Paliwal Sarvesh K, Verma Ankita Narayan, Paliwal Shailendra
Banasthali University, Distt-Tonk, 304022, Rajasthan, India.
Sci Pharm. 2011 Jul-Sep;79(3):389-428. doi: 10.3797/scipharm.1012-08. Epub 2011 May 10.
Human African Trypanosomiasis (HAT) also called sleeping sickness is caused by subspecies of the parasitic hemoflagellate Trypanosoma brucei that mostly occurs in sub-Saharan Africa. The current chemotherapy of the human trypanosomiases relies on only six drugs, five of which have been developed more than 30 years ago, have undesirable toxic side effects and most of them show drug-resistance. Though development of new anti-trypanosomal drugs seems to be a priority area research in this area has lagged far behind. The given review mainly focus upon the recent synthetic and computer based approaches made by various research groups for the development of newer anti-trypanosomal analogues which may have improved efficacy and oral bioavailability than the present ones. The given paper also attempts to investigate the relationship between the various physiochemical parameters and anti-trypanosomal activity that may be helpful in development of potent anti-trypanosomal agents against sleeping sickness.
人类非洲锥虫病(HAT),又称昏睡病,由寄生性血鞭毛虫布氏锥虫的亚种引起,主要发生在撒哈拉以南非洲地区。目前治疗人类锥虫病的化疗仅依赖六种药物,其中五种是30多年前研发的,具有不良的毒副作用,而且大多数都出现了耐药性。尽管开发新的抗锥虫药物似乎是一个优先研究领域,但该领域的研究远远滞后。本综述主要关注各研究小组最近采用的合成方法和基于计算机的方法,以开发新型抗锥虫类似物,这些类似物可能比现有药物具有更高的疗效和口服生物利用度。本文还试图研究各种物理化学参数与抗锥虫活性之间的关系,这可能有助于开发针对昏睡病的强效抗锥虫药物。