The discovery of novel calcium sensing receptor negative allosteric modulators

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Abstract

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.

Graphical abstract

The discovery of a structurally novel, orally bioavailable series of calcium sensing receptor negative allosteric modulators is described.

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