What's new for 'Trypanosomatids' in PubMed

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Sent on Saturday, 2010 Aug 28
Search kinetoplastids OR kinetoplastid OR Kinetoplastida OR "trypanosoma brucei" OR leishmania OR brucei OR leishmaniasis OR "African trypanosomiasis"
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PubMed Results

Items 1 - 4 of 4

1.	ChemMedChem. 2010 Aug 26. [Epub ahead of print] alpha-Ketoheterocycles as Inhibitors of Leishmania mexicana Cysteine Protease CPB. Steert K, Berg M, Mottram JC, Westrop GD, Coombs GH, Cos P, Maes L, Joossens J, Van der Veken P, Haemers A, Augustyns K. Department of Medicinal Chemistry, University of Antwerp, Universiteitsplein 1, 2610 Antwerp (Belgium), Fax: (+32) 3-265-27-39. Abstract Cysteine proteases of the papain superfamily are present in nearly all eukaryotes and also play pivotal roles in the biology of parasites. Inhibition of cysteine proteases is emerging as an important strategy to combat parasitic diseases such as sleeping sickness, Chagas disease, and leishmaniasis. Inspired by the in vivo antiparasitic activity of the vinylsulfone-based cysteine protease inhibitors, a series of alpha-ketoheterocycles were developed as reversible inhibitors of a recombinant L. mexicana cysteine protease, CPB2.8. Three isoxazoles and especially one oxadiazole compound are potent reversible inhibitors of CPB2.8; however, in vitro whole-organism screening against a panel of protozoan parasites did not fully correlate with the observed inhibition of the cysteine protease.
	PMID: 20799311 [PubMed - as supplied by publisher]
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2.	East Mediterr Health J. 2010 Mar;16(3):344-5. Lupoid leishmaniasis due to Leishmania major with remaining large scars: report of 2 cases. Sadeghian G, Ziaei H, Shirani-Bidabadi L, Nilforoushzadeh MA. Skin Disease and Leishmaniasis Research Center, Isfahan University of Medical Sciences, Isfahan, Islamic Republic of Iran. Sadeghian@sdlrc.mui.ac.ir
	PMID: 20795453 [PubMed - in process]
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3.	East Mediterr Health J. 2010 Mar;16(3):340-3. Disseminated leishmaniasis caused by Leishmania tropica in HIV-positive patients in the Islamic Republic of Iran. Jafari S, Hajiabdolbaghi M, Mohebali M, Hajjaran H, Hashemian H. Department of Infectious Diseases, Imam Khomeini Hospital, Islamic Republic of Iran.
	PMID: 20795452 [PubMed - in process]
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4.	Bioorg Med Chem. 2010 Jun 1;18(11):4056-66. Epub 2010 Apr 9. Synthesis and characterization of potent inhibitors of Trypanosoma cruzi dihydrofolate reductase. Schormann N, Velu SE, Murugesan S, Senkovich O, Walker K, Chenna BC, Shinkre B, Desai A, Chattopadhyay D. Department of Medicine, University of Alabama, Birmingham, Birmingham, AL 35294, USA. Abstract Dihydrofolate reductase (DHFR) of the parasite Trypanosoma cruzi (T. cruzi) is a potential target for developing drugs to treat Chagas' disease. We have undertaken a detailed structure-activity study of this enzyme. We report here synthesis and characterization of six potent inhibitors of the parasitic enzyme. Inhibitory activity of each compound was determined against T. cruzi and human DHFR. One of these compounds, ethyl 4-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy)butanoate (6b) was co-crystallized with the bifunctional dihydrofolate reductase-thymidylate synthase enzyme of T. cruzi and the crystal structure of the ternary enzyme:cofactor:inhibitor complex was determined. Molecular docking was used to analyze the potential interactions of all inhibitors with T. cruzi DHFR and human DHFR. Inhibitory activities of these compounds are discussed in the light of enzyme-ligand interactions. Binding affinities of each inhibitor for the respective enzymes were calculated based on the experimental or docked binding mode. An estimated 60-70% of the total binding energy is contributed by the 2,4-diaminoquinazoline scaffold.
	PMID: 20452776 [PubMed - indexed for MEDLINE]
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