Antimicrobial activity of simplified mimics of celogentin C
Varsha J Thombare, James A Holden, Sreetama Pal, Eric C Reynolds, Amitabha Chattopadhyay, Neil M O'Brien-Simpson, Craig A Hutton
TETRAHEDRON | PERGAMON-ELSEVIER SCIENCE LTD | Published : 2018
Linear and bicyclic analogues of the peptide natural product, celogentin C, have been prepared in which the sidechain–sidechain crosslinks in celogentin are omitted or replaced with a mesitylenyl moiety. The simplified bicyclic peptides display moderate antibacterial activity, potentially through inhibition of bacterial protomicrotubule formation, while the linear analogs show higher antibacterial activity through a possible membrane disruption mechanism.
This work was supported by the Australian Research Council, The University of Melbourne (IRRTF, MRS to V.T.) and the Council of Scientific and Industrial Research, Govt. of India (A.C.). S.P. thanks the University Grants Commission (Govt. of India) for the award of a Senior Research Fellowship. A.C. is an Adjunct Professor of Tata Institute of Fundamental Research (Mumbai), RMIT University (Melbourne, Australia), Indian Institute of Technology (Kanpur), and Indian Institute of Science Education and Research (Mohali). A.C. gratefully acknowledges support from J.C. Bose Fellowship (Department of Science and Technology, Govt. of India).