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Synthesis and in vitro bio-activity evaluation of N4-benzyl substituted 5-chloroisatin-3-thiosemicarbazones as urease and glycation inhibitors

Humayun Pervez, Nazia Khan, Jamshed Iqbal, Sumera Zaib, Muhammad Yaqub, Muhammad Moazzam Naseer


A series of fifteen N4-benzyl substituted 5-chloroisatin-3-thiosemicarbazones 5ao were synthesized and screened mainly for their antiurease and antiglycation effects. Lemna aequinocitalis growth and Artemia salina assays were carried out to determine their phytotoxicity and cytotoxicity potential. All the compounds proved to be extremely effective urease inhibitors, demonstrating enzyme inhibition much better than the reference inhibitor, thiourea (IC50 values 1.31 ± 0.06 to 3.24 ± 0.15 vs. 22.3 ± 1.12 μM). On the other hand, eight out of fifteen compounds tested, i.e. 5b, 5c, 5hk, 5m and 5n were found to be potent glycation inhibitors. Of these, five viz. 5c, 5hj and 5n proved to be exceedingly efficient, displaying glycation inhibition greater than the reference inhibitor, rutin (IC50 values 114.51 ± 1.08 to 229.94 ± 3.40 vs. 294.5 ± 1.5 μM).


5-Chloroisatin; Glycation inhibition; Heterocyclics; Schiff bases; Thiosemicarbazones; Urease inhibition

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