Literature DB >> 27622649

Onchocerca volvulus Molting Inhibitors Identified through Scaffold Hopping.

Major Gooyit1, Tyler L Harris1, Nancy Tricoche2, Sacha Javor1, Sara Lustigman2, Kim D Janda1.   

Abstract

The anthelmintic closantel has shown promise in abrogating the L3 molting of Onchocerca volvulus, the causative agent of the infectious disease onchocerciasis. In our search for alternative scaffolds, we utilized a fragment replacement/modification approach to generate novel chemotypes with improved chitinase inhibitory properties. Further evaluation of the compounds unveiled the potential of urea-tropolones as potent inhibitors of O. volvulus L3 molting.

Entities:  

Keywords:  molting; onchocerciasis; tropolones

Year:  2015        PMID: 27622649     DOI: 10.1021/acsinfecdis.5b00017

Source DB:  PubMed          Journal:  ACS Infect Dis        ISSN: 2373-8227            Impact factor:   5.084


  5 in total

1.  Reprofiled anthelmintics abate hypervirulent stationary-phase Clostridium difficile.

Authors:  Major Gooyit; Kim D Janda
Journal:  Sci Rep       Date:  2016-09-16       Impact factor: 4.379

2.  Macrofilaricidal Benzimidazole-Benzoxaborole Hybrids as an Approach to the Treatment of River Blindness: Part 2. Ketone Linked Analogs.

Authors:  David S Carter; Robert T Jacobs; Yvonne R Freund; Pamela W Berry; Tsutomu Akama; Eric E Easom; Christopher S Lunde; Fernando Rock; Rianna Stefanakis; James McKerrow; Chelsea Fischer; Christina A Bulman; Kee Chong Lim; Brian M Suzuki; Nancy Tricoche; Judy A Sakanari; Sara Lustigman; Jacob J Plattner
Journal:  ACS Infect Dis       Date:  2020-01-28       Impact factor: 5.084

3.  Macrofilaricidal Benzimidazole-Benzoxaborole Hybrids as an Approach to the Treatment of River Blindness: Part 1. Amide Linked Analogs.

Authors:  Tsutomu Akama; Yvonne R Freund; Pamela W Berry; David S Carter; Eric E Easom; Kurt Jarnagin; Christopher S Lunde; Jacob J Plattner; Fernando Rock; Rianna Stefanakis; Chelsea Fischer; Christina A Bulman; Kee Chong Lim; Brian M Suzuki; Nancy Tricoche; Abdelmoneim Mansour; Utami DiCosty; Scott McCall; Ben Carson; John W McCall; James McKerrow; Marc P Hübner; Sabine Specht; Achim Hoerauf; Sara Lustigman; Judy A Sakanari; Robert T Jacobs
Journal:  ACS Infect Dis       Date:  2020-01-14       Impact factor: 5.084

4.  Identification and activity of inhibitors of the essential nematode-specific metalloprotease DPY-31.

Authors:  David J France; Gillian Stepek; Douglas R Houston; Lewis Williams; Gillian McCormack; Malcolm D Walkinshaw; Antony P Page
Journal:  Bioorg Med Chem Lett       Date:  2015-11-03       Impact factor: 2.823

5.  Structure-based virtual screening of highly potent inhibitors of the nematode chitinase CeCht1.

Authors:  Wei Chen; Qi Chen; Ashutosh Kumar; Xi Jiang; Kam Y J Zhang; Qing Yang
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051

  5 in total

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