The Experts below are selected from a list of 20061 Experts worldwide ranked by ideXlab platform
Filipe Silva Villela - One of the best experts on this subject based on the ideXlab platform.
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synthesis and structure activity relationship study of a new series of Antiparasitic aryloxyl thiosemicarbazones inhibiting trypanosoma cruzi cruzain
European Journal of Medicinal Chemistry, 2015Co-Authors: Jose Wanderlan Pontes Espindola, Diogo Rodrigo Magalhães Moreira, Milena Botelho Pereira Soares, Marcos Verissimo De Oliveira Cardoso, Gevanio Bezerra De Oliveira Filho, Dayane Albuquerque Oliveira E Silva, Tanira Matutino Bastos, Carlos A De Simone, Filipe Silva VillelaAbstract:The discovery of new Antiparasitic compounds against Trypanosoma cruzi, the etiological agent of Chagas disease, is necessary. Novel aryloxy/aryl thiosemicarbazone-based conformationally constrained analogs of thiosemicarbazones (1) and (2) were developed as potential inhibitors of the T. cruzi protease cruzain, using a rigidification strategy of the iminic bond of (1) and (2). A structure–activity relationship analysis was performed in substituents attached in both aryl and aryloxy rings. This study indicated that apolar substituents or halogen atom substitution at the aryl position improved cruzain inhibition and Antiparasitic activity in comparison to unsubstituted thiosemicarbazone. Two of these compounds displayed potent inhibitory Antiparasitic activity by inhibiting cruzain and consequently were able to reduce the parasite burden in infected cells and cause parasite cell death through necrosis. In conclusion, we demonstrated that conformational restriction is a valuable strategy in the development of Antiparasitic thiosemicarbazones.
Milena Botelho Pereira Soares - One of the best experts on this subject based on the ideXlab platform.
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synthesis and structure activity relationship study of a new series of Antiparasitic aryloxyl thiosemicarbazones inhibiting trypanosoma cruzi cruzain
European Journal of Medicinal Chemistry, 2015Co-Authors: Jose Wanderlan Pontes Espindola, Diogo Rodrigo Magalhães Moreira, Milena Botelho Pereira Soares, Marcos Verissimo De Oliveira Cardoso, Gevanio Bezerra De Oliveira Filho, Dayane Albuquerque Oliveira E Silva, Tanira Matutino Bastos, Carlos A De Simone, Filipe Silva VillelaAbstract:The discovery of new Antiparasitic compounds against Trypanosoma cruzi, the etiological agent of Chagas disease, is necessary. Novel aryloxy/aryl thiosemicarbazone-based conformationally constrained analogs of thiosemicarbazones (1) and (2) were developed as potential inhibitors of the T. cruzi protease cruzain, using a rigidification strategy of the iminic bond of (1) and (2). A structure–activity relationship analysis was performed in substituents attached in both aryl and aryloxy rings. This study indicated that apolar substituents or halogen atom substitution at the aryl position improved cruzain inhibition and Antiparasitic activity in comparison to unsubstituted thiosemicarbazone. Two of these compounds displayed potent inhibitory Antiparasitic activity by inhibiting cruzain and consequently were able to reduce the parasite burden in infected cells and cause parasite cell death through necrosis. In conclusion, we demonstrated that conformational restriction is a valuable strategy in the development of Antiparasitic thiosemicarbazones.
Jose Wanderlan Pontes Espindola - One of the best experts on this subject based on the ideXlab platform.
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synthesis and structure activity relationship study of a new series of Antiparasitic aryloxyl thiosemicarbazones inhibiting trypanosoma cruzi cruzain
European Journal of Medicinal Chemistry, 2015Co-Authors: Jose Wanderlan Pontes Espindola, Diogo Rodrigo Magalhães Moreira, Milena Botelho Pereira Soares, Marcos Verissimo De Oliveira Cardoso, Gevanio Bezerra De Oliveira Filho, Dayane Albuquerque Oliveira E Silva, Tanira Matutino Bastos, Carlos A De Simone, Filipe Silva VillelaAbstract:The discovery of new Antiparasitic compounds against Trypanosoma cruzi, the etiological agent of Chagas disease, is necessary. Novel aryloxy/aryl thiosemicarbazone-based conformationally constrained analogs of thiosemicarbazones (1) and (2) were developed as potential inhibitors of the T. cruzi protease cruzain, using a rigidification strategy of the iminic bond of (1) and (2). A structure–activity relationship analysis was performed in substituents attached in both aryl and aryloxy rings. This study indicated that apolar substituents or halogen atom substitution at the aryl position improved cruzain inhibition and Antiparasitic activity in comparison to unsubstituted thiosemicarbazone. Two of these compounds displayed potent inhibitory Antiparasitic activity by inhibiting cruzain and consequently were able to reduce the parasite burden in infected cells and cause parasite cell death through necrosis. In conclusion, we demonstrated that conformational restriction is a valuable strategy in the development of Antiparasitic thiosemicarbazones.
