New thiazole-based thiazolidinone derivatives: Synthesis, in vitro α-amylase, α-glucosidase activities and silico molecular docking study

被引：36

作者：

Khan, Shoaib ^{[1
]}

Ullah, Hayat ^{[2
]}

Rahim, Fazal ^{[1
]}

Taha, Muhammad ^{[3
]}

Hussain, Rafaqat ^{[1
]}

Khan, Muhammad Saleem ^{[4
]}

Ali, Hamid ^{[1
]}

Khan, Misbah Ullah ^{[5
]}

Shah, Syed Adnan Ali ^{[6
,7
]}

Khan, Khalid Mohammed ^{[8
]}

机构：

[1] Hazara Univ, Dept Chem, Mansehra 21120, KP, Pakistan

[2] Univ Okara, Dept Chem, Okara 56130, Pakistan

[3] Imam Abdulrahman Bin Faisal Univ, Inst Res & Med Consultat IRMC, Dept Clin Pharm, POB 1982, Dammam 31441, Saudi Arabia

[4] Univ Okara, Fac Life Sci, Dept Zool, Okara 56130, Pakistan

[5] Univ Okara, Ctr Nanosci, Okara 56130, Pakistan

[6] Univ Teknol MARA, Fac Pharm, Cawangan Selangor Kampus Puncak Alam, Bandar Puncak Alam 42300, Selangor, Malaysia

[7] Univ Teknol MARA, Atta ur Rahman Inst Nat Prod Discovery AuRIns, Cawangan Selangor Kampus Puncak Alam, Bandar Puncak Alam 42300, Selangor, Malaysia

[8] Univ Karachi, HEJ Res Inst Chem, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan

来源：

CHEMICAL DATA COLLECTIONS | 2022年 / 42卷

关键词：

Synthesis; alpha-glucosidase; alpha-amylase; Thiazolidinone; Molecular docking; NONLINEAR-OPTICAL PROPERTIES; INHIBITORS; ANALOGS;

D O I：

10.1016/j.cdc.2022.100967

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of thiazole-based thiazolidinone derivatives (1-20) have been synthesized and evaluated against alpha-glucosidase and alpha-amylase enzymes. All derivatives showed good alpha-glucosidase activity having IC50 values ranging from 2.40 +/- 0.10 to 31.40 +/- 0.90 mu M and for alpha-amylase having IC50 values ranging from 1.80 +/- 0.05 to 27.60 +/- 0.80 mu M as compared to standard drug acarbose (IC50 = 9.80 +/- 0.20 mu M & 10.30 +/- 0.20 mu M respectively). Analogues 5 (IC50 = 1.80 +/- 0.05 & 2.40 +/- 0.10 mu M) and 10 (IC50 = 2.10 +/- 0.10 & 3.60 +/- 0.20 mu M) showed potent inhibitory potential against both alpha-glucosidase and alpha-amylase enzymes. The structure-activity relationship has been established which mainly depends upon the number, nature, position, and electron donating/withdrawing effect of substituent/s on the aryl ring. A molecular docking study was also carried out to determine the binding interactions of the most potent analogues with the active site of the enzyme.

引用

页数：16

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