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Project TitleNovel Antibiotics for Drug Resistant Bacteria
Track Code2016-021
Short Description
Abstract
 
Tagsantibiotic, antibiotic resistance, therapeutic
 
Posted DateMay 18, 2016 1:17 PM

Challenge

Infectious diseases are currently the second leading cause of death worldwide and the third leading cause of death in developed countries such as the United States. Moreover, the emergence of bacterial resistance to currently used antibiotics poses a serious threat to human health and represents a severe global problem. New chemical entities having different mechanisms of action from common antibiotics and that are particularly effective against drug resistant bacteria are needed.

Solution

Rice researchers have developed novel antibacterial agents that possess high potency against drug resistant bacteria. These compounds are analogs of antibiotic CJ-16,264 which is a relatively new candidate useful for the control of number of infectious bacteria. An optimized enantioselective route to synthesis of CJ-16,264 has been invented. Simpler and more potent analogs of CJ-16,264 have been identified through comprehensive structure-activity relationship (SAR) studies.

Benefits and Features

  • Potent antibacterial compounds
  • Enantioselective synthesis of antibiotic CJ-16,264
  • Simple synthetic route to active analogs that is amenable to large scale production

Market Potential / Applications

Antibiotic resistance is emerging as a global health crisis and is attributed to the misuse and overuse of these medications. Reduced economic incentives and challenging regulatory requirements have led several pharmaceutical companies to abandon research in this area and this has further worsened the issue. The present invention addresses the problem of antibiotic resistance and could be useful to combat infections caused by drug resistant bacteria.

Development and Licensing Status

Synthetic feasibility of antibiotic CJ-16,264 and related analogs has been demonstrated on laboratory scale. Biological evaluation of the compounds for antibacterial activity has been conducted. The technology is available for licensing from Rice University.

Rice Researcher

Prof. Nicolaou is the Harry C. and Olga K. Wiess Professor of Chemistry at Rice University, and the recent recipient of the Wolfe Prize in Chemistry. Research in the Nicolaou lab is focused on the study of the chemistry and biology of architecturally novel and biologically important natural products as well as designed molecules encompassing total synthesis, solid phase chemistry, molecular design, combinatorial synthesis and biological investigations.

Technology Relevant Papers and Web Links

  • Nicolaou KC, Shah AA, Korman H, Khan T, Shi L, Worawalai W, Theodorakis EA Total Synthesis and Structural Revision of Antibiotic CJ-16,264 Angew. Chem. Int. Ed. Engl., 2015, 54(32), 9203-8.
  • US provisional patent application claiming the synthetic methods, compositions and biological activity of novel CJ-16,264 analogs and their potential uses has been filed.
  • Researcher web site: http://nicolaou.rice.edu/kcn.html

Case #

2016-021

Inquiries to:

Neha Malik, neha.malik@rice.edu, (713) 348-4106