Literature DB >> 15755653

Synthesis of potent and selective inhibitors of Candida albicans N-myristoyltransferase based on the benzothiazole structure.

Kazuo Yamazaki1, Yasushi Kaneko, Kie Suwa, Shinji Ebara, Kyoko Nakazawa, Kazuhiro Yasuno.   

Abstract

Two parallel synthetic methods using solid-supported reagents were established to examine the rapid optimization of weak hit compound 1. Several compounds showed high potency in the low nanomolar range against N-myristoyltransferase. The structure-activity relationship (SAR) and antifungal activities of a series of novel 2-aminobenzothiazole N-myristoyltransferase inhibitors are presented.

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Year:  2005        PMID： 15755653     DOI： 10.1016/j.bmc.2005.01.033

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  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.  Protein Lipidation: Occurrence, Mechanisms, Biological Functions, and Enabling Technologies.

Authors:  Hong Jiang; Xiaoyu Zhang; Xiao Chen; Pornpun Aramsangtienchai; Zhen Tong; Hening Lin
Journal:  Chem Rev       Date:  2018-01-02       Impact factor: 60.622

3.  Novel Thienopyrimidine Inhibitors of Leishmania N-Myristoyltransferase with On-Target Activity in Intracellular Amastigotes.

Authors:  Andrew S Bell; Zhiyong Yu; Jennie A Hutton; Megan H Wright; James A Brannigan; Daniel Paape; Shirley M Roberts; Charlotte L Sutherell; Markus Ritzefeld; Anthony J Wilkinson; Deborah F Smith; Robin J Leatherbarrow; Edward W Tate
Journal:  J Med Chem       Date:  2020-07-14       Impact factor: 7.446

4.  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

Review 5.  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

6.  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

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.  Selective inhibitors of protozoan protein N-myristoyltransferases as starting points for tropical disease medicinal chemistry programs.

Authors:  Andrew S Bell; James E Mills; Gareth P Williams; James A Brannigan; Anthony J Wilkinson; Tanya Parkinson; Robin J Leatherbarrow; Edward W Tate; Anthony A Holder; Deborah F Smith
Journal:  PLoS Negl Trop Dis       Date:  2012-04-24

9.  Synthesis of benzo[d]thiazole-hydrazone analogues: molecular docking and SAR studies of potential H+/K+ ATPase inhibitors and anti-inflammatory agents.

Authors:  Shi-Meng Wang; Gao-Feng Zha; K P Rakesh; N Darshini; T Shubhavathi; H K Vivek; N Mallesha; Hua-Li Qin
Journal:  Medchemcomm       Date:  2017-04-26       Impact factor: 3.597

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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