Synthesis, β-hematin inhibition studies and antimalarial evaluation of dehydroxy isotebuquine derivatives against Plasmodium berghei. Issue 15 (1st August 2015)

• Record Type: Journal Article
• Authors: Romero, Angel H.; Acosta, María E.; Gamboa, Neira; Charris, Jaime E.; Salazar, José; López, Simón E.
• Is Part Of: Bioorganic & medicinal chemistry. Volume 23:Issue 15(2015)
• Page Start: 4755
• Page End: 4762
• Publication Date: 2015-08-01
• Subjects: Malaria -- Isotebuquine -- 4-Aminoquinoline -- Haemozoin formation -- β-Hematin -- Antimalarial activity; 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.2015.05.040
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Abstract: Diverse dehydroxy-isotebuquine derivatives were prepared by using a five step synthetic sequence in good yields. All these new 4-aminoquinolines were evaluated as inhibitors of haemozoin formation, where most of them showed a significant inhibition value (% IHF >97). The best inhibitors were tested in vivo as potential antimalarials in mice infected with Plasmodium berghei ANKA chloroquine susceptible strain, three of them (11b, 11d and 11h ) displayed an antimalarial activity comparable to that of chloroquine.