Synthesis and biological evaluation of indole derivatives containing thiazolidine-2,4-dione as α-glucosidase inhibitors with antidiabetic activity

European Journal of Medicinal Chemistry, Journal Year: 2023, Volume and Issue: 264, P. 115957 - 115957

Published: Nov. 24, 2023

Language: Английский

---

Investigation on the inhibition mechanism and binding behavior of cryptolepine to α-glucosidase and its hypoglycemic activity by multi-spectroscopic method

Journal of Luminescence, Journal Year: 2024, Volume and Issue: 269, P. 120437 - 120437

Published: Jan. 3, 2024

Language: Английский

---

Identification of 1,3,4-Thiadiazolyl-Containing Thiazolidine-2,4-dione Derivatives as Novel PTP1B Inhibitors with Antidiabetic Activity

Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 67(10), P. 8406 - 8419

Published: May 9, 2024

Forty-one 1,3,4-thiadiazolyl-containing thiazolidine-2,4-dione derivatives (MY1–41) were designed and synthesized as protein tyrosine phosphatase 1B (PTP1B) inhibitors with activity against diabetes mellitus (DM). All compounds presented potential PTP1B inhibitory activities, half-maximal concentration (IC50) values ranging from 0.41 ± 0.05 to 4.68 0.61 μM, compared that of the positive control lithocholic acid (IC50 = 9.62 0.14 μM). The most potent compound, MY17 μM), was a reversible, noncompetitive inhibitor PTP1B. Circular dichroism spectroscopy molecular docking employed analyze binding interaction between In HepG2 cells, treatment could alleviate palmitic (PA)-induced insulin resistance by upregulating expression phosphorylated receptor substrate kinase B. vivo, oral administration reduce fasting blood glucose level improve tolerance dyslipidemia in mice suffering DM.

Language: Английский

---

Novel thiosemicarbazide-based β-carboline derivatives as α-glucosidase inhibitors: Synthesis and biological evaluation

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 275, P. 116595 - 116595

Published: June 12, 2024

Language: Английский

---

Thiazolidine-2,4-dione derivatives as potential α-glucosidase inhibitors: Synthesis, inhibitory activity, binding interaction and hypoglycemic activity

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 144, P. 107177 - 107177

Published: Feb. 6, 2024

Language: Английский

---

Synthesis, anti-α-glucosidase activity, inhibition interaction, and anti-diabetic activity of novel cryptolepine derivatives

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: 1310, P. 138311 - 138311

Published: April 11, 2024

Language: Английский

---

Alpha-glucosidase inhibitory and hypoglycemic effects of imidazole-bearing thioquinoline derivatives with different substituents: In silico, in vitro, and in vivo evaluations

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 144, P. 107106 - 107106

Published: Jan. 8, 2024

Language: Английский

---

Investigation on the inhibition mechanism and binding behavior of paeonol to tyrosinase and its anti-browning property by multi-spectroscopic and molecular docking methods

International Journal of Biological Macromolecules, Journal Year: 2023, Volume and Issue: 253, P. 126962 - 126962

Published: Sept. 16, 2023

Language: Английский

---

Synthesis of modified 1,3,4-thiadiazole incorporating substituted thiosemicarbazide derivatives: Elucidating the in vitro and in silico studies to develop promising anti-diabetic agent

Results in Chemistry, Journal Year: 2024, Volume and Issue: 8, P. 101556 - 101556

Published: May 24, 2024

Hybrid molecules based on the 1,3,4-thiadiazole were always choice of different researchers due to their significant application in medicinal as well pharmaceutical application. In present study, twenty analogs 1,3,4-thiadiazole-bearing thiosemicarbazide moiety (1–20) synthesized and screened for anti-diabetic profile. The compounds spectroscopically characterized through spectroscopic techniques such 1HNMR, 13CNMR, HREI-MS. Comparing whole set afforded standard glimepiride drugs (16.01 ± 0.02 μM), inhibition profiles against α-amylase ranged from 21.02 0.08 54.08 0.04 μM. synthetic normal (IC50 = 14.06 0.05 range α-glucosidase activity was likewise variable, ranging 18.04 0.07 μM IC50 51.05 0.03 (against α-glucosidase). Compound 19 demonstrated high potency among produced since it had both ortho-nitro substitution at aryl ring. pattern substitutions around ring used all determine structure–activity relationship. addition, a molecular docking study conducted potent examine interactions between active residues targeted enzymes with compound. molecule showed types amino acid. outcome demonstrates that these provide several essential sites enzymes, hence strengthening enzymatic future prediction drug competitors.

Language: Английский

---

α-Glucosidase Inhibition Research of Derivatives Based on 2β-Acetoxyferruginol Scaffold Excluding Acetic Acid Group

Chinese Journal of Organic Chemistry, Journal Year: 2024, Volume and Issue: 44(2), P. 613 - 613

Published: Jan. 1, 2024

a 五邑大学生物科技与大健康学院 广东江门 529020) ( b 深圳大学生命与海洋科学学院 广东深圳 518060) c 兰州大学药学院 兰州 730000) 摘要 合成了系列 2β-acetoxyferruginol 去醋酸基骨架衍生物(1～24), 并测定了其 α-葡萄糖苷酶抑制活性.结果表明: 化合物 1～24 均有较好的 α-葡萄糖苷酶抑制作用.其中(3R,4aS,10aS)-6-羟基-1,1,4-三甲基-1,2,3,4,4a,9,10,10-八氢邻蒽-3-基-4-(三氟甲基)苯甲酸酯(15)抑制 α-葡萄糖苷酶活性最强[IC50＝(23.91±2.34)μmol/L], 是阿卡波糖抑制活性的 23.6 倍. 构效关系分析表明三氟甲基的引入更有利于提高化合物的活性.动力学结果显示化合物 15 为可逆非竞争性的 α-葡 萄糖苷酶抑制剂.3D 荧光结果表明化合物 与 α-葡萄糖苷酶的结合可改变 α-葡萄糖苷酶的构象.分子对接结果显示化

---