Synthesis and antiplasmodial activity of novel indoleamide derivatives bearing sulfonamide and triazole pharmacophores.
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 IC50of 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.
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow, 226031, India.
N
N
Devender
Parasitology Division, CSIR-Central Drug Research Institute, Lucknow, 226031, India; Academy of Scientific and Innovative Research (AcSIR), New Delhi, 110001, India.
Sarika
S
Gunjan
Parasitology Division, CSIR-Central Drug Research Institute, Lucknow, 226031, India; Academy of Scientific and Innovative Research (AcSIR), New Delhi, 110001, India. Electronic address: renu1113@rediffmail.com.
Renu
R
Tripathi
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow, 226031, India; Academy of Scientific and Innovative Research (AcSIR), New Delhi, 110001, India. Electronic address: rpt.cdri@gmail.com.
Rama Pati
RP
Tripathi
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D004305:Dose-Response Relationship, Drug; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects*; D013329:Structure-Activity Relationship; D000077145:Sulfanilamide; D013424:Sulfanilamides / Q000737:chemistry / Q000494:pharmacology*; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology*; D014709:Vero Cells
D000962:Antimalarials; D007211:Indoles; D013424:Sulfanilamides; D014230:Triazoles; D000077145:Sulfanilamide
Antiplasmodial activity; Indoleamide; Sulfonamide; Triazole