The Experts below are selected from a list of 327 Experts worldwide ranked by ideXlab platform
Patricia Sartorelli - One of the best experts on this subject based on the ideXlab platform.
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Antiparasitic Activity of Natural and Semi-Synthetic Tirucallane Triterpenoids from Schinus terebinthifolius (Anacardiaceae): Structure/Activity Relationships
Molecules (Basel Switzerland), 2014Co-Authors: Thiago R. Morais, Andre G. Tempone, Alberto De Oliveira, Thais A. Costa-silva, Samanta Etel Treiger Borborema, Marcus Tullius Scotti, Raquel M.f. Sousa, Ana Carolina C. Araujo, Sérgio Antônio Lemos De Morais, Patricia SartorelliAbstract:Leishmaniasis and Chagas are diseases caused by parasitic protozoans that affect the poorest population in the World, causing a high mortality and morbidity. As a result of highly toxic and long-term treatments, the discovery of novel, safe and more efficacious drugs is essential. In this work, the in vitro Antiparasitic Activity and mammalian cytotoxicity of three natural tirucallane triterpenoids, isolated from leaves of Schinus terebinthifolius (Anacardiaceae), and nine semi-synthetic derivatives were investigated against Leishmania (L.) infantum and Trypanosoma cruzi. Trypomastigotes of T. cruzi were the most susceptible parasites and seven compounds demonstrated a trypanocidal Activity with IC50 values in the range between 15 and 58 µg/mL. Four compounds demonstrated selectivity towards the intracellular amastigotes of Leishmania, with IC50 values in the range between 28 and 97 µg/mL. The complete characterization of triterpenoids was afforded after thorough analysis of nuclear magnetic resonance (NMR) data as well as electrospray ionization mass spectrometry (ESI-MS). Additionally, structure-Activity relationships were performed using Decision Trees.
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Antiparasitic Activity of natural and semi synthetic tirucallane triterpenoids from schinus terebinthifolius anacardiaceae structure Activity relationships
Molecules, 2014Co-Authors: Thiago R. Morais, Andre G. Tempone, Alberto De Oliveira, Samanta Etel Treiger Borborema, Marcus Tullius Scotti, Raquel M.f. Sousa, Ana Carolina C. Araujo, Sérgio Antônio Lemos De Morais, Thais A Costasilva, Patricia SartorelliAbstract:Leishmaniasis and Chagas are diseases caused by parasitic protozoans that affect the poorest population in the World, causing a high mortality and morbidity. As a result of highly toxic and long-term treatments, the discovery of novel, safe and more efficacious drugs is essential. In this work, the in vitro Antiparasitic Activity and mammalian cytotoxicity of three natural tirucallane triterpenoids, isolated from leaves of Schinus terebinthifolius (Anacardiaceae), and nine semi-synthetic derivatives were investigated against Leishmania (L.) infantum and Trypanosoma cruzi. Trypomastigotes of T. cruzi were the most susceptible parasites and seven compounds demonstrated a trypanocidal Activity with IC50 values in the range between 15 and 58 µg/mL. Four compounds demonstrated selectivity towards the intracellular amastigotes of Leishmania, with IC50 values in the range between 28 and 97 µg/mL. The complete characterization of triterpenoids was afforded after thorough analysis of nuclear magnetic resonance (NMR) data as well as electrospray ionization mass spectrometry (ESI-MS). Additionally, structure-Activity relationships were performed using Decision Trees.
Alberto De Oliveira - One of the best experts on this subject based on the ideXlab platform.
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New alkenyl derivative from Piper malacophyllum and analogues: Antiparasitic Activity against Trypanosoma cruzi and Leishmania infantum.
Chemical biology & drug design, 2017Co-Authors: Marina T. Varela, Marta L. Lima, Mariana K. Galuppo, Andre G. Tempone, Alberto De Oliveira, João Henrique G. Lago, João Paulo S. FernandesAbstract:Alkylphenols isolated from Piper malacophyllum (Piperaceae), gibbilimbols A and B, showed interesting Activity against the parasites Trypanosoma cruzi and Leishmania infantum. In continuation to our previous work, a new natural product from the essential oil of the leaves of P. malacophyllum was isolated, the 5-[(3E)-oct-3-en-1-il]-1,3-benzodioxole, and also a new set of five compounds was prepared. The Antiparasitic Activity of the natural product was evaluated in vitro against these parasites, indicating potential against the promastigote/trypomastigote/amastigote forms (IC50 32-83 μm) of the parasites and low toxicity (CC50 > 200 μm) to mammalian cells. The results obtained to the synthetic compounds indicated that the new derivatives maintained the promising Antiparasitic Activity, but the cytotoxicity was considerably lowered. The amine derivative LINS03011 displayed the most potent IC50 values (13.3 and 16.7 μm) against amastigotes of T. cruzi and L. infantum, respectively, indicating comparable Activity to the phenolic prototype LINS03003, with threefold decreased (CC50 73.5 μm) cytotoxicity, leading the selectivity index (SI) towards the parasites up to 24.5. In counterpart, LINS03011 has not shown membrane disruptor Activity in SYTOX Green model. In summary, this new set showed the hydroxyl is not essential for the Antiparasitic Activity, and its substitution could decrease the toxicity to mammalian cells.
