Esterre P, Jamet P
Med Trop (Mars). 1987 Jan-Mar;47(1):47-52.
The antifungal and antiparasitic drugs research is particularly active for about twenty years and has provided many families of interesting molecules. The earliest antifungal imidazoles (kétoconazole and soon itraconazole) show a large activity spectrum and a good efficiency, especially in the deeply localized mycoses. As concerns the anthelmintics, the drugs recently introduced on the human medical market (flubendazole, albendazole, praziquantel) are largely used in veterinary medicine for many years. The most promising molecule for the future is the invermectin, peculiarly for the treatment of filariasis. The nitro-5-imidazoles family has some molecules with a good activity against protozoa, although they are bad contact amoebicid. Some rare molecules, escaped from a large laboratory screening (méfloquine, halofantrine) present an interesting antiplasmodial activity. But many tropical diseases (i.e. filariasis, leishmaniasis, trypanosomiasis) are, for the moment, inaccessible for the lack of enough potent chemotherapy.
抗真菌和抗寄生虫药物研究在大约二十年间一直特别活跃,并已提供了许多有趣的分子家族。最早的抗真菌咪唑类药物(酮康唑以及不久后的伊曲康唑)显示出广泛的活性谱和良好的疗效,尤其在深部局限性真菌病方面。至于驱虫药,最近进入人类医学市场的药物(氟苯达唑、阿苯达唑、吡喹酮)多年来在兽医学中大量使用。未来最有前景的分子是伊维菌素,特别是用于治疗丝虫病。硝基 - 5 - 咪唑类家族有一些对原生动物具有良好活性的分子,尽管它们是不良的接触性杀阿米巴药。一些从大型实验室筛选中脱颖而出的罕见分子(甲氟喹、卤泛群)具有有趣的抗疟活性。但目前许多热带疾病(如丝虫病、利什曼病、锥虫病)因缺乏足够有效的化疗而无法得到治疗。