In the present study, a series of 3-(5-cyclohexyl-1,3,4-oxadiazol-2-yl)-N-substituted aniline have been synthesized by multistep reaction scheme. Benzohydrazide was used as the starting material. The structures of all synthesized compounds are characterized and confirmed by FT-IR, H and C NMR and mass spectral studies with the intention of developing the novel biologically active compounds. All title synthetic compounds were screened for their antidiabetic, anti-inflammatory and anticancer activities.

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<p class="Abstract">Six compounds of benzothiazole derivatives were synthesized, and structures were confirmed by FT-IR, ¹H-NMR, ¹³C-NMR and LC-MS. The resulting compounds were evaluated for anti-plasmodial activity against <em>Plasmodium falciparum</em> by Giemsa stain. Among them the compounds 3b and 4 showed potent anti-plasmodial activity against <em>P. falciparum</em>. The com-pounds 3a, 5a, 5b also showed moderate anti-plasmodial activity. The structure-activity relationships of benzothiazole derivatives also discussed which were useful for exploring and developing benzothiazole derivatives as novel anti-malarial drugs.</p><p> </p>