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Your search keyword '"Al-Barazanji KA"' showing total 2 results
Start Over Author "Al-Barazanji KA" Journal bioorganic medicinal chemistry letters
2 results on '"Al-Barazanji KA"'

1. Novel benzimidazole-based MCH R1 antagonists.

Author

Carpenter AJ, Al-Barazanji KA, Barvian KK, Bishop MJ, Britt CS, Cooper JP, Goetz AS, Grizzle MK, Hertzog DL, Ignar DM, Morgan RO, Peckham GE, Speake JD, and Swain WR

Subjects
Animals, Benzimidazoles pharmacokinetics, Biological Availability, Body Composition, Dose-Response Relationship, Drug, Mice, Models, Animal, Structure-Activity Relationship, Weight Loss drug effects, Benzimidazoles pharmacology, Obesity drug therapy, Receptors, Somatostatin antagonists & inhibitors
Abstract

The identification of an MCH R1 antagonist screening hit led to the optimization of a class of benzimidazole-based MCH R1 antagonists. Structure-activity relationships and efforts to optimize pharmacokinetic properties are detailed along with the demonstration of the effectiveness of an MCH R1 antagonist in an animal model of obesity.

Published
2006
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2. The discovery and optimization of pyrimidinone-containing MCH R1 antagonists.

Author

Hertzog DL, Al-Barazanji KA, Bigham EC, Bishop MJ, Britt CS, Carlton DL, Cooper JP, Daniels AJ, Garrido DM, Goetz AS, Grizzle MK, Guo YC, Handlon AL, Ignar DM, Morgan RO, Peat AJ, Tavares FX, and Zhou H

Subjects
Animals, Body Weight drug effects, Mice, Mice, Inbred AKR, Models, Molecular, Molecular Structure, Pyrimidinones chemical synthesis, Receptors, Pituitary Hormone metabolism, Structure-Activity Relationship, Sulfhydryl Compounds chemistry, Pyrimidinones chemistry, Pyrimidinones pharmacology, Receptors, Pituitary Hormone antagonists & inhibitors
Abstract

Optimization of a series of constrained melanin-concentrating hormone receptor 1 (MCH R1) antagonists has provided compounds with potent and selective MCH R1 activity. Details of the optimization process are provided and the use of one of the compounds in an animal model of diet-induced obesity is presented.

Published
2006
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