synthesis and anti-intestinal nematode activity of variously substituted benzonaphthyridine derivatives合成和anti-intestinal线虫的活性不同取代benzonaphthyridine衍生品.pdf

Molecules 2011, 16, 1593-1602; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis and Anti-Intestinal Nematode Activity of Variously Substituted Benzonaphthyridine Derivatives Li-Ping Duan, Ai-Dan Wen, Ning-Bo Wu, Yi Tao and Hao-Bing Zhang * Key Laboratory of Parasitology and Vector Biology at National Institute of Parasitic Diseases, Chinese Center for Disease Control and Prevention, WHO Collaborating Centre for Malaria, Schistosomiasis, and Filariasis, National Institute of Parasitic Diseases, Shanghai 200025, China * Author to whom correspondence should be addressed; E-Mail: zhanghaobing@. Received: 21 December 2010; in revised form: 18 January 2011 / Accepted: 25 January 2011 / Published: 14 February 2011 Abstract: A series of benzonaphthyridine derivatives bearing the C=N linkage moiety were designed and synthesized. The structures of all the newly synthesized compounds were identified by elemental analysis, 1H-NMR, 13C-NMR and MS. Their anti-intestinal nematode activities against Nippostrongylus brazilliensis were evaluated in vivo by an oral route in male rats. Among these compounds, at concentrations of 10 mg/kg of rat, the compound 7-chloro-2-methoxy-10-(4-(4′-(1H-indol-5′-yl)methylene)aminophenyl)- amino-benzo[b][1,5] naphthyridine (4n) produced the highest activity, with 80.2% deparasitization. These compounds may find usefulness in the discovery and dev