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Discovery of potent, orally active benzimidazole glucagon receptor antagonists |
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| Authors: | Kim Ronald M Chang Jiang Lins Ashley R Brady Ed Candelore Mari R Dallas-Yang Qing Ding Victor Dragovic Jasminka Iliff Susan Jiang Guoqiang Mock Steven Qureshi Sajjad Saperstein Richard Szalkowski Deborah Tamvakopoulos Constantin Tota Laurie Wright Michael Yang Xiaodong Tata James R Chapman Kevin Zhang Bei B Parmee Emma R |
| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. ron_kim@merck.com |
| Abstract: | The discovery and optimization of potent and selective aminobenzimidazole glucagon receptor antagonists are described. One compound possessing moderate pharmacokinetic properties in multiple preclinical species was orally efficacious at inhibiting glucagon-mediated glucose excursion in transgenic mice expressing the human glucagon receptor, and in rhesus monkeys. The compound also significantly lowered glucose levels in a murine model of diabetes. |
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