The discovery of novel calcium sensing receptor negative allosteric modulators

被引：36

作者：

Balan, Gayatri ^{[1
]}

Bauman, Jonathan ^{[1
]}

Bhattacharya, Samit ^{[1
]}

Castrodad, Mayda ^{[1
]}

Healy, David R. ^{[1
]}

Herr, Michael ^{[1
]}

Humphries, Paul ^{[1
]}

Jennings, Sandra ^{[1
]}

Kalgutkar, Amit S. ^{[1
]}

Kapinos, Brendon ^{[1
]}

Khot, Vishal ^{[1
]}

Lazarra, Kimberly ^{[1
]}

Li, Mei ^{[1
]}

Li, Yan ^{[1
]}

Neagu, Constantin ^{[1
]}

Oliver, Robert ^{[1
]}

Piotrowski, David W. ^{[1
]}

Price, David ^{[1
]}

Qi, Hong ^{[1
]}

Simmons, Holly A. ^{[1
]}

Southers, James ^{[1
]}

Wei, Liuqing ^{[1
]}

Zhang, Yan ^{[1
]}

Paralkar, Vishwas M. ^{[1
]}

机构：

[1] Pfizer Inc, Groton New London Labs, Pfizer Global Res & Dev, Groton, CT 06340 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 12期

关键词：

Calcium sensing receptor; Negative allosteric modulators; Osteoporosis; Parathyroid hormone; PARATHYROID-HORMONE; EPIBATIDINE; SECRETION; SKELETON; RATS;

D O I：

10.1016/j.bmcl.2009.04.044

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The design and profile of a series of zwitterionic calcium sensing receptor negative allosteric modulators is described. Evaluation of key analogues using a rat model demonstrate a robust response, significantly improved potency over ronacaleret and have the potential as an oral, anabolic treatment for osteoporosis. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：3328 / 3332

页数：5

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