The Experts below are selected from a list of 213 Experts worldwide ranked by ideXlab platform
Emanuel Hernandeznunez - One of the best experts on this subject based on the ideXlab platform.
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synthesis of benzologues of nitazoxanide and tizoxanide a comparative study of their in vitro broad spectrum Antiprotozoal activity
ChemInform, 2011Co-Authors: Gabriel Navarretevazquez, Fabiola Chavezsilva, Rocio Argotteramos, Maria Del Carmen Rodriguezgutierrez, Manuel Jesus Chanbacab, Roberto Cedillorivera, Rosa Moopuc, Emanuel HernandeznunezAbstract:Two new annulated analogues (I) of the Antiprotozoal Agent nitazoxanide (NIT) and its metabolite tizoxanide (TIZ), are prepared using a short synthetic route.
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synthesis of benzologues of nitazoxanide and tizoxanide a comparative study of their in vitro broad spectrum Antiprotozoal activity
Bioorganic & Medicinal Chemistry Letters, 2011Co-Authors: Gabriel Navarretevazquez, Fabiola Chavezsilva, Rocio Argotteramos, Maria Del Carmen Rodriguezgutierrez, Manuel Jesus Chanbacab, Roberto Cedillorivera, Rosa Moopuc, Emanuel HernandeznunezAbstract:Abstract We have synthesized two new benzologues of Nitazoxanide (NIT) and Tizoxanide (TIZ), using a short synthetic route. Both compounds were tested in vitro against six protozoa ( Giardia intestinalis , Trichomonas vaginalis , Entamoeba histolytic a, Plasmodium berghei , Leishmania mexicana and Trypanosoma cruzi ). Compound 1 (benzologue of NIT) showed broad Antiprotozoal effect against all parasites tested, showing IC 50 ’s G. intestinalis. It was 10-times more active than pentamidine against L. mexicana , and it was sevenfold more potent than benznidazole versus T. cruzi . This compound could be considered as a new broad spectrum Antiprotozoal Agent.
Thomas Tobin - One of the best experts on this subject based on the ideXlab platform.
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Toltrazuril sulfone sodium salt: synthesis, analytical detection, and pharmacokinetics in the horse.
Journal of Veterinary Pharmacology and Therapeutics, 2011Co-Authors: Levent Dirikolu, W. Karpiesiuk, Andreas F. Lehner, Thomas TobinAbstract:Dirikolu, L., Karpiesiuk, W., Lehner, A. F., Tobin, T. Toltrazuril sulfone sodium salt: synthesis, analytical detection, and pharmacokinetics in the Horse. J. vet. Pharmacol. Therap. 35, 265–274. Toltrazuril sulfone (ponazuril) is a triazine-based Antiprotozoal Agent with clinical application in the treatment of equine protozoal myeloencephalomyelitis (EPM). In this study, we synthesized and determined the bioavailability of a sodium salt formulation of toltrazuril sulfone that can be used for the treatment and prophylaxis of EPM in horses. Toltrazuril sulfone sodium salt was rapidly absorbed, with a mean peak plasma concentration of 2400 ± 169 (SEM) ng/mL occurring at 8 h after oral-mucosal dosing and was about 56% bioavailable compared with the i.v. administration of toltrazuril sulfone in dimethylsulfoxide (DMSO). The relative bioavailability of toltrazuril sulfone suspended in water compared with toltrazuril sulfone sodium salt was 46%, indicating approximately 54% less oral bioavailability of this compound suspended in water. In this study, we also investigated whether this salt formulation of toltrazuril sulfone can be used as a feed additive formulation without significant reduction in oral bioavailability. Our results indicated that toltrazuril sulfone sodium salt is relatively well absorbed when administered with feed with a mean oral bioavailability of 52%. Based on these data, repeated oral administration of toltrazuril sulfone sodium salt with or without feed will yield effective plasma and cerebrospinal fluid (CSF) concentrations of toltrazuril sulfone for the treatment and prophylaxis of EPM and other protozoal diseases of horses and other species. As such, toltrazuril sulfone sodium salt has the potential to be used as feed additive formulations for both the treatment and prophylaxis of EPM and various other apicomplexan diseases.
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Toltrazuril sulfone sodium salt: synthesis, analytical detection, and pharmacokinetics in the horse.
