8-Quinolinamines conjugated with amino acids are exhibiting potent blood-schizontocidal antimalarial activities |
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Authors: | Vangapandu Suryanarayana Sachdeva Sandeep Jain Meenakshi Singh Savita Singh Prati Pal Kaul Chaman Lal Jain Rahul |
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Institution: | National Institute of Pharmaceutical Education and Research, Sector 67, S.A.S. Nagar, Punjab, 160 062, India. |
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Abstract: | Alanine, lysine, ornithine and valine conjugated to primaquine and other 8-quinolinamine antimalarials were prepared for blood-schizontocidal antimalarial activity evaluation. The analogues were examined in vivo against Plasmodium berghei (drug-sensitive strain) and Plasmodium yoelii nigeriensis (highly virulent multi-drug-resistant strain) infected mice models. N(1)-4-(5-Butoxy-4-ethyl-6-methoxy-8-quinolylamino)pentyl]-(2S)-2,6-diaminohexanamide (20) which showed curative activity at 5mg/kg in the P. berghei test emerged as the most effective compound. N(1)-4-(4-Ethyl-5-hexoxy-6-methoxy-8-quinolylamino)pentyl]-(2S)-2,6-diaminohexanamide (22) exhibited curative activity at 50mg/kg against P. yoelii nigeriensis in mice and emerged as the most potent analogue against multi-drug resistant strain. The results of this study represent development of highly potent 8-quinolinamines for antimalarial drug development. |
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