SYNTHESIS, ANTIMICROBIAL AND α-GLUCOSIDASE INHIBITORY POTENTIAL OF MANNICH BASES OF MERCAPTO OXADIAZOLES AND THEIR MOLECULAR DOCKING STUDIES

被引：9

作者：

Ahmad, Sakina ^{[1
]}

Nadeem, Humaira ^{[1
]}

Muhammad, Syed Aun ^{[2
]}

Naz, Shagufta ^{[1
]}

Imran, Muhammad ^{[1
]}

Saeed, Adil ^{[1
]}

机构：

[1] Riphah Int Univ, Riphah Inst Pharmaceut Sci, Dept Pharmaceut Chem, 7th Ave,Sect G 7-4, Islamabad 44000, Pakistan

[2] Bahauddin Zakariya Univ, Dept Biotechnol, Multan, Pakistan

来源：

FARMACIA | 2018年 / 66卷 / 04期

关键词：

synthesis; Mannich bases; alpha-glucosidase inhibitors; diabetes mellitus; SUBSTITUTED 1,3,4-OXADIAZOLE; DERIVATIVES; ANTIFUNGAL; AGENTS;

D O I：

10.31925/farmacia.2018.4.22

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

In the current study a series of eight Mannich bases were synthesized by incorporating 5-subsituted-1,3,4-oxadiazole-2-th one scaffold. The target compounds were evaluated for their antimicrobial and a-glucosidase inhibitory activity. All the synthesized Mannich bases exhibited alpha-glucosidase inhibitory activity with IC50 values between 43.05 +/- 0.11 and 78.27 +/- 0.44 when compared with standard acarbose 27.10 +/- 0.51. Two compounds 3c and 4c containing morpholine moiety exhibited 85% & 82% inhibition as compared to the standard drug (acarbose) which gives 94% inhibition at dose level of 100 mu g/mL. None of the compounds showed significant antimicrobial activity. The interactions of the all compounds with alpha-glucosidase enzyme were further studied with the help of docking analysis.

引用

页码：708 / 717

页数：10

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