Synthesis, in vitro and in silico study of novel 1,3-diphenylurea derived Schiff bases as competitive α-glucosidase inhibitors

被引：1

作者：

Pasha, Anam Rubbab ^{[1
,2
]}

Ullah, Saeed ^{[2
]}

Khan, Ajmal ^{[2
,8
]}

Halim, Sobia Ahsan ^{[2
]}

Hussain, Javid ^{[3
]}

Rehman, Tanzila ^{[4
]}

Talib, Rimsha ^{[1
]}

Alharthy, Rima D. ^{[5
]}

Kashtoh, Hamdy ^{[6
]}

Abdellattif, Magda H. ^{[7
]}

Al-Harrasi, Ahmed ^{[2
]}

Shafiq, Zahid ^{[1
]}

机构：

[1] Bahauddin Zakariya Univ, Inst Chem Sci, Multan 60800, Pakistan

[2] Univ Nizwa, Nat & Med Sci Res Ctr, POB 33,PC 616, Nizwa, Oman

[3] Univ Nizwa, Dept Biol Sci & Chem, Nizwa, Oman

[4] Women Univ, Dept Chem, Multan 60000, Pakistan

[5] King Abdulaziz Univ, Sci & Arts Coll, Dept Chem, Rabigh Branch, Rabigh 21911, Saudi Arabia

[6] Yeungnam Univ, Dept Biotechnol, Gyongsan 38541, Gyeongbuk, South Korea

[7] Taif Univ, Univ Coll Taraba, Coll Sci, Chem Dept, Taif 21944, Saudi Arabia

[8] Korea Univ, Coll Engn, Dept Chem & Biol Engn, 145 Anam Ro, Seoul 02841, South Korea

来源：

RSC ADVANCES | 2024年 / 14卷 / 40期

关键词：

UREA; SALICYLALDEHYDE; IDENTIFICATION; DERIVATIVES;

D O I：

10.1039/d4ra05767h

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Diabetes mellitus has become a major global health burden because of several related consequences, including heart disease, retinopathy, cataracts, metabolic syndrome, collapsed renal function, and blindness. In the recent study, thirty Schiff base derivatives of 1,3-diphenylurea were synthesized and their anti-diabetic activity was evaluated by targeting alpha-glucosidase. The compounds exhibited an overwhelming inhibitory potential for alpha-glucosidase with higher potency ranging from 2.49-37.16 mu M. The most effective compound, 5h, showed competitive inhibition of alpha-glucosidase (K-i = 3.96 +/- 0.0048 mu M) in the kinetic analysis and strong binding interactions with key residues alpha-glucosidase in docking analysis, indicating its potential for better glycemic control in diabetes patients.

引用

页码：29288 / 29300

页数：13

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