نتایج جستجو برای: pteridine reductase 1

تعداد نتایج: 2784388  

2011
Daniel Spinks Han B Ong Chidochangu P Mpamhanga Emma J Shanks David A Robinson Iain T Collie Kevin D Read Julie A Frearson Paul G Wyatt Ruth Brenk Alan H Fairlamb Ian H Gilbert

Genetic studies indicate that the enzyme pteridine reductase 1 (PTR1) is essential for the survival of the protozoan parasite Trypanosoma brucei. Herein, we describe the development and optimisation of a novel series of PTR1 inhibitors, based on benzo[d]imidazol-2-amine derivatives. Data are reported on 33 compounds. This series was initially discovered by a virtual screening campaign (J. Med. ...

Journal: :Indian Journal of Pharmaceutical Education and Research 2018

2017
Pasquale Linciano Alice Dawson Ina Pöhner David M. Costa Monica S. Sá Anabela Cordeiro-da-Silva Rosaria Luciani Sheraz Gul Gesa Witt Bernhard Ellinger Maria Kuzikov Philip Gribbon Jeanette Reinshagen Markus Wolf Birte Behrens Véronique Hannaert Paul A. M. Michels Erika Nerini Cecilia Pozzi Flavio di Pisa Giacomo Landi Nuno Santarem Stefania Ferrari Puneet Saxena Sandra Lazzari Giuseppe Cannazza Lucio H. Freitas-Junior Carolina B. Moraes Bruno S. Pascoalino Laura M. Alcântara Claudia P. Bertolacini Vanessa Fontana Ulrike Wittig Wolfgang Müller Rebecca C. Wade William N. Hunter Stefano Mangani Luca Costantino Maria P. Costi

Pteridine reductase-1 (PTR1) is a promising drug target for the treatment of trypanosomiasis. We investigated the potential of a previously identified class of thiadiazole inhibitors of Leishmania major PTR1 for activity against Trypanosoma brucei (Tb). We solved crystal structures of several TbPTR1-inhibitor complexes to guide the structure-based design of new thiadiazole derivatives. Subseque...

2012
Alexandra Kirsch Sharon Burgmayer

The Synthesis and Characterization of Ru(bpy)2(L-pteridine) and Ru(phen)2(L-pteridine) complexes Ruthenium (II) polypyridyl complexes are very important biochemical compounds because of their interactions with DNA. In this study, these complexes are analyzed to understand how their physical properties, chemical properties, and interactions with DNA are affected by structural differences of the ...

Journal: :Experimental parasitology 1997
Hardy Matthews Nare Beverley

The study of antifolate-resistant mutants of the protozoan parasite Leishmania has provided useful information about genetic processes such as gene amplification and mutation and knowledge of the unique features of the pteridine metabolic pathway in this primitive eukaryote. The novel bifunctional dihydrofolate reductase-thymidylate synthase (DHFR-TS) is an essential enzyme, yet most DHFR-TS in...

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