Synthesis of Novel Valine-based Dipeptide Carboxamide Bearing Benzene Sulfonamide Moiety as Antimalarial Agent

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James. A. Ezugwu
Uchechukwu C. Okoro
Mercy A. Ezeokonkwo
China Raju Bhimapaka

Abstract

Communication in Physical Sciences 2020, 5(2): 176-197


Authors: James A. Ezugwu, *Ucheckukwu. C. Okoro, Mercy A. Ezeokonkwo, and China R. Bhimapaka


Received 15 April 2020/Accepted 14 May 2020


 


Syntheses of eleven novel Valine-based dipeptide carboxamide derivatives bearing benzensulphonamide are reported. These were achieved by facile amidation reaction of p- substituted benzenesulphonamoyl alkanamides with 2-amino-4-methyl-N-substituted phenyl butanamide using classical peptide coupling reagents. The chemical structures of the synthesized compounds were established by 1H-NMR, 13C-NMR, ESI- HRMS, and FT-IR spectroscopic techniques. The synthesized compounds were evaluated for in vivo antimalarial against P. berghei. Haematological analysis was also evaluated on the synthesized compounds. At 50mg/kg body weight, the compounds 8e, 8g, 8i, 8k, 8d and 8h inhibited the multiplication of the parasite by 46-71% on day seven of post-treatment exposure comparable to the 67% reduction with artemisinin.

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Articles
Author Biographies

James. A. Ezugwu, University of Nigeria, Nsukka, 410001, Enugu State, Nigeria

Department of Pure and Industrial Chemistry

Uchechukwu C. Okoro, University of Nigeria, Nsukka, 410001, Enugu State, Nigeria

Department of Pure and Industrial Chemistry

Mercy A. Ezeokonkwo, University of Nigeria, Nsukka, 410001, Enugu State, Nigeria

Department of Pure and Industrial Chemistry

China Raju Bhimapaka, Division, CSIR-India Institute of Chemical Technology, Hyderabad, Telangana, India

Organic synthesis and process chemistry

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