title: Synthesis and anti-intestinal nematode activity of variously substituted benzonaphthyridine derivatives.
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.
authors.affiliation: 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.
authors.forename: Li-Ping
authors.initials: LP
authors.lastname: Duan
authors.forename: Ai-Dan
authors.initials: AD
authors.lastname: Wen
authors.forename: Ning-Bo
authors.initials: NB
authors.lastname: Wu
authors.forename: Yi
authors.initials: Y
authors.lastname: Tao
authors.forename: Hao-Bing
authors.initials: HB
authors.lastname: Zhang
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000969:Antinematodal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D007422:Intestines / Q000187:drug effects / Q000469:parasitology*; D008297:Male; D013058:Mass Spectrometry; D015394:Molecular Structure; D009287:Naphthyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D009559:Nippostrongylus / Q000187:drug effects*; D019906:Nuclear Magnetic Resonance, Biomolecular; D051381:Rats
chemical_list: D000962:Antimalarials; D000969:Antinematodal Agents; D009287:Naphthyridines