Tags

Type your tag names separated by a space and hit enter

Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor.
J Med Chem. 2007 Dec 13; 50(25):6303-6.JM

Abstract

Biaryl anthranilides are reported as potent and selective full agonists for the high affinity niacin receptor GPR109A. The SAR presented outlines approaches to reduce serum shift and both CYPCYP2C8 and CYP2C9 liabilities, while improving PK and maintaining excellent receptor activity. Compound 2i exhibited good in vivo antilipolytic efficacy while providing a significantly improved therapeutic index over vasodilation (flushing) with respect to niacin in the mouse model.

Authors+Show Affiliations

Merck Research Laboratories, Merck & Co., Inc., Rahway, New Jersey 07065-0900, USA. hong_shen@merck.comNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

17994679

Citation

Shen, Hong C., et al. "Discovery of Biaryl Anthranilides as Full Agonists for the High Affinity Niacin Receptor." Journal of Medicinal Chemistry, vol. 50, no. 25, 2007, pp. 6303-6.
Shen HC, Ding FX, Luell S, et al. Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor. J Med Chem. 2007;50(25):6303-6.
Shen, H. C., Ding, F. X., Luell, S., Forrest, M. J., Carballo-Jane, E., Wu, K. K., Wu, T. J., Cheng, K., Wilsie, L. C., Krsmanovic, M. L., Taggart, A. K., Ren, N., Cai, T. Q., Deng, Q., Chen, Q., Wang, J., Wolff, M. S., Tong, X., Holt, T. G., ... Colletti, S. L. (2007). Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor. Journal of Medicinal Chemistry, 50(25), 6303-6.
Shen HC, et al. Discovery of Biaryl Anthranilides as Full Agonists for the High Affinity Niacin Receptor. J Med Chem. 2007 Dec 13;50(25):6303-6. PubMed PMID: 17994679.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor. AU - Shen,Hong C, AU - Ding,Fa-Xiang, AU - Luell,Silvi, AU - Forrest,Michael J, AU - Carballo-Jane,Ester, AU - Wu,Kenneth K, AU - Wu,Tsuei-Ju, AU - Cheng,Kang, AU - Wilsie,Larissa C, AU - Krsmanovic,Mihajlo L, AU - Taggart,Andrew K, AU - Ren,Ning, AU - Cai,Tian-Quan, AU - Deng,Qiaolin, AU - Chen,Qing, AU - Wang,Junying, AU - Wolff,Michael S, AU - Tong,Xinchun, AU - Holt,Tom G, AU - Waters,M Gerard, AU - Hammond,Milton L, AU - Tata,James R, AU - Colletti,Steven L, Y1 - 2007/11/10/ PY - 2007/11/13/pubmed PY - 2008/3/11/medline PY - 2007/11/13/entrez SP - 6303 EP - 6 JF - Journal of medicinal chemistry JO - J Med Chem VL - 50 IS - 25 N2 - Biaryl anthranilides are reported as potent and selective full agonists for the high affinity niacin receptor GPR109A. The SAR presented outlines approaches to reduce serum shift and both CYPCYP2C8 and CYP2C9 liabilities, while improving PK and maintaining excellent receptor activity. Compound 2i exhibited good in vivo antilipolytic efficacy while providing a significantly improved therapeutic index over vasodilation (flushing) with respect to niacin in the mouse model. SN - 0022-2623 UR - https://www.unboundmedicine.com/medline/citation/17994679/Discovery_of_biaryl_anthranilides_as_full_agonists_for_the_high_affinity_niacin_receptor_ L2 - https://doi.org/10.1021/jm700942d DB - PRIME DP - Unbound Medicine ER -