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Synthesis and antimalarial evaluation of cyclic beta-amino acid-containing dipeptides.
- Source :
-
Molecules (Basel, Switzerland) [Molecules] 2008 Feb 18; Vol. 13 (2), pp. 432-43. Date of Electronic Publication: 2008 Feb 18. - Publication Year :
- 2008
-
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.
- Subjects :
- Amino Acids, Cyclic chemistry
Animals
Antimalarials chemistry
Dipeptides chemistry
Drug Resistance drug effects
Humans
Inhibitory Concentration 50
Mice
Parasitic Sensitivity Tests
Plasmodium berghei drug effects
Plasmodium falciparum drug effects
Schizonts drug effects
Amino Acids, Cyclic chemical synthesis
Amino Acids, Cyclic pharmacology
Antimalarials chemical synthesis
Antimalarials pharmacology
Dipeptides chemical synthesis
Dipeptides pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1420-3049
- Volume :
- 13
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Molecules (Basel, Switzerland)
- Publication Type :
- Academic Journal
- Accession number :
- 18305429
- Full Text :
- https://doi.org/10.3390/molecules13020432