
Published in Journal of medicinal chemistry (01-05-1990)“…2-Heterosubstituted-4-aryl-1,4-dihydro-6-methyl-5-pyrimidinecar box ylic acid esters 8, which lack the potential CS symmetry of dihydropyridine calcium channel…”
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Utilization of a nitrogen–sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38α MAP kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (01-10-2010)“…An intramolecular nitrogen–sulfur nonbonding interaction has been used in the design of a novel series of 2-aminothiazol-5-yl-pyrimidines as p38α MAP kinase…”
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Characterization of NADP + binding to perdeuterated MurB: backbone atom NMR assignments and chemical-shift changes
Published in Journal of molecular biology (18-04-1997)“…Backbone-atom resonances have been assigned for both the substrate-free and the NADP +-complexed forms of UDP- N-acetylenolpyruvylglucosamine reductase (MurB),…”
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Studies towards understanding the mechanism of the unusual rearrangement of certain 5-propargyloxyindoles
Published in Tetrahedron letters (06-05-2000)“…A mechanism of the rearrangement of 5-propargyloxyindoles is proposed and supported by the formation of a novel tetracyclic indole derivative 12 as the major…”
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Synthesis of Novel Potent Dipeptidyl Peptidase IV Inhibitors with Enhanced Chemical Stability: Interplay between the N-Terminal Amino Acid Alkyl Side Chain and the Cyclopropyl Group of α-Aminoacyl-l-cis-4,5-methanoprolinenitrile-Based Inhibitors
Published in Journal of medicinal chemistry (06-05-2004)“…A series of methanoprolinenitrile-containing dipeptide mimetics were synthesized and assayed as inhibitors of the N-terminal sequence-specific serine protease…”
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Discovery of (R)-9-Ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol- 6(2H)-one, a Selective, Orally Active Agonist of the 5-HT2C Receptor
Published in Journal of medicinal chemistry (22-03-2007)“…Robust pharmaceutical treatment of obesity has been limited by the undesirable side-effect profile of currently marketed therapies. This paper describes the…”
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Cannabinoid CB1 receptor ligand binding and function examined through mutagenesis studies of F200 and S383
Published in European journal of pharmacology (25-01-2011)“…The cannabinoid CB1 G protein-coupled receptor has been shown to be a regulator of food consumption and has been studied extensively as a drug target for the…”
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Urea based CCR3 antagonists employing a tetrahydro-1,3-oxazin-2-one spacer
Published in Bioorganic & medicinal chemistry letters (2009)“…Conformational restriction of open chain analogs with a more polar tetrahydro-1,3-oxazin-2-one spacer led to the identification of potent urea-based CCR3…”
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Synthesis and antiviral activity of enantiomeric forms of cyclobutyl nucleoside analogs
Published in Journal of medicinal chemistry (01-04-1991)“…The syntheses of the enantiomeric cyclobutyl guanine nucleoside analogues [1R-1 alpha, 2 beta, 3 alpha]- and [1S-1 alpha, 2 beta, 3 alpha]-2-…”
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Novel 1,4-Homofragmentation via an α-Lactone
Published in Journal of organic chemistry (27-10-2006)“…Conversion of an α,α-dichloroester to the corresponding α-keto acid was unexpectedly complicated by a novel 1,4-homofragmentation. Investigation of the…”
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Synthesis of substituted 1,2,3,4-tetrahydro-6-methyl-2-thioxo-5-pyrimidinecarboxylic acid esters
Published in Heterocycles (01-05-1987)Get full text
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Practical synthesis of an enantiomerically pure synthon for the preparation of mevinic acid analogs
Published in Journal of organic chemistry (01-05-1991)Get full text
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Neutral, seven-coordinate dioxime complexes of technetium(III): synthesis and characterization
Published in Inorganic chemistry (01-06-1990)“…The tin-capped complexes {sup 99}Tc(oxime){sub 3}({mu}-OH)SnCl{sub 3} (oxime = dimethylglyoxime (DMG) or cyclohexanedione dioxime (CDO)) can be prepared by the…”
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