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Your search keyword '"Falls HD"' showing total 3 results
Start Over Author "Falls HD" Topic amides
3 results on '"Falls HD"'

1. Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity.

Author

Judd AS, Souers AJ, Wodka D, Zhao G, Mulhern MM, Iyengar RR, Gao J, Lynch JK, Freeman JC, Falls HD, Brodjian S, Dayton BD, Reilly RM, Gintant G, Limberis JT, Mikhail A, Leitza ST, Houseman KA, Diaz G, Bush EN, Shapiro R, Knourek-Segel V, Hernandez LE, Marsh KC, Sham HL, Collins CA, and Kym PR

Subjects
Animals, Ether-A-Go-Go Potassium Channels drug effects, Humans, Inhibitory Concentration 50, Mice, Obesity drug therapy, Patch-Clamp Techniques, Pharmacokinetics, Amides pharmacology, Chromones pharmacology, Ether-A-Go-Go Potassium Channels metabolism, Receptors, Pituitary Hormone antagonists & inhibitors
Abstract

A series of potent 2-carboxychromone-based melanin-concentrating hormone receptor 1 (MCHr1) antagonists were synthesized and evaluated for hERG (human Ether-a-go-go Related Gene) channel affinity and functional blockade. Basic dialkylamine-terminated analogs were found to weakly bind the hERG channel and provided marked improvement in a functional patch-clamp assay versus previously reported antagonists of the series.

Published
2007
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2. Structure-activity relationship studies on tetralin carboxamide growth hormone secretagogue receptor antagonists.

Author

Zhao H, Xin Z, Patel JR, Nelson LT, Liu B, Szczepankiewicz BG, Schaefer VG, Falls HD, Kaszubska W, Collins CA, Sham HL, and Liu G

Subjects
Administration, Oral, Amides pharmacology, Animals, Binding Sites, Biological Availability, Drug Design, Inhibitory Concentration 50, Phenylenediamines chemistry, Rats, Receptors, G-Protein-Coupled metabolism, Receptors, Ghrelin, Structure-Activity Relationship, Amides chemical synthesis, Receptors, G-Protein-Coupled antagonists & inhibitors, Tetrahydronaphthalenes pharmacology
Abstract

The structure-activity relationship studies on a series of tetralin carboxamide growth hormone secretagogue receptor (GHS-R) antagonists are discussed. It was found that certain 2-alkoxycarbonylamino substituted tetralin carboxamides are potent, selective, and orally bioavailable GHS-R antagonists.

Published
2005
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3. Novel isoxazole carboxamides as growth hormone secretagogue receptor (GHS-R) antagonists.

Author

Liu B, Liu G, Xin Z, Serby MD, Zhao H, Schaefer VG, Falls HD, Kaszubska W, Collins CA, and Sham HL

Subjects
Amides chemistry, Amides pharmacology, Animals, CHO Cells, Cricetinae, Cricetulus, Humans, Isoxazoles chemistry, Isoxazoles pharmacology, Mice, Radioligand Assay, Rats, Receptors, Ghrelin, Solubility, Stereoisomerism, Structure-Activity Relationship, Water, Amides chemical synthesis, Isoxazoles chemical synthesis, Receptors, G-Protein-Coupled antagonists & inhibitors
Abstract

Novel isoxazole carboxamides have been identified as growth hormone secretagogue receptor (GHS-R) antagonists. Substituent modification off the 5-position of the isoxazole ring led to analogues with potent binding affinity and functional antagonism of GHS-R. A potent analogue (32) with high aqueous solubility and good GPCR selectivity was also identified as a potential pharmacological tool for in vivo studies.

Published
2004
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