全部文献期刊学位论文会议报纸专利标准年鉴图书|学者科研项目
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作者:Prateep Pakavathkumar , Anastasia Noël , Clotilde Lecrux ...
来源:[J].Molecular Neurodegeneration(IF 4.007), 2017, Vol.12 (1)Springer
摘要:... Caspase-6 inhibitors could be useful against these neurodegenerative diseases but most Caspase-6 inhibitors have been exclusively studied in vitro or show acute liver toxicity in humans. Here, we assessed vinyl sulfone small molecule peptide caspase inhibitors for potential ...
作者:Eduardo R. Cobo , Sharon L. Reed , Lynette B. Corbeil
来源:[J].International Journal of Antimicrobial Agents(IF 4.415), 2012, Vol.39 (3), pp.259-262Elsevier
摘要:... In this study, the efficacies of the vinyl sulfone CP inhibitors K11777 and WRR-483 were tested against CPs of T. foetus . The activity of secreted T. foetus CPs in culture supernatants was decreased in the presence of vinyl sulfone inhibitors. Inhibitor K11777 reduced the in...
作者:Jindřich Fanfrlík , Pathik S Brahmkshatriya , Jan Řezáč ...
来源:[J].J. Phys. Chem. B, 2013, Vol.117 (48), pp.14973鈥?4982ACS
摘要:† Institute of Organic Chemistry and Biochemistry, v.v.i., and Gilead Sciences and IOCB Research Center, Academy of Sciences of the Czech Republic, Flemingovo nám. ... This work was a part of research project RVO: 61388963 of the Institute of Organic Chemistry and Biochemist...
作者:Fanfrlík Jindřich , Brahmkshatriya Pathik S , Řezáč Jan ...
来源:[J].The journal of physical chemistry. B, 2013, Vol.117 (48), pp.14973-82PubMed
摘要:... This enhanced QM-based scoring function is applied to a series of 20 vinyl sulfone-based inhibitory compounds inactivating the cysteine peptidase cathepsin B1 of the Schistosoma mansoni parasite (SmCB1). The available X-ray structure of the SmCB1 in complex with a potent vinyl sulfone...
作者:Kathleen E Rogers , Henrik Keränen , Jacob D. Durrant ...
来源:[J].Chemical Biology & Drug Design(IF 2.469), 2012, Vol.80 (3), pp.398-405Wiley
摘要:... Recent advances in a class of vinyl sulfone inhibitors are encouraging; however, as most potential therapeutics fail in clinical trials and both disease progression and resistance call for combination therapy with several drugs, the identification of additional classes of i...
作者:Marion G. Götz , Conor R. Caffrey , Elizabeth Hansell ...
来源:[J].Bioorganic & Medicinal Chemistry(IF 2.903), 2004, Vol.12 (19), pp.5203-5211Elsevier
摘要:Abstract(#br)A new series of peptidyl allyl sulfone inhibitors was discovered while trying to synthesize epoxy sulfone inhibitors from vinyl sulfones using basic oxidizing conditions. The various dipeptidyl allyl sulfones were evaluated with calpain I, papain, cathepsins B and L,...
作者:Karl A. Scheidt , William R. Roush , James H. McKerrow ...
来源:[J].Bioorganic & Medicinal Chemistry(IF 2.903), 1998, Vol.6 (12), pp.2477-2494Elsevier
摘要:... A crystal structure of cruzain, covalently inactivated by fluoromethyl ketone inhibitor 1 (Cbz-Phe-Ala-FMK), was used as a template to design potential inhibitors. Conformationally constrained γ-lactams containing electrophilic aldehyde ( 12, 17, 18, 25, 26, and 29 ) or vinyl sulfone...
作者:Paulo M.C. Glória , Isabel Coutinho , Lídia M. Gonçalves ...
来源:[J].European Journal of Medicinal Chemistry(IF 3.499), 2011, Vol.46 (6), pp.2141-2146Elsevier
摘要:Abstract(#br)In this article we describe an expanded structure–activity relationship study for vinyl sulfones as caspase-3 inhibitors, a topic virtually unexplored in the existing literature. Most remarkably, and to our surprise, tripeptidyl vinyl sulfones were not active ...

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