Discovery of a Potent and Selective ROMK Inhibitor with Pharmacokinetic Properties Suitable for Preclinical Evaluation

التفاصيل البيبلوغرافية
العنوان: Discovery of a Potent and Selective ROMK Inhibitor with Pharmacokinetic Properties Suitable for Preclinical Evaluation
المؤلفون: Lee-Yuh Pai, Yuping Zhu, Richard Visconti, Xiaoyan Zhou, John P. Felix, Melba Hernandez, Jing Chen, Michael Margulis, Nardos Teumelsan, Sophie Roy, Kathleen A. Sullivan, Jessica Liu, Joseph M. Metzger, Aaron Corona, Gregory J. Kaczorowski, Maria L. Garcia, Lihu Yang, Shawn P. Walsh, Birgit T. Priest, Alexander Pasternak, Caryn Hampton, Emma R. Parmee, Vincent Tong, Brande Thomas-Fowlkes, Haifeng Tang, Magdalena Alonso-Galicia, Kashmira Shah, Michael J. Forrest, Richard M. Brochu, Ross Bentley, Sookhee Ha, Karen Owens, Aurash Shahripour, Andrew M. Swensen, Jessica Frie, Adam B. Weinglass, Timothy Bailey
المصدر: ACS Medicinal Chemistry Letters. 6:747-752
بيانات النشر: American Chemical Society (ACS), 2015.
سنة النشر: 2015
مصطلحات موضوعية: Pharmacokinetics, Chemistry, Pharmacodynamics, Organic Chemistry, Drug Discovery, ROMK, Pharmacology, Biochemistry
الوصف: A new subseries of ROMK inhibitors exemplified by 28 has been developed from the initial screening hit 1. The excellent selectivity for ROMK inhibition over related ion channels and pharmacokinetic properties across preclinical species support further preclinical evaluation of 28 as a new mechanism diuretic. Robust pharmacodynamic effects in both SD rats and dogs have been demonstrated.
تدمد: 1948-5875
DOI: 10.1021/ml500440u
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::454c1f32ec6c3f7a915fe446fd2867a1
https://doi.org/10.1021/ml500440u
Rights: OPEN
رقم الانضمام: edsair.doi.dedup.....454c1f32ec6c3f7a915fe446fd2867a1
قاعدة البيانات: OpenAIRE
الوصف
تدمد:19485875
DOI:10.1021/ml500440u