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Antiparasitic Activity of Natural and Semi-Synthetic Tirucallane Triterpenoids from Schinus terebinthifolius (Anacardiaceae): Structure/Activity Relationships
Molecules (Basel Switzerland), 2014Co-Authors: Thiago R. Morais, Andre G. Tempone, Alberto De Oliveira, Thais A. Costa-silva, Samanta Etel Treiger Borborema, Marcus Tullius Scotti, Raquel M.f. Sousa, Ana Carolina C. Araujo, Sérgio Antônio Lemos De Morais, Patricia SartorelliAbstract:Leishmaniasis and Chagas are diseases caused by parasitic protozoans that affect the poorest population in the World, causing a high mortality and morbidity. As a result of highly toxic and long-term treatments, the discovery of novel, safe and more efficacious drugs is essential. In this work, the in vitro Antiparasitic Activity and mammalian cytotoxicity of three natural tirucallane triterpenoids, isolated from leaves of Schinus terebinthifolius (Anacardiaceae), and nine semi-synthetic derivatives were investigated against Leishmania (L.) infantum and Trypanosoma cruzi. Trypomastigotes of T. cruzi were the most susceptible parasites and seven compounds demonstrated a trypanocidal Activity with IC50 values in the range between 15 and 58 µg/mL. Four compounds demonstrated selectivity towards the intracellular amastigotes of Leishmania, with IC50 values in the range between 28 and 97 µg/mL. The complete characterization of triterpenoids was afforded after thorough analysis of nuclear magnetic resonance (NMR) data as well as electrospray ionization mass spectrometry (ESI-MS). Additionally, structure-Activity relationships were performed using Decision Trees.
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Antiparasitic Activity of natural and semi synthetic tirucallane triterpenoids from schinus terebinthifolius anacardiaceae structure Activity relationships
Molecules, 2014Co-Authors: Thiago R. Morais, Andre G. Tempone, Alberto De Oliveira, Samanta Etel Treiger Borborema, Marcus Tullius Scotti, Raquel M.f. Sousa, Ana Carolina C. Araujo, Sérgio Antônio Lemos De Morais, Thais A Costasilva, Patricia SartorelliAbstract:Leishmaniasis and Chagas are diseases caused by parasitic protozoans that affect the poorest population in the World, causing a high mortality and morbidity. As a result of highly toxic and long-term treatments, the discovery of novel, safe and more efficacious drugs is essential. In this work, the in vitro Antiparasitic Activity and mammalian cytotoxicity of three natural tirucallane triterpenoids, isolated from leaves of Schinus terebinthifolius (Anacardiaceae), and nine semi-synthetic derivatives were investigated against Leishmania (L.) infantum and Trypanosoma cruzi. Trypomastigotes of T. cruzi were the most susceptible parasites and seven compounds demonstrated a trypanocidal Activity with IC50 values in the range between 15 and 58 µg/mL. Four compounds demonstrated selectivity towards the intracellular amastigotes of Leishmania, with IC50 values in the range between 28 and 97 µg/mL. The complete characterization of triterpenoids was afforded after thorough analysis of nuclear magnetic resonance (NMR) data as well as electrospray ionization mass spectrometry (ESI-MS). Additionally, structure-Activity relationships were performed using Decision Trees.
Andre G. Tempone - One of the best experts on this subject based on the ideXlab platform.
