RATIONAL DRUG DESIGN FOR GIARDIASIS

这个子项目是许多利用 由NIH/NCRR资助的中心赠款提供的资源。子项目和 研究者（PI）可能从另一个NIH来源获得了主要资金， 因此可在其他CRISP条目中表示。所列机构为 研究中心，而研究中心不一定是研究者所在的机构。 贾第虫病是非细菌性腹泻的最常见原因，目前没有FDA批准的药物可用。贾第鞭毛虫果糖-1，6-二磷酸醛缩酶是贾第鞭毛虫的关键酶之一，是引起贾第鞭毛虫病的直接原因。目的是开发紧密结合的、可逆的蓝氏贾第鞭毛虫中的II类贾第鞭毛虫果糖-1，6-二磷酸醛缩酶抑制剂，用于贾第鞭毛虫病的替代治疗。利用InsightII和Autodock等分子模拟技术，设计了几种贾第虫醛缩酶抑制剂候选物。在2006年夏天，设计的抑制剂之一，氨甲基膦磺酰胺（AMPS）的主要中间体，已经合成。

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. 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.