Martin Crook
Merck & Co.
5 Papers
57 Citations
Martin Crook is an academic researcher from Merck & Co.. The author has contributed to research in topics: Mineralocorticoid receptor & Oxazolidinedione. The author has an hindex of 5, co-authored 5 publications.
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Papers
Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series.
Jason M. Cox,Hong D. Chu,Christine Yang,Hong C. Shen,Zhicai Wu,Jaume Balsells,Alejandro Crespo,Patricia Brown,Beata Zamlynny,Judyann Wiltsie,Joseph Clemas,Jack Gibson,Lisa Contino,JeanMarie Lisnock,Gaochao Zhou,Margarita Garcia-Calvo,Thomas Bateman,Ling Xu,Xinchun Tong,Martin Crook,Peter J. Sinclair +20 more
TL;DR: Structural-activity relationship efforts focused on improving lipophilic ligand efficiency (LLE) while maintaining nuclear hormone receptor selectivity and reasonable pharmacokinetic profiles.
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Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.
Christine Yang,Hong C. Shen,Zhicai Wu,Hong D. Chu,Jason M. Cox,Jaume Balsells,Alejandro Crespo,Patricia Brown,Beata Zamlynny,Judyann Wiltsie,Joseph Clemas,Jack Gibson,Lisa Contino,JeanMarie Lisnock,Gaochao Zhou,Margarita Garcia-Calvo,Thomas Bateman,Ling Xu,Xinchun Tong,Martin Crook,Peter J. Sinclair +20 more
TL;DR: Novel oxazolidinedione analogs were discovered as potent and selective mineralocorticoid receptor (MR) antagonists and structure-activity relationship (SAR) studies were focused on improving the potency and microsomal stability.
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Discovery of Benzimidazole Oxazolidinediones as Novel and Selective Nonsteroidal Mineralocorticoid Receptor Antagonists
Christine Yang,Jaume Balsells,Hong D. Chu,Jason M. Cox,Alejandro Crespo,Xiuying Ma,Lisa Contino,Patricia Brown,Sheng Gao,Beata Zamlynny,Judyann Wiltsie,Joseph Clemas,JeanMarie Lisnock,Jack Gibson,Gaochao Zhou,Margarita Garcia-Calvo,Thomas Bateman,Vincent Tong,Ling Xu,Martin Crook,Peter J. Sinclair,Hong C. Shen +21 more
TL;DR: The structure-activity relationship (SAR) exploration resulted in the discovery of potent and selective nonsteroidal mineralocorticoid receptor (MR) antagonists with significantly improved microsomal stability and pharmacokinetic (PK) profile relative to the HTS hit 1a.
Chronic Antagonism of the Mineralocorticoid Receptor Ameliorates Hypertension and End Organ Damage in a Rodent Model of Salt-Sensitive Hypertension
Xiaoyan Zhou,Martin Crook,Wanda Sharif-Rodriguez,Yonghua Zhu,Zadok Ruben,Yi Pan,Olga Urosevic-Price,Li Wang,Amy M. Flattery,Gail Forrest,Daphne Szeto,Huawei Zhao,Sophie Roy,Michael J. Forrest +13 more
TL;DR: It is demonstrated that mineralocorticoid receptor antagonism provides target organ protection and attenuates the development of elevated blood pressure (BP) in a model of salt-sensitive hypertension.
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Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists.
Anthony Ogawa,Ellen K. Vande Bunte,Rudrajit Mal,Ping Lan,Zhongxiang Sun,Alejandro Crespo,Judyann Wiltsie,Joseph Clemas,Jack Gibson,Lisa Contino,JeanMarie Lisnock,Gaochao Zhou,Margarita Garcia-Calvo,Nina Jochnowitz,Xiuying Ma,Yi Pan,Patricia Brown,Beata Zamlynny,Thomas Bateman,Dennis Leung,Ling Xu,Xinchun Tong,Kun Liu,Martin Crook,Peter J. Sinclair +24 more
TL;DR: A series of reverse indoles that represent novel non-steroidal mineralocorticoid receptor (MR) antagonists are reported that demonstrated efficacy in an acute natriuresis rodent model comparable to marketed MR antagonists, spironolactone and eplerenone.
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