| Title : Synthesis, in Vitro -Glucosidase, and Acetylcholinesterase Inhibitory Activities of Novel Indol-Fused Pyrano[2,3-D]Pyrimidine Compounds - Nguyen_2023_Bioorg.Med.Chem.Lett__129566 |
| Author(s) : Nguyen HT , Tuan AN , Thi TAD , Van KT , Le-Nhat-Thuy G , Thi PH , Thi QGN , Thi CB , Quang HT , Van Nguyen T |
| Ref : Bioorganic & Medicinal Chemistry Lett , :129566 , 2023 |
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Abstract :
In this study, new indol-fused pyrano[2,3-d]pyrimidines were designed and synthesized. These products were obtained in moderate to good yields and their structures were assigned by NMR, MS, and IR analysis. Afterwards, the biological important of the products was highlighted by evaluating in vitro for alpha-glucosidase inhibitory activity as well as acetylcholinesterase (AChE) inhibitory activity. Eleven products revealed substantial inhibitory activity against alpha-glucosidase enzyme, among which, two most potent products 11d,e were approximately 93-fold more potent than acarbose as a standard antidiabetic drug. Besides that, product 11k exhibited good AChE inhibition. The substituents on the 5-phenyl ring, attached to the pyran ring, played a critical role in inhibitory activities. The biological potencies have provided an opportunity to further investigations of indol-fused pyrano[2,3-d]pyrimidines as potential anti-diabetic agents. |
| PubMedSearch : Nguyen_2023_Bioorg.Med.Chem.Lett__129566 |
| PubMedID: 38008338 |
Nguyen HT, Tuan AN, Thi TAD, Van KT, Le-Nhat-Thuy G, Thi PH, Thi QGN, Thi CB, Quang HT, Van Nguyen T (2023)
Synthesis, in Vitro -Glucosidase, and Acetylcholinesterase Inhibitory Activities of Novel Indol-Fused Pyrano[2,3-D]Pyrimidine Compounds
Bioorganic & Medicinal Chemistry Lett
:129566
Nguyen HT, Tuan AN, Thi TAD, Van KT, Le-Nhat-Thuy G, Thi PH, Thi QGN, Thi CB, Quang HT, Van Nguyen T (2023)
Bioorganic & Medicinal Chemistry Lett
:129566