Synthesis and anti-intestinal nematode activity of variously substituted benzonaphthyridine derivatives.

Molecules

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.

Published: February 2011

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.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6259630PMC
http://dx.doi.org/10.3390/molecules16021593DOI Listing

Publication Analysis

Top Keywords

anti-intestinal nematode
8
benzonaphthyridine derivatives
8
synthesis anti-intestinal
4
nematode activity
4
activity variously
4
variously substituted
4
substituted benzonaphthyridine
4
derivatives series
4
series benzonaphthyridine
4
derivatives bearing
4

Similar Publications

Efficacy and safety of praziquantel, tribendimidine and mebendazole in patients with co-infection of Clonorchis sinensis and other helminths.

PLoS Negl Trop Dis

August 2014

National Institute of Parasitic Diseases, Chinese Center for Disease Control and Prevention, Shanghai, People's Republic of China; WHO Collaborative Center for Malaria, Schistosomiasis and Filariasis, Key Laboratory of Parasite and Vector Biology, Ministry of Health, Shanghai, People's Republic of China.

Background: Both tribendimidine and mebendazole are broad-spectrum drugs for anti-intestinal nematodes. We aim to assess the efficacy and safety of tribendimidine and mebendazole in patients with co-infection of Clonorchis sinensis and other helminths.

Method: We performed a randomized open-label trial in Qiyang, People's Republic of China.

View Article and Find Full Text PDF

Synthesis and anti-intestinal nematode activity of variously substituted benzonaphthyridine derivatives.

Molecules

February 2011

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.

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.

View Article and Find Full Text PDF

A series of 1-acyl-3-(2'-aminophenyl) thiourea derivatives were designed and synthesized. The structures of all the newly synthesized compounds were identified by IR, elemental analysis, ¹H-NMR and ¹³C-NMR. Their anti-intestinal nematode activities against Nippostrongylus brazilliensis were evaluated in rats by an oral route.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!