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Most Requested Journal Articles 4Q07-Chemistry and Related Science

Following is one of the journal articles most requested by researchers using CAS electronic products.

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CAS indexed 188 chemical substances from this document. CAS subject entries for this document include: Structure-activity relationship; Cytotoxicity; Malaria; and 5 additional concepts

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TITLE:	Synthesis and in Vitro Antiprotozoal Activities of Dicationic 3,5-Diphenylisoxazoles
AUTHOR(S):	Patrick, Donald A.; Bakunov, Stanislav A.; Bakunova, Svetlana M.; Kumar, E. V. K. Suresh; Lombardy, Richard J.; Jones, Susan Kilgore; Bridges, Arlene S.; Zhirnov, Oksana; Hall, James Edwin; Wenzler, Tanja; Brun, Reto; Tidwell, Richard R.
CORPORATE SOURCE:	Department of Pathology and Laboratory Medicine, School of Medicine, University of North Carolina, Chapel Hill, NC, 27599-7525, USA
SOURCE:	Journal of Medicinal Chemistry (2007), 50(10), 2468-2485 CODEN: JMCMAR; ISSN: 0022-2623
PUBLISHER:	American Chemical Society
LANGUAGE:	English

ABSTRACT:
3,5-Bis(4-amidinophenyl)isoxazole - an analog of 2,5-bis(4-amidinophenyl)furan (furamidine) in which the central furan ring is replaced by isoxazole - and 42 novel analogs were prepd. by two general synthetic pathways. The 43 isoxazole derivs. were assayed against Trypanosoma brucei rhodesiense (T. brucei rhodesiense) STIB900, Plasmodium falciparum (P. falciparum) K1, and rat myoblast L6 cells (for cytotoxicity) in vitro. Eleven compds. exhibited antitrypanosomal IC50 values less than 10 nM, five of which displayed cytotoxic indexes (ratios of cytotoxic IC50 to antiprotozoal IC50 values) at least 10 times higher than that of furamidine. Eighteen compds. were more active against P. falciparum than furamidine, with IC50 values less than 15 nM. Fourteen of these compds. had cytotoxic indexes ranging between 10 and 120 times higher than that of furamidine, and five analogs exhibited high selectivity for P. falciparum over T. brucei rhodesiense.