On peroxide antimalarials | Zendy

Igor Opsenica | Zendy; Dejan Opsenica | Zendy; Milka Jadranin | Zendy; Kirsten S. Smith | Zendy; Wilbur K. Milhous | Zendy; Manolis Stratakis | Zendy; Bogdan A. Šolaja | Zendy

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On peroxide antimalarials

Author(s) -

Igor Opsenica,

Dejan Opsenica,

Milka Jadranin,

Kirsten S. Smith,

Wilbur K. Milhous,

Manolis Stratakis,

Bogdan A. Šolaja

Publication year - 2007

Publication title -

journal of the serbian chemical society

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.227

H-Index - 45

eISSN - 1820-7421

pISSN - 0352-5139

DOI - 10.2298/jsc0712181o

Subject(s) - chemistry , chloroquine , plasmodium falciparum , peroxide , natural product , pharmacology , multiple drug resistance , combinatorial chemistry , hydrogen peroxide , stereochemistry , malaria , biochemistry , biology , organic chemistry , antibiotics , immunology

Several dicyclohexylidene tetraoxanes were prepared in order to gain a further insight into structure-activity relationship of this kind of antimalarials. The tetraoxanes 2-5, obtained as a cis/trans mixture, showed pronounced antimalarial activity against Plasmodium falciparum chloroquine susceptible D6, chloroquine resistant W2 and multidrug-resistant TM91C235 (Thailand) strains. They have better than or similar activity to the corresponding desmethyl dicyclohexylidene derivatives. Two chimeric endoperoxides with superior antimalarial activity to the natural product ascaridole were also synthesized.

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