首页 | 本学科首页   官方微博 | 高级检索  
   检索      


Discovery of new organoselenium compounds as antileishmanial agents
Institution:1. Department of Pharmaceutical Chemistry, College of Pharmacy, Prince Sattam Bin Abdulaziz University, P.O. Box 173, Alkharj 11942, Saudi Arabia;2. University of Navarra, School of Pharmacy and Nutrition, Department of Pharmaceutical Technology and Chemistry, Irunlarrea 1, 31008 Pamplona, Spain;3. Departamento de Biología de Sistemas, Universidad de Alcala, E-28805 Alcala de Henares, Madrid, Spain;4. Department of Otorhinolaryngology, Faculty of Medicine and Life Sciences, University of Tampere and Tampere University Hospital, Finland;5. Faculty of Medicine and Life Sciences, University of Tampere and Fimlab Ltd, Tampere University Hospital, Finland;6. Department of Neuroscience, Psychology, Drug Research and Child’s Health (NEUROFARBA), Section of Pharmaceutical and Nutraceutical Sciences, Via Ugo Schiff 6, 50019, Sesto Fiorentino, Italy;1. University of Florence, Department of Chemistry “Ugo Schiff”, Via della Lastruccia 3-13, I-50019 Sesto Fiorentino (Florence), Italy;2. University of Florence, Department of Health Sciences - Section of Clinical Pharmacology and Oncology, Viale Pieraccini 6, 50139 Firenze, Italy;3. University of Florence, Department of Neurosciences, Psychology, Drug Research and Child’s Health - Section of Pharmaceutical and Nutraceutical Sciences, via Ugo Schiff 6, 50019 Sesto Fiorentino (FI), Italy;4. University of Florence, Department of Neurosciences, Psychology, Drug Research and Child’s Health - Section of Pharmacology, Viale Pieraccini 6, 50139 Firenze, Italy;1. University of Florence, Department of Chemistry \"Ugo Schiff\", Via della Lastruccia 3-13, I-50019, Sesto Fiorentino, Italy;2. NEUROFARBA Department, Section of Pharmacology and Toxicology, Università degli Studi di Firenze, Viale Pieraccini 6, 50139, Florence, Italy;3. CSIRO, 343 Royal Parade, Parkville, Victoria, 3052, Australia;4. Department of University of Florence, NEUROFARBA Dept., Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019, Sesto Fiorentino, Florence, Italy;5. Centre of Advanced Research in Bionanoconjugates and Biopolymers Department, “Petru Poni” Institute of Macromolecular Chemistry, Iasi, Romania;1. University of Florence, NEUROFARBA Dept, Sezione di Scienze Farmaceutiche e Nutraceutiche, Via Ugo Schiff 6, 50019, Sesto Fiorentino, Florence, Italy;2. University of Florence, Department of Chemistry “Ugo Schiff”, Via della Lastruccia 3, 50019, Sesto Fiorentino, Florence, Italy;3. Breakthrough Breast Unit and Division of Pathology, Institute of Genetics and Molecular Medicine, Edinburgh, EH4 2XU, UK;4. Department of Pharmaceutical Chemistry, College of Pharmacy, Prince Sattam Bin Abdulaziz University, PO Box 173, Alkharj, 11942, Saudi Arabia;1. Departamento de Química Orgánica and UMYMFOR (CONICET–FCEyN), Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Pabellón 2, Ciudad Universitaria, C1428EHA Buenos Aires, Argentina;2. Center for Tropical and Emerging Global Diseases and Department of Cellular Biology, University of Georgia, Athens, GA 30602, USA;3. Departamento de Química Inorgánica, Analítica y Química Física/INQUIMAE-CONICET, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Pabellón 2, Buenos Aires C1428EGA, Argentina;1. Università degli Studi di Firenze, NEUROFARBA Dept., Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy;2. Department of Biological Sciences and Chemistry, University of Nizwa, Birkat Al-Mauz, P.O.Box 33, Nizwa 616, Oman;3. Istituto di Bioscienze e Biorisorse, CNR, Via Pietro Castellino 111, 80131 Napoli, Italy
Abstract:We report new organoselenium compounds bearing the sulfonamide moiety as effective inhibitors of the β-isoform of Carbonic Anhydrase from the unicellular parasitic protozoan L. donovani chagasi. All derivatives were evaluated in vitro for their leishmanicidal activities against Leishmania infantum amastigotes along with their cytotoxicities in human THP-1 cells. Compounds 3e-g showed their activity in the low micromolar range with IC50 values spanning from 0.72 to 0.81 µM and selectivity indexes (SI) > 8 (for 3g SI > 30), thus much higher than those observed for the reference drugs miltefosine and edelfosine. This is the first study which reports new selenoderivatives with promising leishmanicidal properties and acting as Carbonic Anhydrase inhibitors too thus paving the way to the development of innovative agents for the treatment of neglected diseases such as leishmaniasis.
Keywords:Carbonic anhydrase  Inhibitor  Metalloenzymes  Selenium
本文献已被 ScienceDirect 等数据库收录!
设为首页 | 免责声明 | 关于勤云 | 加入收藏

Copyright©北京勤云科技发展有限公司  京ICP备09084417号