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Guo L, Parker DL, Zang Y, et al. Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes. ACS Med Chem Lett. 2016;7(12):1107-1111doi: 10.1021/acsmedchemlett.6b00314.
Guo, L., Parker, D. L., Zang, Y., Sweis, R. F., Liu, W., Sherer, E. C., Buist, N., Terebetski, J., Kelly, T., Bugianesi, R., Priest, B. T., Dingley, K. H., Li, X., Mitelman, S., Salituro, G., Trujillo, M. E., Pachanski, M., Kirkland, M., Powles, M. A., Eiermann, G. J., Feng, Y., Shang, J., Howard, A. D., Ujjainwalla, F., Sinz, C. J., Debenham, J. S., Edmondson, S. D., Nargund, R. P., Hagmann, W. K., & Li, D. (2016). Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes. ACS medicinal chemistry letters, 7(12), 1107-1111. https://doi.org/10.1021/acsmedchemlett.6b00314
Guo, Liangqin, et al. "Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes." ACS medicinal chemistry letters vol. 7,12 (2016): 1107-1111. doi: https://doi.org/10.1021/acsmedchemlett.6b00314
Guo L, Parker DL, Zang Y, Sweis RF, Liu W, Sherer EC, Buist N, Terebetski J, Kelly T, Bugianesi R, Priest BT, Dingley KH, Li X, Mitelman S, Salituro G, Trujillo ME, Pachanski M, Kirkland M, Powles MA, Eiermann GJ, Feng Y, Shang J, Howard AD, Ujjainwalla F, Sinz CJ, Debenham JS, Edmondson SD, Nargund RP, Hagmann WK, Li D. Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes. ACS Med Chem Lett. 2016 Oct 12;7(12):1107-1111. doi: 10.1021/acsmedchemlett.6b00314. eCollection 2016 Dec 08. PMID: 27994747; PMCID: PMC5150677.
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ACS Med Chem Lett. 2016 Oct 12;7(12):1107-1111. doi: 10.1021/acsmedchemlett.6b00314. eCollection 2016 Dec 08.

Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes.

ACS medicinal chemistry letters

Liangqin Guo, Dann L Parker, Yi Zang, Ramzi F Sweis, Weiguo Liu, Edward C Sherer, Nicole Buist, Jenna Terebetski, Terri Kelly, Randal Bugianesi, Birgit T Priest, Karen H Dingley, Xiaofang Li, Stan Mitelman, Gino Salituro, Maria E Trujillo, Michele Pachanski, Melissa Kirkland, Mary Ann Powles, George J Eiermann, Yue Feng, Jin Shang, Andrew D Howard, Feroze Ujjainwalla, Christopher J Sinz, John S Debenham, Scott D Edmondson, Ravi P Nargund, William K Hagmann, Derun Li

Affiliations

  1. Departments of Medicinal Chemistry, Discovery Pharmaceutical Sciences, Pharmacokenetics Pharmacodynamics Drug Metabolism, Diabetes Research, and Cardiometabolic Disease, Merck & Co., Inc., MRL , 126 East Lincoln Avenue, PO Box 2000, Rahway, New Jersey 07065, United States.

PMID: 27994747 PMCID: PMC5150677 DOI: 10.1021/acsmedchemlett.6b00314

Abstract

GPR142 has been identified as a potential glucose-stimulated insulin secretion (GSIS) target for the treatment of type 2 diabetes mellitus (T2DM). A class of triazole GPR142 agonists was discovered through a high throughput screen. The lead compound

Keywords: GPR142 agonists; glucose-stimulated insulin secretion (GSIS); solubility; triazole; type 2 diabetes mellitus (T2DM)

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