Synthesis and antimalarial activity of hydroxyethylpiperazine derivatives

Structures of three (2R,3S)-4-(arylmethyl)-1-(4-phenyl-3-amino-2-hydroxy-butyl)-piperazine derivatives, potential anti-malarial agents

“…Molecules containing hydroxyethylamine moieties [9] have been found, for example, to be potent inhibitors of these enzymes. Some of us have been studying the potential of hydroxyethylamines as anti-malarial agents and recently reported 1) against P. falciparum, the most dangerous of the four malaria parasites that infect humans [10][11][12].…”

Spectral investigations, DFT computations and molecular docking studies of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-{3-[4-(2-methylphenyl)piperazin-1-yl]propyl}-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione

“…The incorporation of piperazine is an important synthetic strategy in drug discovery due to its easy modificability, proper alkality, water solubility, the capacity for the formation of hydrogen bonds and adjustment of molecular physicochemical properties [1,2]. Arylpiperazine derivatives exhibit a wide range of biological activities such as antiviral [3], anticancer [4,5], antioxidative [6], anti-fungal [7], anti-parasitic [8], anti-histamin [9] and psychotolytic [10]. The effect of 1,4-bis-(4-(1H-benzo[d]imidazol-2-yl-phenyl))piperazine, on U937 leukemia cell viability was investigated [11].…”

Piperazine scaffold: A remarkable tool in generation of diverse pharmacological agents

“…Hydroxyethylpiperazine derivatives developed by Cunico et al were screened for antimalarial activity. Compound 130 was found to be most active with an IC 50 of 5.1 µg/mL[224]. In another series of hydroxyethylpiperazines developed by Cunico et al, compound 131 was most active antimalarial agent with an IC 50 of 16.9 µM[225].…”