Literature DB >> 19419862

Discovery of new S-adenosylmethionine decarboxylase inhibitors for the treatment of Human African Trypanosomiasis (HAT).

Bradford Hirth1, Robert H Barker, Cassandra A Celatka, Jeffrey D Klinger, Hanlan Liu, Bakela Nare, Amarjit Nijjar, Margaret A Phillips, Edmund Sybertz, Erin K Willert, Yibin Xiang.   

Abstract

Modification of the structure of trypanosomal AdoMetDC inhibitor 1 (MDL73811) resulted in the identification of a new inhibitor 7a, which features a methyl substituent at the 8-position. Compound 7a exhibits improved potencies against both the trypanosomal AdoMetDC enzyme and parasites, and better blood brain barrier penetration than 1.

Entities:  

Mesh：

Substances：

Year:  2009        PMID： 19419862     DOI： 10.1016/j.bmcl.2009.04.096

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


  7 in total

Review 1.  Recent developments in drug discovery for leishmaniasis and human African trypanosomiasis.

Authors:  Advait S Nagle; Shilpi Khare; Arun Babu Kumar; Frantisek Supek; Andriy Buchynskyy; Casey J N Mathison; Naveen Kumar Chennamaneni; Nagendar Pendem; Frederick S Buckner; Michael H Gelb; Valentina Molteni
Journal:  Chem Rev       Date:  2014-11-03       Impact factor: 60.622

2.  Improved Synthesis of MDL 73811 - a Potent AdoMetDC Inhibitor and Anti-Trypanosomal Compound.

Authors:  Anthony J Brockway; Casey C Cosner; Oleg A Volkov; Margaret A Phillips; Jef K De Brabander
Journal:  Synthesis (Stuttg)       Date:  2016-07       Impact factor: 3.157

3.  High affinity S-Adenosylmethionine plasma membrane transporter of Leishmania is a member of the folate biopterin transporter (FBT) family.

Authors:  Larbi Dridi; Amin Ahmed Ouameur; Marc Ouellette
Journal:  J Biol Chem       Date:  2010-04-20       Impact factor: 5.157

4.  The Trypanosoma cruzi Diamine Transporter Is Essential for Robust Infection of Mammalian Cells.

Authors:  Marie-Pierre Hasne; Radika Soysa; Buddy Ullman
Journal:  PLoS One       Date:  2016-04-06       Impact factor: 3.240

5.  Structure-Based Design, Synthesis and Biological Evaluation of Bis-Tetrahydropyran Furan Acetogenin Mimics Targeting the Trypanosomatid F1 Component of ATP Synthase.

Authors:  Marija K Zacharova; Lindsay B Tulloch; Eoin R Gould; Andrew L Fraser; Elizabeth F King; Stefanie K Menzies; Terry K Smith; Gordon J Florence
Journal:  European J Org Chem       Date:  2019-05-29

6.  Development of Novel Isoindolone-Based Compounds against Trypanosoma brucei rhodesiense.

Authors:  Daniel G Silva; Pim-Bart Feijens; Rik Hendrickx; An Matheeussen; Lucie Grey; Guy Caljon; Louis Maes; Flavio S Emery; Anna Junker
Journal:  ChemistryOpen       Date:  2021-09       Impact factor: 2.911

7.  Novel S-adenosyl-L-methionine decarboxylase inhibitors as potent antiproliferative agents against intraerythrocytic Plasmodium falciparum parasites.

Authors:  Dina le Roux; Pieter B Burger; Jandeli Niemand; Anne Grobler; Patricia Urbán; Xavier Fernàndez-Busquets; Robert H Barker; Adelfa E Serrano; Abraham I Louw; Lyn-Marie Birkholtz
Journal:  Int J Parasitol Drugs Drug Resist       Date:  2013-12-05       Impact factor: 4.077
  7 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.