Oxadiazole-Containing Cyclic Peptides

Macrocycles are among the most promising compounds pursued by the pharmaceutical industry. The combination of a (N-isocyanoimino) phosphorane, an aldehyde, and a linear peptide produces cyclic peptides containing 1,3,4,-oxadiazole moieties, imbedded within the peptide backbone, in a single step. The proprietary process involves connecting the ends of a linear peptide chain and simultaneously introducing an oxadiazole (ODZ) ring at the point of suture resulting in the so-called “ODZ macrocycles”. The oxadiazole ring is well regarded for its ability to mimic peptide bonds, yet impart superior drug-like properties to the corresponding molecules. This invention is a method that facilitates the rapid assembly of structurally and functionally diverse therapeutically relevant cyclic compounds by “depeptidizing” lead molecules and bestowing upon them the key attributes of medicinally relevant heterocycles.

ID:

P1908

Keywords:

Chemical Synthesis , Drug Discovery , Peptides

VPRI Contact

Marilee Krinsky

Technology Commercialization Manager
Innovations & Partnerships Office (IPO)
(416) 978-2514

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