Abstract
Schistosomiasis is one of the world's major public health problems. Besides praziquantel (PZQ), there is currently no other effective treatment against schistosomiasis. The development of new antischistosomal agents to curb the emergence of PZQ resistance should be a high priority. Oxadiazole-2-oxides have been identified as potential antischistosomal reagents, with thioredoxin glutathione reductase (TGR) being one of their molecular targets. To develop novel treatment reagents against Schistosoma japonicum, 30 novel oxadiazole-2-oxides were synthesised and their antischistosomal activities on juvenile and adult S. japonicum were evaluated in vitro and in vivo. Their inhibitory activities against S. japonicum thioredoxin glutathione reductase (SjTGR) were also analysed. Most of the oxadiazole-2-oxides showed good juvenile and adult S. japonica killing activities in vitro. However, the antischistosomal effects of these compounds were not positively correlated with either their inhibition of SjTGR, or with nitric oxide (NO) release. Compounds 4a, 4b, 7c, 13, 16 and 20 resulted in 87.7%, 83.1%, 87.1%, 84.6%, 90.8% and 69.5%, respectively, mortality in the adult worms, when used to treat infected mice at schistosomula stage. These ...Continue Reading
References
Aug 1, 1995·The American Journal of Tropical Medicine and Hygiene·F F StelmaB Gryseels
Dec 9, 1994·Journal of Medicinal Chemistry·C MedanaA Gasco
Sep 1, 1993·Parasitology·R Harrop, R A Wilson
Aug 23, 2001·International Immunopharmacology·L R Brunet
Sep 10, 2003·Chembiochem : a European Journal of Chemical Biology·Giovanni SorbaFrancesco Dubini
Mar 21, 2006·Trends in Parasitology·Ana Rivero
May 17, 2006·British Journal of Pharmacology·Catriona M TurnbullIan L Megson
Sep 26, 2006·Lancet·Bruno GryseelsLuc Kestens
Jun 9, 2007·Bioorganic & Medicinal Chemistry Letters·Fiona RonkettiMatthew H Todd
Sep 12, 2007·Journal of Medicinal Chemistry·M Federica BuonsantiAlberto Gasco
Mar 18, 2008·Nature Medicine·Ahmed A SayedDavid L Williams
Sep 19, 2009·Journal of Medicinal Chemistry·Ganesha RaiCraig J Thomas
Oct 10, 2009·Parasitology·T ManneckJ Keiser
Oct 24, 2009·Parasitology Research·Shu-Hua XiaoPei-Ying Jiao
Nov 10, 2009·Parasitology Research·Lizandra G MagalhãesAdemar A Da Silva Filho
Dec 8, 2009·Parasitology·J Keiser
Mar 23, 2010·Bioorganic & Medicinal Chemistry Letters·Yuxiang DongJonathan L Vennerstrom
Aug 3, 2010·ChemMedChem·Alexander Dömling, Kareem Khoury
Jul 8, 2011·Current Opinion in Infectious Diseases·Conor R Caffrey, W Evan Secor
Jan 6, 2012·Bioorganic & Medicinal Chemistry Letters·Partha Sarathi SadhuVaidya Jayathirtha Rao
Jan 24, 2012·Bioorganic & Medicinal Chemistry Letters·Wen-wen DuanChao-ming Xia
Mar 3, 2012·PloS One·LiJun SongChuanXin Yu
Jul 31, 2012·International Journal for Parasitology. Drugs and Drug Resistance·R S TregerJ J Vermeire
Sep 26, 2012·Journal of Medicinal Chemistry·Malay PatraGilles Gasser
Oct 12, 2012·Parasitology Research·Wei WangYou-Sheng Liang
Jan 9, 2013·Chemistry : a European Journal·Malay PatraGilles Gasser
Feb 8, 2013·International Journal of Molecular Sciences·Dieudonné NdjonkaCarsten Wrenger
Apr 27, 2013·Chemical Biology & Drug Design·Zhi-xia WangChunhua Qiao
Jun 6, 2013·Parasites & Vectors·Jian LiuWei Hu
Jun 14, 2013·PloS One·Jian LiuWei Hu
Citations
Dec 14, 2017·Future Medicinal Chemistry·Eloi M LagoJosué de Moraes
Sep 14, 2018·ChemMedChem·Patrick MäderMartin Schlitzer
Oct 21, 2017·Journal of Cellular Biochemistry·Rohit ShuklaTimir Tripathi
Dec 19, 2016·BioMed Research International·Doaa A YonesAhmed M El-Moghazy
Apr 4, 2021·Pathogens·Viatcheslav A MordvinovMaria Y Pakharukova
Jan 26, 2018·Chemico-biological Interactions·Luana Maria Mariz Gomes da SilvaMonica Camelo Pessoa de Azevedo Albuquerque