Synthesis and evaluation of urea and thiourea derivatives of lopinavir intermediate as potent antimicrobial, antioxidant agents and molecular docking studies against Staphopain

被引：13

作者：

Sudhamani, H. ^{[1
]}

Basha, S. K. Thaslim ^{[1
]}

Adam, S. ^{[2
]}

Madhusudhana, S. ^{[3
]}

Rani, A. Usha ^{[3
]}

Raju, C. Naga ^{[1
]}

机构：

[1] Sri Venkateswara Univ, Dept Chem, Tirupati, Andhra Pradesh, India

[2] Reg Agr Res Stn, Nanotechnol Lab, Inst Frontier Technol, Tirupati 517502, Andhra Pradesh, India

[3] Sri Venkateswara Univ, Dept Bioinformat, Tirupati, Andhra Pradesh, India

来源：

RESEARCH ON CHEMICAL INTERMEDIATES | 2017年 / 43卷 / 01期

关键词：

Lopinavir intermediate; Isocyanates; Isothiocyanates; Antimicrobial and antioxidant activity; Molecular docking studies; BIOLOGICAL EVALUATION; PROTEASE INHIBITORS; ASCORBIC-ACID; PLASMA; ANTIBACTERIAL; RESISTANT; POWER;

D O I：

10.1007/s11164-016-2609-5

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of new urea and thiourea derivatives of lopinavir intermediate 7a-k was designed and synthesized from lopinavir intermediate by treating various biopotent isocyanates and isothiocyanates in the presence of base, 1,4-dimethyl piperazine, and their biological activity was evaluated . The bio-assay revealed that the compounds exhibited moderate to good antimicrobial and antioxidant activities; particularly, 7k showed high activity against Staphylococcus aureus. Further, to know the binding interactions of the title products with protease enzyme, molecular studies were performed, which revealed that 7j exhibited high binding affinity towards the enzyme cysteine protease from Staphylococcus aureus. The results from in vitro studies revealed that they can be used as effective antimicrobial and antioxidant agents. Furthermore, molecular docking studies shown very good interaction.

引用

页码：103 / 120

页数：18

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