Discovery of a novel lead structure for anti-malarials.

作者: Jochen Wiesner , Pia Wißner , Hans-Martin Dahse , Hassan Jomaa , Martin Schlitzer

DOI: 10.1016/S0968-0896(00)00296-0

关键词:

摘要: From a library of 61 compounds available from former studies 2,5-bis-acylaminobenzophenone 7p was identified as lead structure for novel class anti-malaria agents active against multi-resistant Plasmodium falciparum strain Dd2. Some structural modifications this initial demonstrated the potential further improvement anti-plasmodial activity anti-malarials.

参考文章(10)
W Trager, J. Jensen, Human malaria parasites in continuous culture Science. ,vol. 193, pp. 673- 675 ,(1976) , 10.1126/SCIENCE.781840
Martin Schlitzer, Markus Böhm, Isabel Sattler, Hans-Martin Dahse, Design, synthesis and early structure-activity relationship of farnesyltransferase inhibitors which mimic both the peptidic and the prenylic substrate. Bioorganic & Medicinal Chemistry. ,vol. 8, pp. 1991- 2006 ,(2000) , 10.1016/S0968-0896(00)00138-3
Martin Schlitzer, Isabel Sattler, Non-thiol farnesyltransferase inhibitors: the concept of benzophenone-based bisubstrate analogue farnesyltransferase inhibitors. European Journal of Medicinal Chemistry. ,vol. 35, pp. 721- 726 ,(2000) , 10.1016/S0223-5234(00)00162-8
R E Desjardins, C J Canfield, J D Haynes, J D Chulay, Quantitative assessment of antimalarial activity in vitro by a semiautomated microdilution technique. Antimicrobial Agents and Chemotherapy. ,vol. 16, pp. 710- 718 ,(1979) , 10.1128/AAC.16.6.710
Kenneth Kaushansky, A New Year Greeting From a New Editor Blood. ,vol. 91, pp. 1- 2 ,(1998) , 10.1182/BLOOD.V91.1.1.1_1_2
Dyann F. Wirth, Chapter 33. Malaria: A Third World Disease in Need of First World Drug Development Annual Reports in Medicinal Chemistry. ,vol. 34, pp. 349- 358 ,(1999) , 10.1016/S0065-7743(08)60595-3
Marie L. Ancelin, Michèle Calas, Jacques Bompart, Gérard Cordina, Dominique Martin, Mohammed Ben Bari, Taı̈b Jei, Pierre Druilhe, Henri J. Vial, Antimalarial activity of 77 phospholipid polar head analogs: close correlation between inhibition of phospholipid metabolism and in vitro Plasmodium falciparum growth. Blood. ,vol. 91, pp. 1426- 1437 ,(1998) , 10.1182/BLOOD.V91.4.1426