P. Caduff-janosa - One of the best experts on this subject based on the ideXlab platform.
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Vigilance der Tierarzneimittel: Gemeldete unerwünschte Wirkungen im Jahr 2009
Schweizer Archiv fur Tierheilkunde, 2010Co-Authors: C R Müntener, L. Bruckner, A. Stürer, Felix R. Althaus, P. Caduff-janosaAbstract:During the year 2009, 134 reports of suspected adverse drug reactions (ADRs) to veterinary medicinal products (VMPs) were received (106 in the year 2008). The distribution according to species and drug classes remained in line with previous years. Companion animals were involved in most of the reports (46 % dogs, 19 % cats), followed by cattle or calves (22 %). Antiparasitic drugs made the biggest part with 30 % of the reports, followed by antiinfectives (19 %) and hormones (13 %). Some reactions following their use are specifically discussed. 95 additional enquiries about ADRs of VMPs were received by the Swiss Toxicological Information Centre in Zurich. Most of them concerned dogs or cats and Antiparasitics or anti-inflammatory drugs. In the vaccinovigilance program, a total of 1020 reports were received, of which 1000 were related to the vaccination against blue tongue disease. The most frequently reported adverse reactions were aborts, mastitis or alterations of milk quality and they are specifically discussed.
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Vigilance der Tierarzneimittel: Gemeldete unerwünschte Wirkungen im Jahr 2008
Schweizer Archiv fur Tierheilkunde, 2009Co-Authors: C R Müntener, L. Bruckner, A. Stürer, Felix R. Althaus, P. Caduff-janosaAbstract:With 106 reports of suspected adverse reactions to veterinary medicinal products (VMPs) there was a slight decrease in the year 2008 compared to 2007. However, the distribution according to species and drug classes remained grossly the same: dogs were involved in 45 % of the cases followed in frequency by cats (26 %) and cows or calves (21 %). Most often the reports described reactions following the use of either an Antiparasitic drug (46 %) or an antibiotic (22 %). One particular case of off-label use and serious skin reactions are presented. For the vaccinovigilance a total of 310 reports were received, with 250 of them related to adverse events following vaccination against blue tongue disease. In most cases, aborts and elevated cell count in the milk were reported. A detailed evaluation of these cases is presented. Finally, 305 enquiries were received by the Swiss Toxicological Information Center in Zurich (concerning mostly dogs or cats). Most of the cases concerned either preparations for the nervous system or anti-inflammatory drugs (human medicinal products) or Antiparasitics (VMPs).
Louis Maes - One of the best experts on this subject based on the ideXlab platform.
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Design and evaluation of Trypanosoma brucei metacaspase inhibitors
Bioorganic & medicinal chemistry letters, 2010Co-Authors: Maya Berg, Pieter Van Der Veken, Jurgen Joossens, Venkatraj Muthusamy, Matthias Breugelmans, Catherine X. Moss, Jana Rudolf, Paul Cos, Graham H. Coombs, Louis MaesAbstract:Metacaspase (MCA) is an important enzyme in Trypanosoma brucei, absent from humans and differing significantly from the orthologous human caspases. Therefore MCA constitutes a new attractive drug target for Antiparasitic chemotherapeutics, which needs further characterization to support the discovery of innovative drug candidates. A first series of inhibitors has been prepared on the basis of known substrate specificity and the predicted catalytic mechanism of the enzyme. In this Letter we present the first inhibitors of TbMCA2 with low micromolar enzymatic and Antiparasitic activity in vitro combined with low cytotoxicity.
