Design and synthesis of tetrazole-based growth hormone secretagogue: the SAR studies of the O-benzyl serine side chain

Autor:	Neil Flynn, Hongjian Zhang, Leah Giupponi, Joseph A. Tino, Dorothy Slusarchyk, Steve Swartz, Haixia Wang, James J. Li, Ramakrishna Seethala, Shiwei Tao, Christa M. Musial, Brian J. Murphy, William G. Humphreys, Gary J. Grover, Andres A. Hernandez, Kenneth E.J. Dickinson, Mujing Yan, David A. Gordon, Jeffrey A. Robl, Blake C. Beehler, Stephanie Y. Chen, Paul G. Sleph, William R. Ewing, Jun Li
Rok vydání:	2008
Předmět:	inorganic chemicals Stereochemistry Clinical Biochemistry Pharmaceutical Science Tetrazoles Alcohol Biochemistry Chemical synthesis Serine chemistry.chemical_compound Structure-Activity Relationship Growth hormone secretagogue Drug Discovery Side chain Moiety Animals heterocyclic compounds Tetrazole Molecular Biology Molecular Structure organic chemicals Organic Chemistry Rats Biphenyl compound chemistry Drug Design Growth Hormone Molecular Medicine Carbamates
Zdroj:	Bioorganicmedicinal chemistry letters. 18(6)
ISSN:	1464-3405
Popis:	The structure-activity relationship of the O-benzyl serine side chain was investigated based on the tetrazole-based growth hormone secretagogue BMS-317180 (2). The ortho position of the benzyl moiety was found to be favorable for introduction of substituents. A series of ortho-substituted compounds were synthesized with improved in-vitro and in-vivo activity. Among them, the biphenyl compound 2p shows twofold improvement in potency compared to its parent compound BMS-317180 (2).
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3ee1df719a0b79baba03f4bd73dce301 https://pubmed.ncbi.nlm.nih.gov/18295486 Zobrazit plný text záznamu Full Text from ScienceDirect