Synthesis and antiplasmodial activity of novel indoleamide derivatives bearing sulfonamide and triazole pharmacophores

被引：46

作者：

Devender, N. ^{[1
]}

Gunjan, Sarika ^{[2
,3
]}

Tripathi, Renu ^{[2
,3
]}

Tripathi, Rama Pati ^{[1
,3
]}

机构：

[1] CSIR, Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226031, Uttar Pradesh, India

[2] CSIR, Cent Drug Res Inst, Parasitol Div, Lucknow 226031, Uttar Pradesh, India

[3] Acad Sci & Innovat Res AcSIR, New Delhi, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2017年 / 131卷

关键词：

Indoleamide; Sulfonamide; Triazole; Antiplasmodial activity; PARASITE PLASMODIUM-FALCIPARUM; BIOLOGICAL EVALUATION; IN-VITRO; PROTEASOME INHIBITORS; ANTIMALARIAL ACTIVITY; MALARIA; DESIGN; MELATONIN; POTENT; UBIQUITIN;

D O I：

10.1016/j.ejmech.2017.03.010

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Due to the recent reports of growing parasite resistance to artemisinins and other antimalarial drugs, development of new antimalarial chemotypes is an urgent priority. Here in, we report a novel series of adamantyl/cycloheptyl indoleamide derivatives bearing sulfonamide and triazole pharmacophores adopting different chemical modifications and evaluated them for antiplasmodial activity in vitro. Among all the indoleamides, compounds 22, 24, 26 and 30 with sulfonamide pharmacophore showed promising activity with IC50 of 1.87,1.93, 2.00, 2.17 mu M against CQsensitive Pf3D7 strain and 1.69, 2.12,1.60, 2.19 mu M against CQ resistant Pfl(1 strain, respectively. (C) 2017 Elsevier Masson SAS. All rights reserved.

引用

页码：171 / 184

页数：14

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