Literature DB >> 11844682

Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 2.

Hirosato Ebiike1, Miyako Masubuchi, Pingli Liu, Ken-ichi Kawasaki, Kenji Morikami, Satoshi Sogabe, Michiko Hayase, Toshihiko Fujii, Kiyoaki Sakata, Hidetoshi Shindoh, Yasuhiko Shiratori, Yuko Aoki, Tatsuo Ohtsuka, Nobuo Shimma.   

Abstract

Modification of the C-2 position of a benzofuran derivative 6 (RO-09-4609), an N-myristoyltransferase (Nmt) inhibitor, has led us to discover antifungal agents that are active in a murine systemic candidiasis model. The drug design is based on the analysis of a crystal structure of a Candida Nmt complex with 2. The optimization has been guided by various biological evaluations including a quasi in vivo assay and pharmacokinetic analysis.

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Year:  2002        PMID： 11844682     DOI： 10.1016/s0960-894x(01)00808-3

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


  13 in total

1.  Homology modeling and molecular dynamics simulation of N-myristoyltransferase from protozoan parasites: active site characterization and insights into rational inhibitor design.

Authors:  Chunquan Sheng; Haitao Ji; Zhenyuan Miao; Xiaoyin Che; Jianzhong Yao; Wenya Wang; Guoqiang Dong; Wei Guo; Jiaguo Lü; Wannian Zhang
Journal:  J Comput Aided Mol Des       Date:  2009-04-16       Impact factor: 3.686

2.  A highly convergent synthesis of myristoyl-carba(dethia)-coenzyme A.

Authors:  Lutz Tautz; Janos Rétey
Journal:  European J Org Chem       Date:  2010-03

3.  Characterization and selective inhibition of myristoyl-CoA:protein N-myristoyltransferase from Trypanosoma brucei and Leishmania major.

Authors:  Chrysoula Panethymitaki; Paul W Bowyer; Helen P Price; Robin J Leatherbarrow; Katherine A Brown; Deborah F Smith
Journal:  Biochem J       Date:  2006-06-01       Impact factor: 3.857

4.  Molecules incorporating a benzothiazole core scaffold inhibit the N-myristoyltransferase of Plasmodium falciparum.

Authors:  Paul W Bowyer; Ruwani S Gunaratne; Munira Grainger; Chrislaine Withers-Martinez; Sasala R Wickramsinghe; Edward W Tate; Robin J Leatherbarrow; Katherine A Brown; Anthony A Holder; Deborah F Smith
Journal:  Biochem J       Date:  2007-12-01       Impact factor: 3.857

5.  Validation of N-myristoyltransferase as an antimalarial drug target using an integrated chemical biology approach.

Authors:  Megan H Wright; Barbara Clough; Mark D Rackham; Kaveri Rangachari; James A Brannigan; Munira Grainger; David K Moss; Andrew R Bottrill; William P Heal; Malgorzata Broncel; Remigiusz A Serwa; Declan Brady; David J Mann; Robin J Leatherbarrow; Rita Tewari; Anthony J Wilkinson; Anthony A Holder; Edward W Tate
Journal:  Nat Chem       Date:  2013-12-22       Impact factor: 24.427

6.  Discovery of a novel class of orally active trypanocidal N-myristoyltransferase inhibitors.

Authors:  Stephen Brand; Laura A T Cleghorn; Stuart P McElroy; David A Robinson; Victoria C Smith; Irene Hallyburton; Justin R Harrison; Neil R Norcross; Daniel Spinks; Tracy Bayliss; Suzanne Norval; Laste Stojanovski; Leah S Torrie; Julie A Frearson; Ruth Brenk; Alan H Fairlamb; Michael A J Ferguson; Kevin D Read; Paul G Wyatt; Ian H Gilbert
Journal:  J Med Chem       Date:  2011-12-07       Impact factor: 7.446

7.  Microwave-assisted preparation and antimicrobial activity of O-alkylamino benzofurancarboxylates.

Authors:  Kinga Ostrowska; Elżbieta Hejchman; Irena Wolska; Hanna Kruszewska; Dorota Maciejewska
Journal:  Monatsh Chem       Date:  2013-08-16       Impact factor: 1.451

8.  N-myristoyltransferase is a cell wall target in Aspergillus fumigatus.

Authors:  Wenxia Fang; David A Robinson; Olawale G Raimi; David E Blair; Justin R Harrison; Deborah E A Lockhart; Leah S Torrie; Gian Filippo Ruda; Paul G Wyatt; Ian H Gilbert; Daan M F van Aalten
Journal:  ACS Chem Biol       Date:  2015-02-27       Impact factor: 5.100

Review 9.  Drug discovery for neglected diseases: molecular target-based and phenotypic approaches.

Authors:  Ian H Gilbert
Journal:  J Med Chem       Date:  2013-09-09       Impact factor: 7.446

10.  Design and synthesis of inhibitors of Plasmodium falciparum N-myristoyltransferase, a promising target for antimalarial drug discovery.

Authors:  Zhiyong Yu; James A Brannigan; David K Moss; A Marek Brzozowski; Anthony J Wilkinson; Anthony A Holder; Edward W Tate; Robin J Leatherbarrow
Journal:  J Med Chem       Date:  2012-10-15       Impact factor: 7.446
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