RATIONAL DRUG DESIGN FOR GIARDIASIS

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This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. Primary support for the subproject and the subproject's principal investigator may have been provided by other sources, including other NIH sources. The Total Cost listed for the subproject likely represents the estimated amount of Center infrastructure utilized by the subproject, not direct funding provided by the NCRR grant to the subproject or subproject staff. Giardiasis is the most frequent cause of non-bacterial diarrhea and currently there is no FDA approved medicine available. Class II Giardia Fructose-1, 6-diphosphate aldolase is one of the key enzymes associated with pathogenic microbe Giardia lamblia, the direct cause of giardiasis. The goal is to develop tight binding, reversible inhibitors of class II Giardia fructose-1, 6-diphosphate aldolase in Giardia lamblia for alternative treatments of giardiasis. By using molecular modeling technology involving Insight II and Autodock, several inhibitor candidates against Giardia aldolase have been designed. In the summer of 2006, major intermediates of one of the designed inhibitors, aminomethylphosphonosulfonamide (AMPS), have been synthesized.