d‑Glucose-Conjugated Benzo[d]thiazole-thiazolidin-4-one Hybrids: Design and Synthesis as Multitarget Anti-Alzheimer Compounds.
| Title: | d‑Glucose-Conjugated Benzo[d]thiazole-thiazolidin-4-one Hybrids: Design and Synthesis as Multitarget Anti-Alzheimer Compounds. |
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| Authors: | Thanh ND; Faculty of Chemistry, VNU University of Science (Vietnam National University, Ha Noi), 19 Le Thanh Tong, Hoan Kiem, Ha Noi 10000, Viet Nam.; Toan VN; Faculty of Chemistry, VNU University of Science (Vietnam National University, Ha Noi), 19 Le Thanh Tong, Hoan Kiem, Ha Noi 10000, Viet Nam.; Institute of Science and Technology, Ministry of Public Security of Vietnam, 47 Pham Van Dong, Cau Giay, Ha Noi 10000, Viet Nam.; Hai DS; Faculty of Chemistry, VNU University of Science (Vietnam National University, Ha Noi), 19 Le Thanh Tong, Hoan Kiem, Ha Noi 10000, Viet Nam.; Institute of New Technology, Military Institute of Science and Technology, 17 Hoang Sam, Cau Giay, Ha Noi 10000, Viet Nam.; Tri NM; Faculty of Chemistry, VNU University of Science (Vietnam National University, Ha Noi), 19 Le Thanh Tong, Hoan Kiem, Ha Noi 10000, Viet Nam.; Institute of Science and Technology, Ministry of Public Security of Vietnam, 47 Pham Van Dong, Cau Giay, Ha Noi 10000, Viet Nam.; Toan DN; Faculty of Chemistry, VNU University of Science (Vietnam National University, Ha Noi), 19 Le Thanh Tong, Hoan Kiem, Ha Noi 10000, Viet Nam.; Faculty of Chemistry, Thai Nguyen University of Education, 20 Luong Ngoc Quyen, Thai Nguyen 10000, Viet Nam.; Trang VM; Faculty of Chemistry, VNU University of Science (Vietnam National University, Ha Noi), 19 Le Thanh Tong, Hoan Kiem, Ha Noi 10000, Viet Nam.; VNU University of Education, Vietnam National University, Hanoi, 144 Xuan Thuy, Cau Giay, Ha Noi 10000, Viet Nam. |
| Source: | ACS medicinal chemistry letters [ACS Med Chem Lett] 2025 May 05; Vol. 16 (6), pp. 1024-1030. Date of Electronic Publication: 2025 May 05 (Print Publication: 2025). |
| Publication Type: | Journal Article |
| Language: | English |
| Journal Info: | Publisher: American Chemical Society Country of Publication: United States NLM ID: 101521073 Publication Model: eCollection Cited Medium: Print ISSN: 1948-5875 (Print) Linking ISSN: 19485875 NLM ISO Abbreviation: ACS Med Chem Lett Subsets: PubMed not MEDLINE |
| Imprint Name(s): | Original Publication: Washington, D.C. : American Chemical Society |
| 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.; (© 2025 American Chemical Society.) |
| Contributed Indexing: | Keywords: 2-iminothiazolidine-4-ones; AChE; BChE; MAOs; benzothiazole; d-glucose |
| Entry Date(s): | Date Created: 20250618 Latest Revision: 20250708 |
| Update Code: | 20260130 |
| PubMed Central ID: | PMC12169603 |
| DOI: | 10.1021/acsmedchemlett.5c00064 |
| PMID: | 40529084 |
| Database: | MEDLINE |
Journal Article