Search Results - "Conder, Mary Lee"
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1
Estimation of hERG inhibition of drug candidates using multivariate property and pharmacophore SAR
Published in Bioorganic & medicinal chemistry (15-09-2007)“…We describe the development and validation of an in silico model of hERG inhibition. The model includes several factors not previously reported for the…”
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2
Pyrrolidine amides of pyrazolodihydropyrimidines as potent and selective Kv1.5 blockers
Published in Bioorganic & medicinal chemistry letters (15-02-2010)“…Design and synthesis of pyrazolodihydropyrimidines as KV1.5 blockers led to the discovery of 7d as a potent and selective antagonist. This compound showed…”
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3
Dihydropyrazolopyrimidine Inhibitors of Kv1.5 (IKur)
Published in Bioorganic & medicinal chemistry letters (15-12-2008)Get full text
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4
Functional Expression of Two KvLQT1-related Potassium Channels Responsible for an Inherited Idiopathic Epilepsy
Published in The Journal of biological chemistry (31-07-1998)“…Benign familial neonatal convulsions (BFNC), a class of idiopathic generalized epilepsy, is an autosomal dominantly inherited disorder of newborns. BFNC has…”
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5
KvLQT1, a Voltage-Gated Potassium Channel Responsible for Human Cardiac Arrhythmias
Published in Proceedings of the National Academy of Sciences - PNAS (15-04-1997)“…The clinical features of long QT syndrome result from episodic life-threatening cardiac arrhythmias, specifically the polymorphic ventricular tachycardia…”
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6
Design and Synthesis of 4-Substituted Benzamides as Potent, Selective, and Orally Bioavailable IKs Blockers
Published in Journal of medicinal chemistry (08-11-2001)Get full text
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7
Selective IKur Inhibitors for the Potential Treatment of Atrial Fibrillation: Optimization of the Phenyl Quinazoline Series Leading to Clinical Candidate 5-[5-Phenyl-4-(pyridin-2-ylmethylamino)quinazolin-2-yl]pyridine-3-sulfonamide
Published in Journal of medicinal chemistry (11-05-2017)“…We have recently disclosed 5-phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine 1 as a potent IKur current blocker with selectivity versus…”
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8
Pseudosaccharin amines as potent and selective KV1.5 blockers
Published in Bioorganic & medicinal chemistry letters (01-11-2015)“…Synthesis of pseudosaccharin amines as KV1.5 blockers led to the discovery of potent antagonists such as 17d. These compounds had potent pharmacodynamic…”
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9
Discovery of 5-Phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine as a Potent IKur Inhibitor
Published in ACS medicinal chemistry letters (08-09-2016)“…A new series of phenylquinazoline inhibitors of K v 1.5 is disclosed. The series was optimized for K v 1.5 potency, selectivity versus h ERG, pharmacokinetic…”
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10
Discovery of (( S )-5-(Methoxymethyl)-7-(1-methyl-1 H -indol-2-yl)-2-(trifluoromethyl)-4,7-dihydropyrazolo[1,5- a ]pyrimidin-6-yl)(( S )-2-(3-methylisoxazol-5-yl)pyrrolidin-1-yl)methanone As a Potent and Selective I Kur Inhibitor
Published in Journal of medicinal chemistry (12-04-2012)Get full text
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11
Pseudosaccharin amines as potent and selective K V 1.5 blockers
Published in Bioorganic & medicinal chemistry letters (01-11-2015)Get full text
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12
Dihydropyrazolopyrimidines containing benzimidazoles as Kv1.5 potassium channel antagonists
Published in Bioorganic & medicinal chemistry letters (15-09-2009)Get full text
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13
Discovery of 5‑Phenyl‑N‑(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine as a Potent I Kur Inhibitor
Published in ACS medicinal chemistry letters (08-09-2016)“…A new series of phenylquinazoline inhibitors of Kv 1.5 is disclosed. The series was optimized for Kv 1.5 potency, selectivity versus hERG, pharmacokinetic…”
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14
Triazolo and imidazo dihydropyrazolopyrimidine potassium channel antagonists
Published in Bioorganic & medicinal chemistry letters (15-03-2013)“…Previously disclosed C6 amido and benzimidazole dihydropyrazolopyrimidines were potent and selective blockers of IKur current. Syntheses and SAR for C6…”
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15
Dihydropyrazolopyrimidine inhibitors of K(V)1.5 (I(Kur))
Published in Bioorganic & medicinal chemistry letters (15-12-2008)“…A series of dihydropyrazolopyrimidine inhibitors of K(V)1.5 (I(Kur)) have been identified. The synthesis, structure-activity relationships and selectivity…”
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16
Correction to Discovery of (( S )-5-(Methoxymethyl)-7-(1-methyl-1 H -indol-2-yl)-2-(trifluoromethyl)-4,7-dihydropyrazolo[1,5- a ]pyrimidin-6-yl)(( S )-2-(3-methylisoxazol-5-yl)pyrrolidin-1-yl)methanone As a Potent and Selective I Kur Inhibitor
Published in Journal of medicinal chemistry (12-09-2013)Get full text
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17
Pyrano-[2,3 b]-pyridines as potassium channel antagonists
Published in Bioorganic & medicinal chemistry (15-04-2008)“…The design and synthesis of a series of highly functionalized pyrano-[2,3 b]-pyridines is described. These compounds were assayed for their ability to block…”
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18
Benzopyran sulfonamides as Kv1.5 potassium channel blockers
Published in Bioorganic & medicinal chemistry letters (15-06-2007)“…K(V)1.5 blockers have the potential to be atrium-selective agents for treatment of atrial fibrillation. The benzopyrans provide a template for the synthesis of…”
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19
Pyrrolidine amides of pyrazolodihydropyrimidines as potent and selective K V1.5 blockers
Published in Bioorganic & medicinal chemistry letters (2010)“…Design and synthesis of pyrazolodihydropyrimidines as K V1.5 blockers led to the discovery of 7d as a potent and selective antagonist. This compound showed…”
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20
Dihydropyrazolopyrimidine Inhibitors of K sub(V)1.5 (I sub(Kur))
Published in Bioorganic & medicinal chemistry (01-12-2008)“…A series of dihydropyrazolopyrimidine inhibitors of K sub(V)1.5 (I sub(Kur)) have been identified. The synthesis, structure-activity relationships and…”
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