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synthesis of novel hybrid molecules from precursors with known antiparasitic activity合成新型混合分子从前体与已知抗寄生物的活动
Molecules 2009, 14, 1483-1494; doi: 10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis of Novel Hybrid Molecules from Precursors With Known Antiparasitic Activity Haythem A. Saadeh 1,*, Ibrahim M. Mosleh 2 and Mohammad S. Mubarak 1,* 1 Chemistry Department, Faculty of Science, University of Jordan, Amman 11942, Jordan 2 Department of Biological Sciences, Faculty of Science, University of Jordan, Amman 11942, Jordan * Authors to whom correspondence should be addressed; E-mail: h.saadeh@.jo (H-A.S.), mmubarak@.jo (M-S.M.); Tel.: +962 6 5355000 ext. 22159 (H-A.S.), +962 6 5355000 ext. 22168 (M-S.M.); Fax: +962 6 5348932 (H-A.S.), +962 6 5348932 (M-S.M.). Received: 4 March 2009; in revised form: 2 April 2009 / Accepted: 7 April 2009 / Published: 9 April 2009 Abstract: Three novel new compounds derived from antiparasitic precursors have been synthesized and tested for their antiamoebic and antigiardial activities. The condensation of 2- (2-methyl-5-1H-nitroimidazolyl)ethylamine (6) with 5-nitro-2-furylacrylic acid (7) gave 3-(5- nitrofuran-2-yl)-N-[2-(5-nitroimidazol-1-yl)ethyl]acrylamide (8). Condensation of 7 with 7- chloro-4-(piperazin-1-yl)quinoline (9) afforded 1-[4-(7-chloroquinolin-4-yl)piperazin-1-yl)-3- (5-nitrofuran-2-yl)propenone as a mixture of two isomers; 10-a (the E-isomer) and 10-b (the Z-isomer). In addition, the reaction of 9 with 1-(2-bromoethyl)-2-methyl-5-nitroimidazole (11) in the presence of K2CO3 and
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