2Q1L

Design and synthesis of hepatoselective, pyrrole-based HMG-CoA reductase inhibitors.

Pfefferkorn, J.A., Song, Y., Sun, K.L., Miller, S.R., Trivedi, B.K., Choi, C., Sorenson, R.J., Bratton, L.D., Unangst, P.C., Larsen, S.D., Poel, T.J., Cheng, X.M., Lee, C., Erasga, N., Auerbach, B., Askew, V., Dillon, L., Hanselman, J.C., Lin, Z., Lu, G., Robertson, A., Olsen, K., Mertz, T., Sekerke, C., Pavlovsky, A., Harris, M.S., Bainbridge, G., Caspers, N., Chen, H., Eberstadt, M.

(2007) Bioorg Med Chem Lett 17: 4538-4544

• PubMed: 17574412 Search on PubMed
• DOI: https://doi.org/10.1016/j.bmcl.2007.05.096
• Primary Citation of Related Structures:  
  2Q1L


• PubMed Abstract: 
  

  This manuscript describes the design and synthesis of a series of pyrrole-based inhibitors of HMG-CoA reductase for the treatment of hypercholesterolemia. Analogs were optimized using structure-based design and physical property considerations resulting in the identification of 44, a hepatoselective HMG-CoA reductase inhibitor with excellent acute and chronic efficacy in a pre-clinical animal models.

   View More

---

Organizational Affiliation: 

Pfizer Global Research & Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. jeffrey.a.pfefferkorn@pfizer.com