Structure-activity and structure-property relationship studies of spirocyclic chromanes with antimalarial activity. (1st March 2022)

• Record Type: Journal Article
• Authors: Iyamu, Iredia D.; Zhao, Yingzhao; Parvatkar, Prakash T.; Roberts, Bracken F.; Casandra, Debora R.; Wojtas, Lukasz; Kyle, Dennis E.; Chakrabarti, Debopam; Manetsch, Roman
• Is Part Of: Bioorganic & medicinal chemistry. Volume 57(2022)
• Publication Date: 2022-03-01
• Subjects: Antimalarial -- Drug resistance -- Natural products -- Spirocyclic chromane -- Structure-activity relationship -- Structure-property relationship; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2022.116629
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Abstract: Malaria is a prevalent and lethal disease. The fast emergence and spread of resistance to current therapies is a major concern and the development of a novel line of therapy that could overcome, the problem of drug resistance, is imperative. Screening of a set of compounds with drug/natural product-based sub-structural motifs led to the identification of spirocyclic chroman-4-one 1 with promising antimalarial activity against the chloroquine-resistant Dd2 and chloroquine-sensitive 3D7 strains of the parasite. Extensive structure-activity and structure-property relationship studies were conducted to identify the essential features necessary for its activity and properties.