A promising α-glucosidase and α-amylase inhibitors based on benzimidazole-oxadiazole hybrid analogues: Evidence based in vitro and in silico studies

被引：4

作者：

Ullah, Hayat ^{[1
]}

Uddin, Imad ^{[2
]}

Ali, Hafeeza Zafar ^{[3
]}

Hassan, Wagma ^{[4
]}

Mehnaz, Gul ^{[5
]}

Maryam, Laiba ^{[3
]}

Sarfraz, Maliha ^{[6
]}

Khan, Muhammad Saleem ^{[7
]}

Islam, Mohammad Shahidul ^{[8
]}

Almarhoon, Zainab M. ^{[8
]}

Iqbal, Rashid ^{[9
,10
]}

Nabi, Muhammad ^{[3
]}

机构：

[1] Univ Okara, Inst Chem, Okara 56300, Pakistan

[2] Univ Haripur, Dept Chem, Haripur 22620, Khyber Pakhtunk, Pakistan

[3] Khyber Med Univ, Inst Pharmaceut Sci, Peshawar 25000, Pakistan

[4] COMSATS Univ, Inst Biotechnol, Abbottabad Campus, Abbottabad, Pakistan

[5] Women Med & Dent Coll, Dept Pharmacol, Abbottabad, Pakistan

[6] Univ Agr Faisalabad, Dept Zool Wildlife & Fisheries, Subcampus, Toba Tek Singh 36080, Pakistan

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

[8] King Saud Univ, Coll Sci, Dept Chem, POB 2455, Riyadh 11451, Saudi Arabia

[9] Islamia Univ Bahawalpur, Fac Agr & Environm, Dept Agron, Bahawalpur 63100, Pakistan

[10] Western Caspian Univ, Dept Life Sci, Baku, Azerbaijan

来源：

RESULTS IN CHEMISTRY | 2024年 / 11卷

关键词：

Benzimidazole; Oxadiazole; Antidiabetic; Molecular Docking; SAR; BIOLOGICAL EVALUATION; DERIVATIVES;

D O I：

10.1016/j.rechem.2024.101832

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The present study reports the design and synthesis of new benzimidazole-oxadiazole compounds as potent inhibitors of alpha-glucosidase and alpha-amylase. The synthesized molecules were characterized through different techniques such as (HNMR)-H-1,(CNMR)-C- 13, HREI-MS and evaluated for their in vitro inhibitory activities against these enzymes. Among the compounds screened, compound 8 demonstrated the highest inhibitory activity against both alpha-glucosidase (IC50 = 11.60 mu M) and alpha-amylase (IC50 = 6.20 mu M). Molecular docking analyses were conducted to investigate the binding modes and interactions of the active compounds within the enzyme active sites. The results demonstrate that several benzimidazole-oxadiazole hybrids exhibited potent inhibitory effects on both alpha-glucosidase and alpha-amylase, suggesting their promise as antidiabetic agents.

引用

页数：11

共 38 条

[1] 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 [J].