Design and synthesis of 4-substituted benzamides as potent, selective, and orally bioavailable IKs blockers

Journal of Medicinal Chemistry

Volumn 44, Issue 23, 2001, Pages 3764-3767

  Lloyd, J ^a   Schmidt, J B ^a   Rovnyak, G ^a   Ahmad, S ^a   Atwal, K S ^a   Bisaha, S N ^a   Doweyko, L M ^a   Stein, P D ^a   Traeger, S C ^a   Mathur, A ^a   Conder, M L ^a   DiMarco, J ^a   Harper, T W ^a   Jenkins West, T ^a   Levesque, P C ^a   Normandin, D E ^a   Russell, A D ^a   Serafino, R P ^a   Smith, M A ^a   Lodge, N J ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 HEXYLOXYBENZAMIDE; ANTIARRHYTHMIC AGENT; BENZAMIDE DERIVATIVE; BENZODIAZEPINE DERIVATIVE; BENZOIC ACID DERIVATIVE; HETEROCYCLIC COMPOUND; ION CHANNEL; POTASSIUM CHANNEL; POTASSIUM CHANNEL BLOCKING AGENT; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANTIARRHYTHMIC ACTIVITY; ARTICLE; DRUG BIOAVAILABILITY; DRUG POTENCY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; GUINEA PIG; HEART MUSCLE CELL; NONHUMAN; OOCYTE; RAT; XENOPUS;

ADMINISTRATION, ORAL; ANIMALS; BENZAMIDES; BIOLOGICAL AVAILABILITY; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; KCNQ POTASSIUM CHANNELS; KCNQ1 POTASSIUM CHANNEL; OOCYTES; OXADIAZOLES; PATCH-CLAMP TECHNIQUES; POTASSIUM CHANNEL BLOCKERS; POTASSIUM CHANNELS; POTASSIUM CHANNELS, VOLTAGE-GATED; RATS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; XENOPUS;

EID: 0035829427     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm015505u     Document Type: Article

References (19)

1. Channel specificity in antiarrhythmic drug action
2. Two components of cardiac delayed rectifier potassium Current. Differential sensitivity to block by class III antiarrhythmic agents
3. Kr potassium current
4. Ks potassium channel
5. A molecular basis for cardiac arrhythmia: HERG mutations cause long QT syndrome
6. Rate dependent prolongation of cardiac action potentials by a methanesulfonanilide class III antiarrhythmic agent
7. Ks by (R)-2-(2,4-trifuoromethyl)-N-[2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)-2, 3-dihydre-1H-benzo[e] [1,4]diazepin-3-yl]-acetamide
8. Cloning of a membrane protein that induces a slow voltage-gated potassium current
9. Ks cardiac potassium current
10. Azines and imines of 4-tert-butyl-lH-pyrrole-2-carboxaldehyde and 5-tert-butyl-lH-pyrrole-2-carboxaldehyde. A useful synthesis of the aldehydes
11. A general one-step synthesis of nitriles from ketones using tosylmethyl isocyanide. Introduction of a one-carbon unit
12. Synthesis and evaluation of 3-substituted analogues of 1,2,3,4-tetrahydroisoquinoline as inhibitors of phenylethanolamine N-methyltransferase
13. D-homo-steroids. Part 6. 1-acetyl-2,2-dimethylcyclopentanol: A monocyclic model for D-homoannulation of 17-hydroxypregnan-20-ones
14. Oxadiazoles as ester bioisosteric replacements in compounds related to disoxaril. Antirhinovirus activity
15. An improved oxadiazole synthesis using peptide coupling agents
16. KvLQT1, a voltage gated potassium channel responsible for human cardiac arrhythmias
17. The novel cardioprotective agent BMS-180448 activates a potassium conductance in cardiac and vascular smooth muscle
18. K1 density in the BIO TO-2 strain of syrian myopathic hamsters