Literature DB >> 12467623

Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 3.

Ken-ichi Kawasaki1, Miyako Masubuchi, Kenji Morikami, Satoshi Sogabe, Tsunehisa Aoyama, Hirosato Ebiike, Satoshi Niizuma, Michiko Hayase, Toshihiko Fujii, Kiyoaki Sakata, Hidetoshi Shindoh, Yasuhiko Shiratori, Yuko Aoki, Tatsuo Ohtsuka, Nobuo Shimma.   

Abstract

A new series of acid-stable antifungal agents having strong inhibitory activity against Candida albicans N-myristoyltransferase (CaNmt) has been developed starting from acid-unstable benzofuranylmethyl aryl ether 2. The inhibitor design is based on X-ray crystallographic analysis of a CaNmt complex with aryl ether 3. Among the new inhibitors, pyridine derivative 8b and benzimidazole derivative 8k showed clear antifungal activity in a murine systemic candidiasis model.

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Year:  2003        PMID： 12467623     DOI： 10.1016/s0960-894x(02)00844-2

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


  16 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 new approach to fused furan ring systems and benzofurans: Intramolecular cyclization reactions of unsaturated acyloxy sulfone derivatives.

Authors:  Yuan Liu; Hollie K Jacobs; Aravamudan S Gopalan
Journal:  Tetrahedron Lett       Date:  2011-06-08       Impact factor: 2.415

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

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

4.  Identifying regulators for EAG1 channels with a novel electrophysiology and tryptophan fluorescence based screen.

Authors:  Tinatin I Brelidze; Anne E Carlson; Douglas R Davies; Lance J Stewart; William N Zagotta
Journal:  PLoS One       Date:  2010-09-02       Impact factor: 3.240

5.  Synthesis of multi-functionalized benzofurans through the condensation of ninhydrin and phenols using SSA as a recyclable heterogeneous acid catalyst.

Authors:  Ashis Kundu; Animesh Pramanik
Journal:  Mol Divers       Date:  2016-02-01       Impact factor: 2.943

6.  A novel and facile synthesis of 3-(2-benzofuroyl)- and 3,6-bis(2-benzofuroyl)carbazole derivatives.

Authors:  Wentao Gao; Meiru Zheng; Yang Li
Journal:  Beilstein J Org Chem       Date:  2011-11-17       Impact factor: 2.883

7.  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

8.  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

9.  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

10.  Discovery of novel and ligand-efficient inhibitors of Plasmodium falciparum and Plasmodium vivax N-myristoyltransferase.

Authors:  Mark D Rackham; James A Brannigan; David K Moss; Zhiyong Yu; Anthony J Wilkinson; Anthony A Holder; Edward W Tate; Robin J Leatherbarrow
Journal:  J Med Chem       Date:  2012-12-17       Impact factor: 7.446
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