title: Synthesis and antimalarial evaluation of cyclic beta-amino acid-containing dipeptides.
abstract: This paper describes an efficient synthesis and the antiparasitic evaluation of cyclic beta-amino acid-containing dipeptides 3.1-3.6 and 4.1-4.5. The antimalarial properties of all these dipeptides have been evaluated in vitro against Plasmodium falciparum and in vivo against Plasmodium berghai. Compounds 4.4 and 4.5 have been found to be very effective in this respect, with IC50 values of 3.87 and 3.64 microg/mL in the in vitro test, while 4.5 has also been found to be active in the in vivo evaluation.
authors.affiliation: Discovery Center, Defence R & D Establishment, Jhansi Road, Gwalior 474002, India.
authors.forename: Manisha
authors.initials: M
authors.lastname: Sathe
authors.forename: Duraipandian
authors.initials: D
authors.lastname: Thavaselvam
authors.forename: Ashish Kumar
authors.initials: AK
authors.lastname: Srivastava
authors.forename: Mahabir Parshad
authors.initials: MP
authors.lastname: Kaushik
mesh_terms: D000598:Amino Acids, Cyclic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004151:Dipeptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004351:Drug Resistance / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D021261:Parasitic Sensitivity Tests; D010962:Plasmodium berghei / Q000187:drug effects; D010963:Plasmodium falciparum / Q000187:drug effects; D052939:Schizonts / Q000187:drug effects
chemical_list: D000598:Amino Acids, Cyclic; D000962:Antimalarials; D004151:Dipeptides