SAR studies on dihydropyrimidinone antibiotics

Lianhong Xu; Lijun Zhang; Robert Jones; Clifford Bryant; Nina Boddeker; Eric Mabery; Gina Bahador; Julia Watson; Jeffery Clough; Murty Arimilli; Wendy Gillette; Dorothy Colagiovanni; Keyu Wang; Craig Gibbs; Choung U Kim

doi:10.1016/j.bmcl.2011.01.099

SAR studies on dihydropyrimidinone antibiotics

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1670-4. doi: 10.1016/j.bmcl.2011.01.099. Epub 2011 Jan 31.

Authors

Lianhong Xu¹, Lijun Zhang, Robert Jones, Clifford Bryant, Nina Boddeker, Eric Mabery, Gina Bahador, Julia Watson, Jeffery Clough, Murty Arimilli, Wendy Gillette, Dorothy Colagiovanni, Keyu Wang, Craig Gibbs, Choung U Kim

Affiliation

¹ Gilead Sciences Inc., Foster City, CA 94404, USA. lianhong.xu@gilead.com

PMID: 21324685
DOI: 10.1016/j.bmcl.2011.01.099

Abstract

There is an urgent need for the development of novel antimicrobial agents that offer effective treatment against MRSA. Using a new class of dipeptide antibiotic TAN-1057A/B as lead, we designed, synthesized and evaluated analogs of TAN-1057A/B. Several novel dihydropyrimidinone antibiotics demonstrating comparable antibiotic efficacy while possessing favorable selectivity were identified.

MeSH terms

Anti-Bacterial Agents / chemistry*
Anti-Bacterial Agents / pharmacology*
Microbial Sensitivity Tests
Pyrimidines / chemistry*
Pyrimidines / pharmacology*
Structure-Activity Relationship

Substances

Anti-Bacterial Agents
Pyrimidines