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Your search keyword '"Jae HS"' showing total 3 results
Start Over Author "Jae HS" Journal bioorganic medicinal chemistry letters
3 results on '"Jae HS"'

1. Discovery of potent and selective inhibitors of 11beta-HSD1 for the treatment of metabolic syndrome.

Author

Richards S, Sorensen B, Jae HS, Winn M, Chen Y, Wang J, Fung S, Monzon K, Frevert EU, Jacobson P, Sham H, and Link JT

Subjects
Carbenoxolone chemistry, Carbenoxolone pharmacology, Enzyme Inhibitors therapeutic use, Humans, Molecular Conformation, Piperazines chemistry, Piperazines pharmacology, Sulfonamides chemistry, Sulfonamides pharmacology, Thiazoles chemistry, Thiazoles pharmacology, 11-beta-Hydroxysteroid Dehydrogenase Type 1 antagonists & inhibitors, Enzyme Inhibitors chemical synthesis, Enzyme Inhibitors pharmacology, Metabolic Syndrome drug therapy
Abstract

High throughput screening efforts have identified a novel class of dichloroaniline amide 11beta-HSD1 inhibitors. SAR studies initiated from dichloroaniline 4 focused on retaining the potency and selectivity profile of the lead.

Published
2006
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2. Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors.

Author

Kurukulasuriya R, Rohde JJ, Szczepankiewicz BG, Basha F, Lai C, Jae HS, Winn M, Stewart KD, Longenecker KL, Lubben TW, Ballaron SJ, Sham HL, and von Geldern TW

Subjects
Animals, Dipeptidyl Peptidase 4 chemistry, Imidazoles pharmacology, Kinetics, Models, Molecular, Protease Inhibitors chemical synthesis, Protein Conformation, Rats, Structure-Activity Relationship, X-Ray Diffraction, Xanthines chemical synthesis, Dipeptidyl-Peptidase IV Inhibitors, Protease Inhibitors pharmacology, Xanthines pharmacology
Abstract

A series of xanthine mimetics containing 5,5 and 5,6 heterocycle fused imidazoles were synthesized as dipeptidyl peptidase IV inhibitors. Compound 7 is potent (h-DPPIV K(i)=2nM) and exhibits excellent selectivity and no species specificity against rat and human enzymes. The X-ray structure confirms that the binding mode of 7 to rat DPPIV is similar to the parent xanthines.

Published
2006
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3. Biaryl amide glucagon receptor antagonists.

Author

Kurukulasuriya R, Sorensen BK, Link JT, Patel JR, Jae HS, Winn MX, Rohde JR, Grihalde ND, Lin CW, Ogiela CA, Adler AL, and Collins CA

Subjects
Amides chemistry, Animals, Haplorhini, Humans, Mice, Rats, Rats, Sprague-Dawley, Amides pharmacology, Receptors, Glucagon antagonists & inhibitors
Abstract

Biaryl amides derived from a reported series of ureas 1 were evaluated and found to be potent human glucagon receptor antagonists. The benzofuran analogue 6i was administered in Sprague-Dawley rats and blocked the effects of an exogenous glucagon challenge.

Published
2004
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