Synthesis and antimalarial evaluation of cyclic beta-amino acid-containing dipeptides.
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.
Sathe
Manisha
M
Discovery Center, Defence R & D Establishment, Jhansi Road, Gwalior 474002, India.
Thavaselvam
Duraipandian
D
Srivastava
Ashish Kumar
AK
Kaushik
Mahabir Parshad
MP
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
D000598:Amino Acids, Cyclic; D000962:Antimalarials; D004151:Dipeptides