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Titolo:
The structure-based design and synthesis of selective inhibitors of Trypanosoma cruzi dihydrofolate reductase
Autore:
Zuccotto, F; Brun, R; Pacanowska, DG; Perez, LMR; Gilbert, IH;
Indirizzi:
Cardiff Univ, Welsh Sch Pharm, Cardiff CF1 3XF, S Glam, Wales Cardiff Univ Cardiff S Glam Wales CF1 3XF Cardiff CF1 3XF, S Glam, Wales Swiss Trop Inst, CH-4002 Basel, Switzerland Swiss Trop Inst Basel Switzerland CH-4002 st, CH-4002 Basel, Switzerland Consejo Suer Invest Cient, Inst Parasitol & Biomed, Granada 18001, Spain Consejo Suer Invest Cient Granada Spain 18001 omed, Granada 18001, Spain
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
fascicolo: 10, volume: 9, anno: 1999,
pagine: 1463 - 1468
SICI:
0960-894X(19990517)9:10<1463:TSDASO>2.0.ZU;2-O
Fonte:
ISI
Lingua:
ENG
Soggetto:
THYMIDYLATE SYNTHASE; METHOTREXATE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
9
Recensione:
Indirizzi per estratti:
Indirizzo: Gilbert, IH Cardiff1Univ, Welsh Sch Pharm, Redwood Bldg,King Edward VII Ave, Cardiff CF Cardiff Univ Redwood Bldg,King Edward VII Ave Cardiff S Glam Wales CF1 3XF
Citazione:
F. Zuccotto et al., "The structure-based design and synthesis of selective inhibitors of Trypanosoma cruzi dihydrofolate reductase", BIOORG MED, 9(10), 1999, pp. 1463-1468

Abstract

This paper describes the design and synthesis of potential inhibitors of Trypanosoma cruzi dihydrofolate reductase using a structure-based approach. A model of the structure of the T cruzi enzyme was compared with the structure of the human enzyme. The differences were used to design modifications of methotrexate to produce compounds which should be selective for the parasite enzyme. The derivatives of methotrexate were synthesised and tested against the enzyme and intact parasites. (C) 1999 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 23/01/21 alle ore 03:45:00