Literature DB >> 21211872

Synthesis of elastin based peptides conjugated to benzisoxazole as a new class of potent antimicrobials--A novel approach to enhance biocompatibility.

R Suhas1, S Chandrashekar, D Channe Gowda.   

Abstract

The peptides of elastin sequences chosen for the present study included tetrapeptides, pentapeptides and tricosapeptides (30 amino acids), synthesized by classical solution phase method and conjugated to [3-(4-piperidyl)-6-fluoro-1,2-benzisoxazole]. The structures of the compounds were confirmed by physical and spectroscopic techniques followed by the antimicrobial evaluation by both agar well diffusion and microdilution methods. Here we wish to report the effect of conjugation of these moieties which enabled us to identify a novel set of peptides conjugated to heterocycle which have exhibited more potent antimicrobial activity than the conventional drugs used. Further, conjugates of tricosamers 34 and 35 were able to inhibit the growth of fungal species at 3-5 μg/mL which is nearly 5 fold more potent than the reference drug. Copyright Â
© 2010 Elsevier Masson SAS. All rights reserved.

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Year:  2010        PMID: 21211872     DOI: 10.1016/j.ejmech.2010.12.005

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  4 in total

1.  A correlation study of biological activity and molecular docking of Asp and Glu linked bis-hydrazones of quinazolinones.

Authors:  H K Kumara; R Suhas; D M Suyoga Vardhan; M Shobha; D Channe Gowda
Journal:  RSC Adv       Date:  2018-03-16       Impact factor: 4.036

2.  Solution-phase synthesis of a diverse library of benzisoxazoles utilizing the [3 + 2] cycloaddition of in situ-generated nitrile oxides and arynes.

Authors:  Anton V Dubrovskiy; Prashi Jain; Feng Shi; Gerald H Lushington; Conrad Santini; Patrick Porubsky; Richard C Larock
Journal:  ACS Comb Sci       Date:  2013-03-08       Impact factor: 3.784

3.  Peptide-conjugated pterins as inhibitors of ricin toxin A.

Authors:  Ryota Saito; Jeff M Pruet; Lawrence A Manzano; Karl Jasheway; Arthur F Monzingo; Paul A Wiget; Ishan Kamat; Eric V Anslyn; Jon D Robertus
Journal:  J Med Chem       Date:  2012-12-19       Impact factor: 7.446

Review 4.  Benzisoxazole: a privileged scaffold for medicinal chemistry.

Authors:  K P Rakesh; C S Shantharam; M B Sridhara; H M Manukumar; Hua-Li Qin
Journal:  Medchemcomm       Date:  2017-10-31       Impact factor: 3.597

  4 in total

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