期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 51, 期 3, 页码 689-693出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm701292s
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Ghrelin receptor ligands based on trisubstituted 1,2,4-triazole structure were synthesized and evaluated for their in vitro binding and biological activity. In this study, we explored the replacement of the alpha-aminoisobutyryl moiety by aromatic or heteroaromatic groups. Compounds 5 and 34 acted as potent in vivo antagonists of hexarelin-stimulated food intake. These two compounds did not stimulate growth hormone secretion in rodents and did not antagonize growth hormone secretion induced by hexarelin.
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