34881-44-2Relevant academic research and scientific papers
Eleven amino acid glucagon-like peptide-1 receptor agonists with antidiabetic activity
Mapelli, Claudio,Natarajan, Sesha I.,Meyer, Jean-Philippe,Bastos, Margarita M.,Bernatowicz, Michael S.,Lee, Ving G.,Pluscec, Jelka,Riexinger, Douglas J.,Sieber-McMaster, Ellen S.,Constantine, Keith L.,Smith-Monroy, Constance A.,Golla, Rajasree,Ma, Zhengping,Longhi, Daniel A.,Shi, Dan,Xin, Li,Taylor, Joseph R.,Koplowitz, Barry,Chi, Cecilia L.,Khanna, Ashish,Robinson, Gordon W.,Seethala, Ramakrishna,Antal-Zimanyi, Ildiko A.,Stoffel, Robert H.,Han, Songping,Whaley, Jean M.,Huang, Christine S.,Krupinski, John,Ewing, William R.
experimental part, p. 7788 - 7799 (2010/06/16)
Glucagon-like peptide 1 (GLP-1) is a 30 or 31 amino acid peptide hormone that contributes to the physiological regulation of glucose homeostasis and food intake. Herein, we report the discovery of a novel class of 11 amino acidGLP-1 receptor agonists. These peptides consist of a structurally optimized 9- mer, which is closely related to the N-terminal 9 amino acids ofGLP-1, linked to a substituted C-terminal biphenylalanine (BIP) dipeptide. SAR studies resulted in 11-mer GLP-1R agonists with similar in vitro potency to the native 30-mer. Peptides 21 and 22 acutely reduced plasma glucose excursions and increased plasma insulin concentrations in a mouse model of diabetes. These peptides also showed sustained exposures over several hours in mouse and dog models. The described 11-mer GLP-1 receptor agonists represent a new tool in further understanding GLP-1 receptor pharmacology that may lead to novel antidiabetic agents.
Process for the preparation of amino acids useful in the preparation of peptide receptor modulators
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Page/Page column 1; 3; 5, (2010/02/15)
The present invention provides process useful for the preparation of intermediates which are useful in the preparation of amino acids useful in preparing peptide receptor modulators, for example agonists or partial agonists of such peptide receptors. Such
A Mild Selective Monobromination Reagent System for Alkoxybenzenes; N-Bromosuccinimide-Silica Gel
Konishi, Hisatoshi,Aritomi, Katsutomo,Okano, Tamon,Kiji, Jitsuo
, p. 591 - 593 (2007/10/02)
The monobromination of alkoxybenzenes with N-bromosuccinimide catalyzed by silica gel in carbon tetrachloride occurred preferentially at the para-position. m-t-Butylmethoxybenzene yielded 4-bromo-3-t-butyl-1-methoxybenzene with a selectivity of 74percent even in the presence of a bulky substituent at the meta-position.
