Thiazole-derived potent, highly bioavailable short duration growth hormone secretagogues

Replacement of the phenyl in 3 with a 2-pyridyl or 4-thiazolyl group resulted in increased potency in the rat pituitary cell GH release assay and in beagles. Replacement of the phenyl in 3 with a 2-pyridyl or 4-thiazolyl group resulted in increased potency in the rat pituitary cell GH release assay...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1999-07, Vol.9 (13), p.1761-1766
Main Authors: Lihu Yang, Morriello, Greg, Kwan Leung, Jacks, Tom, Kang Cheng, Schleim, Klaus D., Smith, Roy, Patchett, Arthur A.
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Biological Availability
Dogs
Growth Hormone - chemical synthesis
Growth Hormone - metabolism
Hormones. Endocrine system
Medical sciences
Models, Chemical
Pharmacology. Drug treatments
Rats
Rats, Sprague-Dawley
Structure-Activity Relationship
Thiazoles - administration & dosage
Thiazoles - chemical synthesis
Thiazoles - pharmacokinetics
Time Factors
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Summary:Replacement of the phenyl in 3 with a 2-pyridyl or 4-thiazolyl group resulted in increased potency in the rat pituitary cell GH release assay and in beagles. Replacement of the phenyl in 3 with a 2-pyridyl or 4-thiazolyl group resulted in increased potency in the rat pituitary cell GH release assay and in beagles. 8-4S has a bioavailability of 44% in beagles.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(99)00286-3