- Structure-Bioactivity Relationships of Lapatinib Derived Analogs against Schistosoma mansoni
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We recently reported a series of compounds for a solubility-driven optimization campaign of antitrypanosomal compounds. Extending a parasite-hopping approach to the series, a subset of compounds from this library has been cross-screened for activity against the metazoan flatworm parasite, Schistosoma mansoni. This study reports the identification and preliminary development of several potently bioactive compounds against adult schistosomes, one or more of which represent promising leads for further assessment and optimization.
- Bachovchin, Kelly A.,Bag, Seema,Buskes, Melissa J.,Caffrey, Conor R.,Campbell, Robert F.,Clements, Monica,El-Sakkary, Nelly,Ferrins, Lori,Jalani, Hitesh B.,Klug, Dana M.,Leonard, Allison,Pollastri, Michael P.,Sciotti, Richard J.,Singh, Baljinder
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supporting information
p. 258 - 265
(2020/03/30)
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- BICYCLIC NITROIMIDAZOLES COVALENTLY LINKED TO SUBSTITUTED PHENYL OXAZOLIDINONES
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The current invention provides a series of bicyclic nitroimidazole- substituted phenyl oxazolidinones in which a bicyclic nitroimidazole pharmacophore is covalently bonded to a phenyl oxazolidinone, their pharmaceutical compositions, and the method of use of the compositions for prevention and treatment of bacterial infections. The bicyclic nitroimidazole-substituted phenyl oxazolidinones possess surprising antibacterial activity against wild- type and resistant strains of pathogens, and are therefore useful for the prevention, control and treatment of a number of human and veterinary bacterial infections caused by these pathogens, such as Mycobacterium tuberculosis.
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Page/Page column 119
(2009/10/22)
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