On the importance of synthetic organic chemistry in drug discovery: reflections on the discovery of antidiabetic agent ertugliflozin

被引：32

作者：

Mascitti, Vincent ^{[1
]}

Thuma, Benjamin A. ^{[1
]}

Smith, Aaron C. ^{[1
]}

Robinson, Ralph P. ^{[1
]}

Brandt, Thomas ^{[1
]}

Kalgutkar, Amit S. ^{[1
]}

Maurer, Tristan S. ^{[1
]}

Samas, Brian ^{[1
]}

Sharma, Raman ^{[1
]}

机构：

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

来源：

MEDCHEMCOMM | 2013年 / 4卷 / 01期

关键词：

GLUCOSE COTRANSPORTER 2; SERGLIFLOZIN ETABONATE; DOSE PHARMACOKINETICS; CLINICAL CANDIDATE; SGLT2; INHIBITOR; REABSORPTION; POTENT; PHARMACODYNAMICS; MECHANISM;

D O I：

10.1039/c2md20163a

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The discovery of antidiabetic agent ertugliflozin is described. The compound belongs to a new class of SGLT2 inhibitors bearing a dioxa-bicyclo[3.2.1]octane motif. This article describes the critical role that organic synthesis played in both influencing our medicinal chemistry strategy and speeding up the progression of our program.

引用

页码：101 / 111

页数：11

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