Literature DB >> 20634066

Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution.

Takuya Miura1, Koushi Hidaka, Tsuyoshi Uemura, Keisuke Kashimoto, Yuto Hori, Yuko Kawasaki, Adam J Ruben, Ernesto Freire, Tooru Kimura, Yoshiaki Kiso.   

Abstract

We attached 2-aminoethylamino groups to allophenylnorstatine-containing plasmepsin (Plm) inhibitors and investigated SAR of the methyl or ethyl substitutions on the amino groups. Unexpectedly, compounds 22 (KNI-10743) and 25 (KNI-10742) exhibited extremely potent Plm II inhibitory activities (K(i)<0.1 nM). Moreover, among our peptidomimetic Plm inhibitors, we identified the compounds with the highest antimalarial activity using a SYBR Green I-based fluorescence assay. 2010 Elsevier Ltd. All rights reserved.

Entities:  

Mesh：

Substances：

Year:  2010        PMID： 20634066     DOI： 10.1016/j.bmcl.2010.06.099

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


  8 in total

1.  Deciphering the mechanism of potent peptidomimetic inhibitors targeting plasmepsins - biochemical and structural insights.

Authors:  Vandana Mishra; Ishan Rathore; Anagha Arekar; Lakshmi Kavitha Sthanam; Huogen Xiao; Yoshiaki Kiso; Shamik Sen; Swati Patankar; Alla Gustchina; Koushi Hidaka; Alexander Wlodawer; Rickey Y Yada; Prasenjit Bhaumik
Journal:  FEBS J       Date:  2018-07-07       Impact factor: 5.542

2.  Structures of plasmepsin II from Plasmodium falciparum in complex with two hydroxyethylamine-based inhibitors.

Authors:  Rosario Recacha; Janis Leitans; Inara Akopjana; Lilija Aprupe; Peteris Trapencieris; Kristaps Jaudzems; Aigars Jirgensons; Kaspars Tars
Journal:  Acta Crystallogr F Struct Biol Commun       Date:  2015-11-27       Impact factor: 1.056

3.  The zymogen of plasmepsin V from Plasmodium falciparum is enzymatically active.

Authors:  Huogen Xiao; Brian C Bryksa; Prasenjit Bhaumik; Alla Gustchina; Yoshiaki Kiso; Shao Q Yao; Alexander Wlodawer; Rickey Y Yada
Journal:  Mol Biochem Parasitol       Date:  2014-10-25       Impact factor: 1.759

Review 4.  Structural studies of vacuolar plasmepsins.

Authors:  Prasenjit Bhaumik; Alla Gustchina; Alexander Wlodawer
Journal:  Biochim Biophys Acta       Date:  2011-04-20

5.  New cathepsin D inhibitor library utilizing hydroxyethyl isosteres with cyclic tertiary amines.

Authors:  Rose M McConnell; Kalyani Inapudi; Naveen Kadasala; Karthika Yarlagadda; Priya Velusamy; Matthew S McConnell; Adam Green; Carol Trana; Kelley Sayyar; James S McConnell
Journal:  Med Chem       Date:  2012-11       Impact factor: 2.745

6.  Protease-associated cellular networks in malaria parasite Plasmodium falciparum.

Authors:  Timothy G Lilburn; Hong Cai; Zhan Zhou; Yufeng Wang
Journal:  BMC Genomics       Date:  2011-12-23       Impact factor: 3.969

7.  Synthesis and antimalarial potential of some novel quinoline-pyrazolopyridine derivatives.

Authors:  Deepika Saini; Sandeep Jain; Ajay Kumar; Neelam Jain
Journal:  EXCLI J       Date:  2016-11-28       Impact factor: 4.068

8.  Trafficked Proteins-Druggable in Plasmodium falciparum?

Authors:  Jasmin Lindner; Kamila Anna Meissner; Isolmar Schettert; Carsten Wrenger
Journal:  Int J Cell Biol       Date:  2013-04-28
  8 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.