Literature DB >> 26555357

Microwave-assisted solid-phase synthesis of side-chain to side-chain lactam-bridge cyclic peptides.

Srinivasa R Tala1, Sathya M Schnell1, Carrie Haskell-Luevano2.   

Abstract

Side-chain to side-chain lactam-bridged cyclic peptides have been utilized as therapeutic agents and biochemical tools. Previous synthetic methods of these peptides need special reaction conditions, form side products and take longer reaction times. Herein, an efficient microwave-assisted synthesis of side-chain to side-chain lactam-bridge cyclic peptides SHU9119 and MTII is reported. The synthesis time and efforts are significantly reduced in the present method, without side product formation. The analytical and pharmacological data of the synthesized cyclic peptides are in accordance with the commercially obtained compounds. This new method could be used to synthesize other side-chain to side-chain lactam-bridge peptides and amenable to automation and extensive SAR compound derivatization.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Cyclic peptides; Lactam-bridge cyclic peptides; MTII; Microwave assisted synthesis; SHU9119

Mesh：

Substances：

Year:  2015        PMID： 26555357      PMCID： PMC4654418          DOI： 10.1016/j.bmcl.2015.10.095

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


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