6-nitro-1-4-dihydroquinoxaline-2-3-dione and Schistosomiasis-mansoni

Schistosomiasis is a neglected disease of poverty that is caused by infection with blood fluke species contained within the genus Schistosoma. For the last 40 years, control of schistosomiasis in endemic regions has predominantly been facilitated by administration of a single drug, praziquantel. Due to limitations in this mono-chemotherapeutic approach for sustaining schistosomiasis control into the future, alternative anti-schistosomal compounds are increasingly being sought by the drug discovery community. Herein, we describe a multi-pronged, integrated strategy that led to the identification and further exploration of the quinoxaline core as a promising anti-schistosomal scaffold. Firstly, phenotypic screening of commercially available small molecules resulted in the identification of a moderately active hit compound against Schistosoma mansoni (1, EC

Topics: Animals; Cell Line, Tumor; Cell Survival; Dose-Response Relationship, Drug; Humans; Molecular Structure; Quinoxalines; Schistosoma haematobium; Schistosoma japonicum; Schistosoma mansoni; Schistosomiasis mansoni; Structure-Activity Relationship