Unit 3 Case Study On Oxamniquine

Case study 4 Even in the absence of a known drug target, a drug can be designed to perform a specific function through the testing of a variety of substituents. Through this, the biological activity of each substituent can be determined in order to create the final product in the form of a marketable drug. An example of this is oxamniquine, which is a drug that is active against schistosomes, the causative agent for schistosomiasis (Patrick, 2013, p. 305). Schistosomiasis, caused by three species of schistosomes, is a disease that is prevalent in much of the world, particularly in developing countries. There were five goals in the design process of developing oxamniquine. These goals were that it should be non-toxic, able to be effective when taken orally, able to be effective in one dose, effective against all three schistosomes species, and affordable to synthesize. These goals were set in place because of the previous drugs that were used to treat schistosomiasis, lucanthone and stibocaptate. Lucanthone was toxic both to cardiac tissue and central nervous tissue and not effective against all strains of schistosomiasis. Additionally, it had to be taken 3-5 times a day. Likewise, stibocaptate was potentially toxic and required multiple doses to produce an affect. …show more content…
The first step that was taken was the removal of two of the rings and replacing them with a chloro group. This left the structure known as mirasan, which consisted of the beta-aminoethylamino and a methyl group in addition to the chloro substituent. Surprisingly, this contributed more biological activity in mice than the two additional rings had. It was, however, not effective in humans. By default, it was determined that the beta-aminoethylamino was the element that contributed the most biological activity against schistosomiasis (Patrick, 2013, p.