Synthesis, in vitro А-Glucosidase, and acetylcholinesterase inhibitory activities of novel Indol-Fused Pyrano[2,3-D]Pyrimidine compounds

被引：4

作者：

Nguyen, Ha Thanh ^{[1
,2
]}

Tuan, Anh Nguyen ^{[1
]}

Thi, Tuyet Anh Dang ^{[1
,2
]}

Van, Ket Tran ^{[2
,3
]}

Giang, Le-Nhat-Thuy ^{[1
,2
]}

Thi, Phuong Hoang ^{[1
]}

Thi, Quynh Giang Nguyen ^{[1
,2
]}

Thi, Cham Ba ^{[1
,2
]}

Quang, Hung Tran ^{[1
,2
]}

Nguyen, Tuyen Van ^{[1
,2
]}

机构：

[1] Vietnam Acad Sci & Technol VAST, Inst Chem, 18 Hoang Quoc Viet, Hanoi, Vietnam

[2] Grad Univ Sci & Technol, VAST, 18 Hoang Quoc Viet, Hanoi, Vietnam

[3] Mil Technol Acad, 236 Hoang Quoc Viet, Hanoi, Vietnam

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2024年 / 98卷

关键词：

Indol-fused pyrano[2; d; pyrimidine; Diabetes mellitus; alpha-glucosidase inhibitors; AChE inhibitors; Multicomponent-component reaction; BIOLOGICAL EVALUATION; COMPLICATIONS TRIAL/EPIDEMIOLOGY; MULTICOMPONENT SYNTHESIS; DIABETES INTERVENTIONS; ALPHA-AMYLASE; DERIVATIVES; DESIGN;

D O I：

10.1016/j.bmcl.2023.129566

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页数：6

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