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Sci Pharm. 2011 Jul-Sep;79(3):389-428. doi: 10.3797/scipharm.1012-08. Epub 2011 May 10.

Neglected disease - african sleeping sickness: recent synthetic and modeling advances.

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1
Banasthali University, Distt-Tonk, 304022, Rajasthan, India.

Abstract

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.

KEYWORDS:

Central nervous system (CNS); Computer assisted drug design (CADD); Human African Trypanosomiasis (HAT); Structure-activity relationship (SAR); Trypanothione reductase (TR)

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