Evaluation of Plasmodium falciparum-microsomal in vitro system for testing pro-drugs
Venkataramaiah, T.; Gajanana, A.
Indian Journal of Medical Research 86: 579-581
1987
ISSN/ISBN: 0019-5340 PMID: 3330544 Document Number: 299587
An in vitro system to test blood schizontocidal activity of drugs that are active after biotransformation (pro-drugs), was further evaluated by assaying 20 biguanide and guanidine derivatives. All the compounds were inactive per se and all but 3 compounds were inactive after incubating microsomal metabolic activating system. The compounds which showed definite schizontocidal activity against Plasmodium falciparum were 2 aniline biguanide and one quinozolyl guanidine derivatives. The results thus confirmed the value of the new in vitro technique for identifying the compounds which are active after bioconversion.