含磺酰胺和三唑药效基团的新型吲哚酰胺衍生物的合成及其抗疟活性
Synthesis and antiplasmodial activity of novel indoleamide derivatives bearing sulfonamide and triazole pharmacophores.
作者信息
Devender N, Gunjan Sarika, Tripathi Renu, Tripathi Rama Pati
机构信息
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow, 226031, India.
Parasitology Division, CSIR-Central Drug Research Institute, Lucknow, 226031, India; Academy of Scientific and Innovative Research (AcSIR), New Delhi, 110001, India.
出版信息
Eur J Med Chem. 2017 May 5;131:171-184. doi: 10.1016/j.ejmech.2017.03.010. Epub 2017 Mar 8.
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 IC of 1.87, 1.93, 2.00, 2.17 μM against CQ sensitive Pf3D7 strain and 1.69, 2.12, 1.60, 2.19 μM against CQ resistant PfK1 strain, respectively.
由于最近有报道称寄生虫对青蒿素和其他抗疟药物的耐药性不断增加，开发新的抗疟化学类型已成为当务之急。在此，我们报道了一系列带有磺酰胺和三唑药效基团的新型金刚烷基/环庚基吲哚酰胺衍生物，采用了不同的化学修饰，并对它们的体外抗疟活性进行了评估。在所有吲哚酰胺中，带有磺酰胺药效基团的化合物22、24、26和30表现出有前景的活性，对氯喹敏感的Pf3D7菌株的IC50分别为1.87、1.93、2.00、2.17 μM，对氯喹耐药的PfK1菌株的IC50分别为1.69、2.12、1.60、2.19 μM。
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