Contribution in an anthology

Appeared in: Neglected Tropical Diseases : Drug Discovery and Development

Editor list: Swinney, D; Pollastri, M; Mannhold, R; Buschmann, H; Holenz, J

Publication year: 2019

Pages: 187-225

ISBN: 978-3-527-80864-9

eISBN: 978-3-527-80865-6

DOI Link: https://doi.org/10.1002/9783527808656.ch8

Title of series: Methods and principles in medicinal chemistry

Abstract: 

Schistosomiasis is a neglected disease of poverty that is caused by several species of the trematode flatworm, Schistosoma. Treatment relies on just one drug, the pyrazinoisoquinoline, praziquantel (PZQ). PZQ has a number of pharmaceutical and pharmacological problems that encourage the search for new drugs. Focusing on the period 2015–2017, and in the context of a target product profile for a new drug, we review a number of molecular targets being considered with a particular perspective on kinases given their importance in the life cycle of the schistosome parasite and their well-established druggability. We also discuss several drug repurposing and structure-based design strategies, and highlight small molecule chemistries (organometallics, natural products, biarylalkyl carboxylic acids, and arylmethylamino steroids) under active development. Overall, drug discovery activity for schistosomiasis is increasingly robust and should yield advanced preclinical development candidates in the near future.

Harvard Citation style: Caffrey, C., El-Sakkary, N., Mäder, P., Krieg, R., Becker, K., Schlitzer, M., et al. (2019) Drug Discovery and Development for Schistosomiasis, in Swinney, D., Pollastri, M., Mannhold, R., Buschmann, H. and Holenz, J. (eds.) Neglected Tropical Diseases : Drug Discovery and Development . Weinheim: Wiley-VCH, pp. 187-225. https://doi.org/10.1002/9783527808656.ch8

APA Citation style: Caffrey, C., El-Sakkary, N., Mäder, P., Krieg, R., Becker, K., Schlitzer, M., Drewry, D., Vennerstrom, J., & Grevelding, C. (2019). Drug Discovery and Development for Schistosomiasis. In Swinney, D., Pollastri, M., Mannhold, R., Buschmann, H., & Holenz, J. (Eds.), Neglected Tropical Diseases : Drug Discovery and Development (pp. 187-225). Wiley-VCH. https://doi.org/10.1002/9783527808656.ch8