Antimalarial activities of ring-substituted bioimidazoles

• Published in: Bioorganic & medicinal chemistry letters Vol. 12; no. 13; pp. 1701 - 1704
• Main Authors: Jain, Rahul, Vangapandu, Suryanarayana, Jain, Meenakshi, Kaur, Navneet, Singh, Savita, Pal Singh, Prati
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 08.07.2002; Elsevier
• Subjects: Animals; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antimalarials - chemical synthesis; Antimalarials - pharmacology; Antiparasitic agents; Biological and medical sciences; Chloroquine - pharmacology; Drug Resistance; Histamine - analogs & derivatives; Histamine - chemical synthesis; Histamine - pharmacology; Histidine - analogs & derivatives; Histidine - chemical synthesis; Histidine - chemistry; Histidine - pharmacology; Imidazoles - chemical synthesis; Imidazoles - chemistry; Imidazoles - pharmacology; In Vitro Techniques; Inhibitory Concentration 50; Medical sciences; Mice; Pharmacology. Drug treatments; Plasmodium berghei - drug effects; Plasmodium falciparum - drug effects; Structure-Activity Relationship; Antimalarial; Imidazole derivatives; Protozoal disease; Five membered ring; Nitrogen heterocycle; Plasmodium falciparum; Plasmodium berghei; Structure activity relation; Parasiticid; Chemical synthesis; Protozoa; Apicomplexa; Malaria; Rodentia; Parasitosis; In vitro; Infection; In vivo; α-Aminoacid; Vertebrata; Chemotherapy; Experimental disease; Mammalia; Treatment; Mouse; Animal; Primary amine
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/S0960-894X(02)00289-5

We report in vitro antimalarial activities against chloroquine sensitive and resistant Plasmodium falciparum strains, and in vivo activities against Plasmodium berghei in mice for four series of ring-substituted- l-histidines and histamines. The in vitro and in vivo antimalarial activities for four series of ring-substituted bioimidazoles (R=H, CO 2H) are reported.