Vial H J, Ancelin M L, Elabbadi N, Gumila C, Bonnet H, Jeong Y H, Philippot J, Calas M, Portefaix P, Piquet G
Interactions membranaires, CNRS URA 530, Montpellier, France.
Parassitologia. 1993 Jul;35 Suppl:125-7.
The aim of our program was to find an original chemotherapeutical treatment (and eventually a preventive treatment) of malaria, an illness largely predominant in developing countries, by interfering on an essential metabolism developed by Plasmodium during its erythrocytic phase. Apart from what has been learnt about metabolism and the pharmacological target, a crucial step has been taken during this contract by passing from micromolar in vitro active concentrations (during 1986-1990) to nanomolar ones (during 1990). These compounds should naturally short-circuit resistance phenomena already established against drugs in current use, as has already been verified on polypharmacoresistant strains or isolates of P. falciparum. The administration of a therapeutic dose of our molecules would now appear to be possible in all cases.
我们项目的目标是通过干扰疟原虫在红细胞阶段所进行的关键代谢过程，找到一种针对疟疾的原创化疗方法（最终也可能是预防方法）。疟疾在发展中国家极为普遍。除了已了解的代谢和药理靶点信息外，在本合同期内还迈出了关键一步，即活性浓度从1986 - 1990年期间的微摩尔级体外浓度提升到了1990年期间的纳摩尔级。这些化合物自然能够绕过已有的针对现有药物的耐药现象，这一点已在恶性疟原虫的多药耐药菌株或分离株上得到验证。现在看来，在所有情况下给予治疗剂量的我们的分子都是可行的。