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Antiparasitic Activity of new gibbilimbol analogues and SAR analysis through efficiency and statistical methods.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 2018Co-Authors: Marina T. Varela, Marta L. Lima, Andre G. Tempone, Samanta Etel Treiger Borborema, Maiara M. Romaneli, João Paulo S. FernandesAbstract:Abstract Chagas' disease and leishmaniasis are parasitic infections enrolled among the neglected tropical diseases, which urge for new treatments. In the search for new chemical entities as prototypes, gibbilimbols A/B have shown Antiparasitic Activity against Trypanosoma cruzi and Leishmania infantum , and then a set of analogues (LINS03 series) of this natural product were synthesized and evaluated in vitro against the parasites. In the present paper we reported five new compounds with Activity against these protozoan parasites, and quite low cytotoxicity. Moreover, the interference of plasma membrane permeability of these analogues were also evaluated. We found that [(4-methoxyphenyl)methyl]octylamine ( 4 ) was noteworthy due to its high Activity against the amastigote form of both parasites (IC 50 1.3–5.8 μM) and good selectivity index. In order to unveil the SAR for this chemotype, we also presented a group efficiency analysis and PCA and HCA study, which indicated that the methoxyl provides good Activity with lower cytotoxicity to mammalian cells. The results from SAR analyses suggest different mechanisms of action between the neutral and basic compounds. In summary, the analogues represent important Activity against these parasites and must be prototypes for further exploitation.
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New alkenyl derivative from Piper malacophyllum and analogues: Antiparasitic Activity against Trypanosoma cruzi and Leishmania infantum.
Chemical biology & drug design, 2017Co-Authors: Marina T. Varela, Marta L. Lima, Mariana K. Galuppo, Andre G. Tempone, Alberto De Oliveira, João Henrique G. Lago, João Paulo S. FernandesAbstract:Alkylphenols isolated from Piper malacophyllum (Piperaceae), gibbilimbols A and B, showed interesting Activity against the parasites Trypanosoma cruzi and Leishmania infantum. In continuation to our previous work, a new natural product from the essential oil of the leaves of P. malacophyllum was isolated, the 5-[(3E)-oct-3-en-1-il]-1,3-benzodioxole, and also a new set of five compounds was prepared. The Antiparasitic Activity of the natural product was evaluated in vitro against these parasites, indicating potential against the promastigote/trypomastigote/amastigote forms (IC50 32-83 μm) of the parasites and low toxicity (CC50 > 200 μm) to mammalian cells. The results obtained to the synthetic compounds indicated that the new derivatives maintained the promising Antiparasitic Activity, but the cytotoxicity was considerably lowered. The amine derivative LINS03011 displayed the most potent IC50 values (13.3 and 16.7 μm) against amastigotes of T. cruzi and L. infantum, respectively, indicating comparable Activity to the phenolic prototype LINS03003, with threefold decreased (CC50 73.5 μm) cytotoxicity, leading the selectivity index (SI) towards the parasites up to 24.5. In counterpart, LINS03011 has not shown membrane disruptor Activity in SYTOX Green model. In summary, this new set showed the hydroxyl is not essential for the Antiparasitic Activity, and its substitution could decrease the toxicity to mammalian cells.
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Antiparasitic Activity of Natural and Semi-Synthetic Tirucallane Triterpenoids from Schinus terebinthifolius (Anacardiaceae): Structure/Activity Relationships
Molecules (Basel Switzerland), 2014Co-Authors: Thiago R. Morais, Andre G. Tempone, Alberto De Oliveira, Thais A. Costa-silva, Samanta Etel Treiger Borborema, Marcus Tullius Scotti, Raquel M.f. Sousa, Ana Carolina C. Araujo, Sérgio Antônio Lemos De Morais, Patricia SartorelliAbstract:Leishmaniasis and Chagas are diseases caused by parasitic protozoans that affect the poorest population in the World, causing a high mortality and morbidity. As a result of highly toxic and long-term treatments, the discovery of novel, safe and more efficacious drugs is essential. In this work, the in vitro Antiparasitic Activity and mammalian cytotoxicity of three natural tirucallane triterpenoids, isolated from leaves of Schinus terebinthifolius (Anacardiaceae), and nine semi-synthetic derivatives were investigated against Leishmania (L.) infantum and Trypanosoma cruzi. Trypomastigotes of T. cruzi were the most susceptible parasites and seven compounds demonstrated a trypanocidal Activity with IC50 values in the range between 15 and 58 µg/mL. Four compounds demonstrated selectivity towards the intracellular amastigotes of Leishmania, with IC50 values in the range between 28 and 97 µg/mL. The complete characterization of triterpenoids was afforded after thorough analysis of nuclear magnetic resonance (NMR) data as well as electrospray ionization mass spectrometry (ESI-MS). Additionally, structure-Activity relationships were performed using Decision Trees.
