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. 2025 May 5;16(6):1024-1030.
doi: 10.1021/acsmedchemlett.5c00064. eCollection 2025 Jun 12.

d‑Glucose-Conjugated Benzo[ d]thiazole-thiazolidin-4-one Hybrids: Design and Synthesis as Multitarget Anti-Alzheimer Compounds

Nguyen Dinh Thanh  1 , Vu Ngoc Toan  1   2 , Do Son Hai  1   3 , Nguyen Minh Tri  1   2 , Duong Ngoc Toan  1   4 , Vu Minh Trang  1   5
Affiliations

d‑Glucose-Conjugated Benzo[ d]thiazole-thiazolidin-4-one Hybrids: Design and Synthesis as Multitarget Anti-Alzheimer Compounds

Nguyen Dinh Thanh et al. ACS Med Chem Lett. .

Abstract

A new series of d-glucose-conjugated 2,3-thiazoline-benzo-[d]-thiazole hybrid compounds 8a-k were synthesized from reaction of the corresponding thioureas 7a-k and ethyl bromoacetate in the presence of sodium acetate in chloroform. The evaluations for anti-Alzheimer activity showed that some compounds exhibited remarkable inhibitory activity against AChE and BChE as well as against MAO-A and MAO-B enzymes. The orders of inhibition for each enzyme of these compounds were as follows: 8j > 8h (against AChE), 8k > 8b (against BChE), 8k > 8g > 8f (against MAO-A), and 8e > 8c (against MAO-B). Compound 8k was an inhibitor of interest due to its potent or good activity against the two studied enzymes BChE and MAO-B, respectively. Compounds 8j (against AChE) and 8k (against (BChE) had a competitive type with K i constants of 16.93 and 17.09 nM, respectively. The most potential compounds 8c, 8j, and 8k were not cytotoxic on 3T3 cells and had high levels of safety.

Keywords: 2-iminothiazolidine-4-ones; AChE; BChE; MAOs; benzothiazole; d-glucose.

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