Search Results - "de Jesus, Reynalda"
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Selective small-molecule inhibition of an RNA structural element
Published in Nature (London) (29-10-2015)“…Riboswitches are non-coding RNA structures located in messenger RNAs that bind endogenous ligands, such as a specific metabolite or ion, to regulate gene…”
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2
Discovery of Selective Small Molecule ROMK Inhibitors as Potential New Mechanism Diuretics
Published in ACS medicinal chemistry letters (10-05-2012)“…The renal outer medullary potassium channel (ROMK or Kir1.1) is a putative drug target for a novel class of diuretics that could be used for the treatment of…”
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3
Pharmacologic inhibition of the renal outer medullary potassium channel causes diuresis and natriuresis in the absence of kaliuresis
Published in The Journal of pharmacology and experimental therapeutics (01-01-2014)“…The renal outer medullary potassium (ROMK) channel, which is located at the apical membrane of epithelial cells lining the thick ascending loop of Henle and…”
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4
Discovery of a potent and selective ROMK inhibitor with improved pharmacokinetic properties based on an octahydropyrazino[2,1-c][1,4]oxazine scaffold
Published in Bioorganic & medicinal chemistry letters (01-12-2016)“…[Display omitted] Following the discovery of small molecule acyl piperazine ROMK inhibitors, the acyl octahydropyrazino[2,1-c][1,4]oxazine series was…”
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5
Differentiation of ROMK potency from hERG potency in the phenacetyl piperazine series through heterocycle incorporation
Published in Bioorganic & medicinal chemistry letters (01-05-2016)“…[Display omitted] Following the discovery of small molecule acyl piperazine ROMK inhibitors and their initial preclinical validation as a novel diuretic agent,…”
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6
Design and synthesis of a new class of malonyl-CoA decarboxylase inhibitors with anti-obesity and anti-diabetic activities
Published in Bioorganic & medicinal chemistry letters (15-10-2010)“…A new series of thiazole-substituted 1,1,1,3,3,3-hexafluoro-2-propanols were prepared and evaluated as malonyl-CoA decarboxylase (MCD) inhibitors. Key analogs…”
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7
4-(Phosphonoalkyl)- and 4-(phosphonoalkenyl)-2-piperidinecarboxylic acids: synthesis, activity at N-methyl-D-aspartic acid receptors and anticonvulsant activity
Published in Journal of medicinal chemistry (01-09-1989)“…A series of 4-(phosphonoalkyl)- and 4-(phosphonoalkenyl)-2-piperidinecarboxylic acids were synthesized, and their biological activity was assessed as…”
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Rapid Evolution of a Fragment-like Molecule to Pan-Metallo-Beta-Lactamase Inhibitors: Initial Leads toward Clinical Candidates
Published in Journal of medicinal chemistry (22-12-2022)“…With the emergence and rapid spreading of NDM-1 and existence of clinically relevant VIM-1 and IMP-1, discovery of pan inhibitors targeting…”
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9
Stimulation of Glucose-Dependent Insulin Secretion by a Potent, Selective sst 3 Antagonist
Published in ACS medicinal chemistry letters (12-04-2012)Get full text
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10
Stimulation of Glucose-Dependent Insulin Secretion by a Potent, Selective sst3 Antagonist
Published in ACS medicinal chemistry letters (12-04-2012)“…This letter provides the first pharmacological proof of principle that the sst3 receptor mediates glucose-stimulated insulin secretion (GSIS) from pancreatic…”
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Ortho-Substituted Benzofused Macrocyclic Lactams as Zinc Metalloprotease Inhibitors
Published in Journal of medicinal chemistry (14-02-1997)“…The design and preparation of ortho-substituted benzofused macrocyclic lactams are described. The benzofused macrocyclic lactams were designed as neutral…”
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12
2-(Arylalkylamino)adenosin-5'-uronamides: a new class of highly selective adenosine A2 receptor ligands
Published in Journal of medicinal chemistry (01-07-1990)“…The synthesis and receptor-binding profiles at adenosine receptor subtypes for a series of 2-(arylalkylamino)-adenosin-5'-uronamides is described. Halogenated…”
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13
2H-[1]Benzopyrano[3,4-b]pyridines. Synthesis and activity at central monoamine receptors
Published in Journal of medicinal chemistry (01-03-1989)“…Two general synthetic approaches to a novel series of 2H-[1]benzopyrano[3,4-b]pyridines are described together with their receptor binding profile at a variety…”
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14
Meta-Substituted Benzofused Macrocyclic Lactams as Zinc Metalloprotease Inhibitors
Published in Journal of medicinal chemistry (14-02-1997)“…The design, synthesis, and biochemical profile of meta-substituted benzofused macrocyclic lactams are described. The meta-substituted benzofused macrocyclic…”
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15
Benzofuro[2,3-c]pyridin-6-ols: synthesis, affinity for opioid-receptor subtypes, and antinociceptive activity
Published in Journal of medicinal chemistry (01-09-1989)“…A general synthetic approach to a novel series of cis-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols is described together with their receptor-binding…”
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16
A study of superoxide reactivity. Reaction of potassium superoxide with alkyl halides and tosylates
Published in Journal of the American Chemical Society (01-11-1978)Get full text
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