What's new for 'Trypanosomatids' in PubMed

This message contains My NCBI what's new results from the National Center for Biotechnology Information (NCBI) at the U.S. National Library of Medicine (NLM).
Do not reply directly to this message.

Sender's message:

Sent on Wednesday, 2012 January 18
Search: kinetoplastids OR kinetoplastid OR Kinetoplastida OR "trypanosoma brucei" OR leishmania OR brucei OR leishmaniasis OR "African trypanosomiasis"

Click here to view complete results in PubMed (Results may change over time.)
To unsubscribe from these e-mail updates click here.

PubMed Results

Items 1 - 3 of 3

1.	Bioorg Med Chem. 2011 Dec 30. [Epub ahead of print] Identification of Trypanosoma brucei leucyl-tRNA synthetase inhibitors by pharmacophore- and docking-based virtual screening and synthesis. Zhao Y, Wang Q, Meng Q, Ding D, Yang H, Gao G, Li D, Zhu W, Zhou H. Source School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, China. Abstract Human African trypanosomiasis (HAT), caused by the protozoan parasite Trypanosoma brucei, is a neglected fatal disease. Leucyl-tRNA synthetase (LeuRS), which has been successfully applied in the development of antifungal agent, represents a potential antiprotozoal drug target. In this study, a 3D model of T. brucei LeuRS (TbLeuRS) synthetic active site was constructed and subjected to virtual screening using a combination of pharmacophore- and docking-based methods. A new 2-pyrrolinone scaffold was discovered and the structure-activity relationship (SAR) studies aided by the docking model and organic synthesis were carried out. Compounds with various substituents on R(1), R(2) and R(3) were synthesized and their SAR was discussed. Copyright © 2012. Published by Elsevier Ltd.
	PMID: 22249121 [PubMed - as supplied by publisher]
	Related citations

2.	Curr Opin Infect Dis. 2012 Jan 13. [Epub ahead of print] Miltefosine and cutaneous leishmaniasis. Machado PR, Penna G. Source aServiço de Imunologia, Complexo Hospitalar Universitário Prof. Edgard Santos, Universidade Federal da Bahia, Salvador, Bahia bTropical Medicine Centre, University of Brasilia, Oswaldo Cruz Foundation (Fiocruz), Rio de Janeiro, Rio de Janeiro, Brazil. Abstract PURPOSE OF REVIEW: Miltefosine is a new oral treatment against leishmaniasis. The evidence about its use in New and Old World cutaneous leishmaniasis is presented and discussed. RECENT FINDINGS: Miltefosine is being tested with small clinical trials mainly in endemic cutaneous leishmaniasis regions of South America and Iran. Severe cutaneous leishmaniasis forms successfully treated with miltefosine are reported. SUMMARY: The use of miltefosine in cutaneous leishmaniasis has been addressed in a few clinical trials. An important advantage of this drug is its oral administration when compared with the standard parenteral drugs in the context of a large-scale use in the inner regions of the endemic countries. Miltefosine also shows activity in severe or refractory cases. However, this review points out the need for further investment on clinical research into cutaneous leishmaniasis treatment.
	PMID: 22248979 [PubMed - as supplied by publisher]
	Related citations

3.	Bioorg Med Chem Lett. 2011 Dec 28. [Epub ahead of print] Synthesis and antikinetoplastid activity of a series of N,N'-substituted diamines. Caminos AP, Panozzo-Zenere EA, Wilkinson SR, Tekwani BL, Labadie GR. Source Instituto de Química Rosario (IQUIR-CONICET-UNR), Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, S2002LRK, Rosario, Argentina. Abstract A series of 25 N,N'-substituted diamines were prepared by controlled reductive amination of free aliphatic diamines with different substituted benzaldehydes. The library was screened in vitro for antiparasitic activity on the causative agents of human African trypanosomiasis, Chagas' disease and visceral leishmaniasis. The most potent compounds were derived from a subset of diamines that contained a 4-OBn substitution, having a 50% parasite growth inhibition in the submicromolar (against Trypanosoma cruzi) or nanomolar (against Trypanosoma brucei and Leishmania donovani) range. We conclude that members of this series of N,N'-substituted diamines provide new lead structures that have potential to treat trypanosomal and leishmanial infections. Copyright © 2011 Elsevier Ltd. All rights reserved.
	PMID: 22248858 [PubMed - as supplied by publisher]
	Related citations