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Research Paper

Synthesis and characterisation of thiobarbituric acid enamine derivatives, and evaluation of their α-glucosidase inhibitory and anti-glycation activity

, , , , , , , , , , , & show all
Pages 692-701 | Received 26 Dec 2019, Accepted 25 Feb 2020, Published online: 11 Mar 2020

Figures & data

Scheme 1. Synthetic route for the synthesis of 3a–k, 4a–d, 5, and 6.

Scheme 1. Synthetic route for the synthesis of 3a–k, 4a–d, 5, and 6.

Table 1. Result of in vitro α-glucosidase enzyme inhibitor and anti-glycation activities.

Figure 1. Lead compounds 3i and 6 with promising activities.

Figure 1. Lead compounds 3i and 6 with promising activities.

Figure 2. Binding mode of thiobarbituric acid derivatives into the α-glucosidase binding cavity. For clarity, acarbose is shown in cyan. Compounds 3g, 3i, and 3j are indicated in pink, and 5 in green. The part of the enzyme in the background is shown as surface model.

Figure 2. Binding mode of thiobarbituric acid derivatives into the α-glucosidase binding cavity. For clarity, acarbose is shown in cyan. Compounds 3g, 3i, and 3j are indicated in pink, and 5 in green. The part of the enzyme in the background is shown as surface model.

Figure 3. Interactions of acarbose with crucial residues of α-glucosidase.

Figure 3. Interactions of acarbose with crucial residues of α-glucosidase.

Figure 4. The predicted binding interactions of compounds 3g, 3i, 3j, and 5 in the active site.

Figure 4. The predicted binding interactions of compounds 3g, 3i, 3j, and 5 in the active site.
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Supplemental Material

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