In Vitro and In Silico Anti-plasmodial Evaluation of Newly Synthesized β-Carboline Derivatives

被引：11

作者：

Kumar, Vipin ^{[1
]}

Sachdeva, Cheryl ^{[2
]}

Waidha, Kamran ^{[3
]}

Sharma, Sunil ^{[4
]}

Ray, Devalina ^{[3
]}

Kaushik, Naveen Kumar ^{[2
]}

Saha, Biswajit ^{[3
]}

机构：

[1] Amity Univ, Amity Inst Click Chem Res & Studies, Sect 125, Noida 201313, Uttar Pradesh, India

[2] Amity Univ, Amity Inst Virol & Immunol Inst, Sect 125, Noida 201313, Uttar Pradesh, India

[3] Amity Univ, Amity Inst Biotechnol, Sect 125, Noida 201313, Uttar Pradesh, India

[4] Natl Tsing Hua Univ, Chem Engn Dept, Hsinchu 30013, Taiwan

来源：

CHEMISTRYSELECT | 2021年 / 6卷 / 21期

关键词：

Antimalarial activity; beta-Carbolines; Conjugates; Guanidine; Molecular Docking; Thiourea; PICTET-SPENGLER; ANTIMALARIAL; ALKALOIDS; DISCOVERY; SPIROINDOLONES; MALARIA; POTENT;

D O I：

10.1002/slct.202101355

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Series of novel thiourea and guanidine conjugated beta-carbolines along with other analogues of this class were designed and synthesized for in vitro antimalarial activity against Plasmodium falciparum to overcome the threat of resistance to anti-malarial drug. Among them, two guanidine conjugated beta-carbolines 7a and 7c showed promising activities against both sensitive and resistant strains Pf3D7 and PfINDO with the IC50 values ranging from 0.6-1.0 mu M. The relative activities were further supported by in silico docking and binding studies of the synthesized scaffolds against specific targets, revealing that DHFR and FP3 may act as a potential target for 7a and 7c respectively.

引用

页码：5338 / 5342

页数：5

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