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Antiparasitic Activity of natural and semi synthetic tirucallane triterpenoids from schinus terebinthifolius anacardiaceae structure Activity relationships
Molecules, 2014Co-Authors: Thiago R. Morais, Andre G. Tempone, Alberto De Oliveira, Samanta Etel Treiger Borborema, Marcus Tullius Scotti, Raquel M.f. Sousa, Ana Carolina C. Araujo, Sérgio Antônio Lemos De Morais, Thais A Costasilva, Patricia SartorelliAbstract:Leishmaniasis and Chagas are diseases caused by parasitic protozoans that affect the poorest population in the World, causing a high mortality and morbidity. As a result of highly toxic and long-term treatments, the discovery of novel, safe and more efficacious drugs is essential. In this work, the in vitro Antiparasitic Activity and mammalian cytotoxicity of three natural tirucallane triterpenoids, isolated from leaves of Schinus terebinthifolius (Anacardiaceae), and nine semi-synthetic derivatives were investigated against Leishmania (L.) infantum and Trypanosoma cruzi. Trypomastigotes of T. cruzi were the most susceptible parasites and seven compounds demonstrated a trypanocidal Activity with IC50 values in the range between 15 and 58 µg/mL. Four compounds demonstrated selectivity towards the intracellular amastigotes of Leishmania, with IC50 values in the range between 28 and 97 µg/mL. The complete characterization of triterpenoids was afforded after thorough analysis of nuclear magnetic resonance (NMR) data as well as electrospray ionization mass spectrometry (ESI-MS). Additionally, structure-Activity relationships were performed using Decision Trees.
Thiago R. Morais - One of the best experts on this subject based on the ideXlab platform.
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Antiparasitic Activity of Natural and Semi-Synthetic Tirucallane Triterpenoids from Schinus terebinthifolius (Anacardiaceae): Structure/Activity Relationships
Molecules (Basel Switzerland), 2014Co-Authors: Thiago R. Morais, Andre G. Tempone, Alberto De Oliveira, Thais A. Costa-silva, Samanta Etel Treiger Borborema, Marcus Tullius Scotti, Raquel M.f. Sousa, Ana Carolina C. Araujo, Sérgio Antônio Lemos De Morais, Patricia SartorelliAbstract:Leishmaniasis and Chagas are diseases caused by parasitic protozoans that affect the poorest population in the World, causing a high mortality and morbidity. As a result of highly toxic and long-term treatments, the discovery of novel, safe and more efficacious drugs is essential. In this work, the in vitro Antiparasitic Activity and mammalian cytotoxicity of three natural tirucallane triterpenoids, isolated from leaves of Schinus terebinthifolius (Anacardiaceae), and nine semi-synthetic derivatives were investigated against Leishmania (L.) infantum and Trypanosoma cruzi. Trypomastigotes of T. cruzi were the most susceptible parasites and seven compounds demonstrated a trypanocidal Activity with IC50 values in the range between 15 and 58 µg/mL. Four compounds demonstrated selectivity towards the intracellular amastigotes of Leishmania, with IC50 values in the range between 28 and 97 µg/mL. The complete characterization of triterpenoids was afforded after thorough analysis of nuclear magnetic resonance (NMR) data as well as electrospray ionization mass spectrometry (ESI-MS). Additionally, structure-Activity relationships were performed using Decision Trees.
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Antiparasitic Activity of natural and semi synthetic tirucallane triterpenoids from schinus terebinthifolius anacardiaceae structure Activity relationships
Molecules, 2014Co-Authors: Thiago R. Morais, Andre G. Tempone, Alberto De Oliveira, Samanta Etel Treiger Borborema, Marcus Tullius Scotti, Raquel M.f. Sousa, Ana Carolina C. Araujo, Sérgio Antônio Lemos De Morais, Thais A Costasilva, Patricia SartorelliAbstract:Leishmaniasis and Chagas are diseases caused by parasitic protozoans that affect the poorest population in the World, causing a high mortality and morbidity. As a result of highly toxic and long-term treatments, the discovery of novel, safe and more efficacious drugs is essential. In this work, the in vitro Antiparasitic Activity and mammalian cytotoxicity of three natural tirucallane triterpenoids, isolated from leaves of Schinus terebinthifolius (Anacardiaceae), and nine semi-synthetic derivatives were investigated against Leishmania (L.) infantum and Trypanosoma cruzi. Trypomastigotes of T. cruzi were the most susceptible parasites and seven compounds demonstrated a trypanocidal Activity with IC50 values in the range between 15 and 58 µg/mL. Four compounds demonstrated selectivity towards the intracellular amastigotes of Leishmania, with IC50 values in the range between 28 and 97 µg/mL. The complete characterization of triterpenoids was afforded after thorough analysis of nuclear magnetic resonance (NMR) data as well as electrospray ionization mass spectrometry (ESI-MS). Additionally, structure-Activity relationships were performed using Decision Trees.
Samanta Etel Treiger Borborema - One of the best experts on this subject based on the ideXlab platform.
