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Molecules 2011, 16(2), 1593-1602; doi:10.3390/molecules16021593

Synthesis and Anti-Intestinal Nematode Activity of Variously Substituted Benzonaphthyridine Derivatives

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
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Author to whom correspondence should be addressed.
Received: 21 December 2010 / Revised: 18 January 2011 / Accepted: 25 January 2011 / Published: 14 February 2011
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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 development of new anti-intestinal drugs.
Keywords: benzonaphthyridine; C=N linkage; Nippostrongylus brazilliensis benzonaphthyridine; C=N linkage; Nippostrongylus brazilliensis
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Duan, L.-P.; Wen, A.-D.; Wu, N.-B.; Tao, Y.; Zhang, H.-B. Synthesis and Anti-Intestinal Nematode Activity of Variously Substituted Benzonaphthyridine Derivatives. Molecules 2011, 16, 1593-1602.

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