Identification, in-vitro anti-plasmodial assessment and docking studies of series of tetrahydrobenzothieno[2,3-d]pyrimidine-acetamide molecular hybrids as potential antimalarial agents

Autor: Kavita Pal, Md Kausar Raza, Jenny Legac, Abdur Rahman, Shoaib Manzoor, Souvik Bhattacharjee, Philip J. Rosenthal, Nasimul Hoda
Rok vydání: 2022
Předmět:
Zdroj: European journal of medicinal chemistry. 248
ISSN: 1768-3254
Popis: Malaria is the most lethal parasitic infections in the world. To address the emergence of drug resistance to current antimalarials, here we report the design and synthesis of new series of tetrahydrobenzothieno[2,3-d]pyrimidine-acetamide hybrids by using multicomponent Petasis reaction as the key step and evaluated in vitro for their antimalarial effectiveness. The structure of all the compounds were confirmed by NMR Spectroscopy and mass spectrometry. Most of the compounds showed potent antimalarial activity against both CQ-sensitive (3D7) and CQ-resistant (W2) strains. A8, A5, and A4 are the most potent compounds that showed excellent anti-plasmodial activity against CQ-resistant strain in the nanomolar range with IC
Databáze: OpenAIRE