Impact of the New Hybrids of Glycoconjugate‐1,2,3‐triazole Tethered with 1,2,4‐oxadiazole as Promising Anticancer, Antimicrobial, and Antimalarial Agents

Abstract

Abstract Click chemistry is adopted to synthesize the new hybrids of glycoconjugates‐1,2,3‐triazole tethered with 1,2,4‐oxadiazole 5a–c in a single step. Structure identification of the synthesized compounds was elucidated from their spectral analyses. The antiproliferative activity of the developed glycoconjugates was evaluated against MCF‐7 breast carcinoma, HeLa cervical carcinoma, and the normal Vero cell lines. Additionally, the antimicrobial and antimalarial potentials of the new glycoconjugates were estimated in vitro against a plethora of Gram‐negative and Gram‐positive bacteria, fungi, and Plasmodium chabaudi . The glycoconjugate 5b (benzyl substituted) exhibited 2.07‐fold more cytotoxic activity than doxorubicin against the MCF‐7 cell line. Regarding the HeLa cervical cell line, the glycoconjugate 5b (benzyl substituted) showed comparable potency to doxorubicin. Glycoconjugates 5a–c displayed significant inhibition against investigated bacterial and fungal strains. The glycoconjugate 5c (4‐trifluoromethylphenyl substituted) exhibited excellent antibacterial activity with 30.6 mm ZOI and MIC value of 1.95 µg/mL against Enterococcus faecalis and 29.8 mm ZOI and MIC value of 1.73 µg/mL against Staphylococcus aureus . The three glycoconjugates showed significant antimalarial activity. The glycoconjugate 5a (phenyl substituted) inhibited the parasite's growth by 94.6% at a concentration of 10 µg/mL, The results revealed the synthesized glycoconjugates as interesting therapeutic candidates for further development.