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Antiparasitic Activity of new gibbilimbol analogues and SAR analysis through efficiency and statistical methods.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 2018Co-Authors: Marina T. Varela, Marta L. Lima, Andre G. Tempone, Samanta Etel Treiger Borborema, Maiara M. Romaneli, João Paulo S. FernandesAbstract:Abstract Chagas' disease and leishmaniasis are parasitic infections enrolled among the neglected tropical diseases, which urge for new treatments. In the search for new chemical entities as prototypes, gibbilimbols A/B have shown Antiparasitic Activity against Trypanosoma cruzi and Leishmania infantum , and then a set of analogues (LINS03 series) of this natural product were synthesized and evaluated in vitro against the parasites. In the present paper we reported five new compounds with Activity against these protozoan parasites, and quite low cytotoxicity. Moreover, the interference of plasma membrane permeability of these analogues were also evaluated. We found that [(4-methoxyphenyl)methyl]octylamine ( 4 ) was noteworthy due to its high Activity against the amastigote form of both parasites (IC 50 1.3–5.8 μM) and good selectivity index. In order to unveil the SAR for this chemotype, we also presented a group efficiency analysis and PCA and HCA study, which indicated that the methoxyl provides good Activity with lower cytotoxicity to mammalian cells. The results from SAR analyses suggest different mechanisms of action between the neutral and basic compounds. In summary, the analogues represent important Activity against these parasites and must be prototypes for further exploitation.
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Antiparasitic Activity of Natural and Semi-Synthetic Tirucallane Triterpenoids from Schinus terebinthifolius (Anacardiaceae): Structure/Activity Relationships
Molecules (Basel Switzerland), 2014Co-Authors: Thiago R. Morais, Andre G. Tempone, Alberto De Oliveira, Thais A. Costa-silva, Samanta Etel Treiger Borborema, Marcus Tullius Scotti, Raquel M.f. Sousa, Ana Carolina C. Araujo, Sérgio Antônio Lemos De Morais, Patricia SartorelliAbstract:Leishmaniasis and Chagas are diseases caused by parasitic protozoans that affect the poorest population in the World, causing a high mortality and morbidity. As a result of highly toxic and long-term treatments, the discovery of novel, safe and more efficacious drugs is essential. In this work, the in vitro Antiparasitic Activity and mammalian cytotoxicity of three natural tirucallane triterpenoids, isolated from leaves of Schinus terebinthifolius (Anacardiaceae), and nine semi-synthetic derivatives were investigated against Leishmania (L.) infantum and Trypanosoma cruzi. Trypomastigotes of T. cruzi were the most susceptible parasites and seven compounds demonstrated a trypanocidal Activity with IC50 values in the range between 15 and 58 µg/mL. Four compounds demonstrated selectivity towards the intracellular amastigotes of Leishmania, with IC50 values in the range between 28 and 97 µg/mL. The complete characterization of triterpenoids was afforded after thorough analysis of nuclear magnetic resonance (NMR) data as well as electrospray ionization mass spectrometry (ESI-MS). Additionally, structure-Activity relationships were performed using Decision Trees.
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Antiparasitic Activity of natural and semi synthetic tirucallane triterpenoids from schinus terebinthifolius anacardiaceae structure Activity relationships
Molecules, 2014Co-Authors: Thiago R. Morais, Andre G. Tempone, Alberto De Oliveira, Samanta Etel Treiger Borborema, Marcus Tullius Scotti, Raquel M.f. Sousa, Ana Carolina C. Araujo, Sérgio Antônio Lemos De Morais, Thais A Costasilva, Patricia SartorelliAbstract:Leishmaniasis and Chagas are diseases caused by parasitic protozoans that affect the poorest population in the World, causing a high mortality and morbidity. As a result of highly toxic and long-term treatments, the discovery of novel, safe and more efficacious drugs is essential. In this work, the in vitro Antiparasitic Activity and mammalian cytotoxicity of three natural tirucallane triterpenoids, isolated from leaves of Schinus terebinthifolius (Anacardiaceae), and nine semi-synthetic derivatives were investigated against Leishmania (L.) infantum and Trypanosoma cruzi. Trypomastigotes of T. cruzi were the most susceptible parasites and seven compounds demonstrated a trypanocidal Activity with IC50 values in the range between 15 and 58 µg/mL. Four compounds demonstrated selectivity towards the intracellular amastigotes of Leishmania, with IC50 values in the range between 28 and 97 µg/mL. The complete characterization of triterpenoids was afforded after thorough analysis of nuclear magnetic resonance (NMR) data as well as electrospray ionization mass spectrometry (ESI-MS). Additionally, structure-Activity relationships were performed using Decision Trees.