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Design, Synthesis, In Silico Testing, and In Vitro Evaluation of Thiazolidinone-Based Benzothiazole Derivatives as Inhibitors of α-Amylase and α-Glucosidase.

ABSTRACT: In this study, a stepwise reaction afforded thiazolidinone-based benzothiazole derivatives 1-15, and the synthesized derivatives were then screened for biological significance and found to be the leading candidates against α-amylase and α-glucosidase enzymes. Almost all derivatives showed excellent to good activity ranging against α-amylase, IC50 = 2.10 ± 0.70 to 37.50 ± 0.70 μM, and α-glucosidase, IC50 = 3.20 ± 0.05 to 39.40 ± 0.80 μM. Some analogues such as 4 (2.40 ± 0.70 and 3.50 ± 0.70 μM), 5 (2.30 ± 0.05 and 4.80 ± 0.10 μM), and 6 (2.10 ± 0.70 and 3.20 ± 0.70 μM) were found with folds better activity than that of the standard drug acarbose (9.10 ± 0.10 and 10.70 ± 0.10 μM), respectively. Moreover, the structure-activity relationship (SAR) has been established for all compounds. A molecular docking study has been carried out to explore the binding interactions against α-amylase and α-glucosidase enzymes.

SUBMITTER: Khan S 

PROVIDER: S-EPMC9610606 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature

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Design, Synthesis, In Silico Testing, and In Vitro Evaluation of Thiazolidinone-Based Benzothiazole Derivatives as Inhibitors of α-Amylase and α-Glucosidase.

Khan Shoaib S   Iqbal Shahid S   Iqbal Shahid S   Khan Marwa M   Rehman Wajid W   Shah Mazloom M   Hussain Rafaqat R   Rasheed Liaqat L   Khan Yousaf Y   Dera Ayed A AA   Pashameah Rami Adel RA   Alzahrani Eman E   Farouk Abd-ElAziem AE  

Pharmaceuticals (Basel, Switzerland) 20220920 10

In this study, a stepwise reaction afforded thiazolidinone-based benzothiazole derivatives <b>1</b>-<b>15</b>, and the synthesized derivatives were then screened for biological significance and found to be the leading candidates against α-amylase and α-glucosidase enzymes. Almost all derivatives showed excellent to good activity ranging against α-amylase, IC50 = 2.10 ± 0.70 to 37.50 ± 0.70 μM, and α-glucosidase, IC50 = 3.20 ± 0.05 to 39.40 ± 0.80 μM. Some analogues such as <b>4</b> (2.40 ± 0.70  ...[more]

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