Journal of Veterinary Pharmacology and Therapeutics, 2011Co-Authors: Levent Dirikolu, W. Karpiesiuk, Andreas F. Lehner, Thomas TobinAbstract:Toltrazuril sulfone (ponazuril) is a triazine-based Antiprotozoal Agent with clinical application in the treatment of equine protozoal myeloencephalomyelitis (EPM). In this study, we synthesized and determined the bioavailability of a sodium salt formulation of toltrazuril sulfone that can be used for the treatment and prophylaxis of EPM in horses. Toltrazuril sulfone sodium salt was rapidly absorbed, with a mean peak plasma concentration of 2400 ± 169 (SEM) ng/mL occurring at 8 h after oral-mucosal dosing and was about 56% bioavailable compared with the i.v. administration of toltrazuril sulfone in dimethylsulfoxide (DMSO). The relative bioavailability of toltrazuril sulfone suspended in water compared with toltrazuril sulfone sodium salt was 46%, indicating approximately 54% less oral bioavailability of this compound suspended in water. In this study, we also investigated whether this salt formulation of toltrazuril sulfone can be used as a feed additive formulation without significant reduction in oral bioavailability. Our results indicated that toltrazuril sulfone sodium salt is relatively well absorbed when administered with feed with a mean oral bioavailability of 52%. Based on these data, repeated oral administration of toltrazuril sulfone sodium salt with or without feed will yield effective plasma and cerebrospinal fluid (CSF) concentrations of toltrazuril sulfone for the treatment and prophylaxis of EPM and other protozoal diseases of horses and other species. As such, toltrazuril sulfone sodium salt has the potential to be used as feed additive formulations for both the treatment and prophylaxis of EPM and various other apicomplexan diseases.
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New therapeutic approaches for equine protozoal myeloencephalitis: pharmacokinetics of diclazuril sodium salts in horses.
Veterinary therapeutics : research in applied veterinary medicine, 2006Co-Authors: Levent Dirikolu, W. Karpiesiuk, Andreas F. Lehner, Charlie Hughes, William E. Woods, J. D. Harkins, J. Boyles, Alfonza Atkinson, D.e. Granstrom, Thomas TobinAbstract:Diclazuril is a triazine-based Antiprotozoal Agent which may have clinical application in the treatment of equine protozoal myeloencephalomyelitis (EPM). In this study, the use of the sodium salt diclazuril to increase the apparent bioavailability of diclazuril for the treatment and prophylaxis of EPM and various other Apicomplexan mediated diseases is described. In this study, diclazuril sodium salt was synthesized and administered to horses as diclazuril sodium salt formulations. The absorption, distribution, and clearance of diclazuril sodium salt in the horse are described. Diclazuril was rapidly absorbed, with peak plasma concentrations occurring at 8-24 hours following an oral mucosal administration of diclazuril sodium salt. The mean oral bioavailability of diclazuril as Clinacox was 9.5% relative to oral mucosal administration of diclazuril sodium salt. Additionally, diclazuril in DMSO administered orally was 50% less bioavailable than diclazuril sodium salt following an oral mucosal administration. It was also shown that diclazuril sodium salt has the potential to be used as a feed additive for the treatment and prophylaxis of EPM and various other Apicomplexan mediated diseases.
Levent Dirikolu - One of the best experts on this subject based on the ideXlab platform.
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Toltrazuril sulfone sodium salt: synthesis, analytical detection, and pharmacokinetics in the horse.
Journal of Veterinary Pharmacology and Therapeutics, 2011Co-Authors: Levent Dirikolu, W. Karpiesiuk, Andreas F. Lehner, Thomas TobinAbstract:Dirikolu, L., Karpiesiuk, W., Lehner, A. F., Tobin, T. Toltrazuril sulfone sodium salt: synthesis, analytical detection, and pharmacokinetics in the Horse. J. vet. Pharmacol. Therap. 35, 265–274. Toltrazuril sulfone (ponazuril) is a triazine-based Antiprotozoal Agent with clinical application in the treatment of equine protozoal myeloencephalomyelitis (EPM). In this study, we synthesized and determined the bioavailability of a sodium salt formulation of toltrazuril sulfone that can be used for the treatment and prophylaxis of EPM in horses. Toltrazuril sulfone sodium salt was rapidly absorbed, with a mean peak plasma concentration of 2400 ± 169 (SEM) ng/mL occurring at 8 h after oral-mucosal dosing and was about 56% bioavailable compared with the i.v. administration of toltrazuril sulfone in dimethylsulfoxide (DMSO). The relative bioavailability of toltrazuril sulfone suspended in water compared with toltrazuril sulfone sodium salt was 46%, indicating approximately 54% less oral bioavailability of this compound suspended in water. In this study, we also investigated whether this salt formulation of toltrazuril sulfone can be used as a feed additive formulation without significant reduction in oral bioavailability. Our results indicated that toltrazuril sulfone sodium salt is relatively well absorbed when administered with feed with a mean oral bioavailability of 52%. Based on these data, repeated oral administration of toltrazuril sulfone sodium salt with or without feed will yield effective plasma and cerebrospinal fluid (CSF) concentrations of toltrazuril sulfone for the treatment and prophylaxis of EPM and other protozoal diseases of horses and other species. As such, toltrazuril sulfone sodium salt has the potential to be used as feed additive formulations for both the treatment and prophylaxis of EPM and various other apicomplexan diseases.
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Toltrazuril sulfone sodium salt: synthesis, analytical detection, and pharmacokinetics in the horse.
Journal of Veterinary Pharmacology and Therapeutics, 2011Co-Authors: Levent Dirikolu, W. Karpiesiuk, Andreas F. Lehner, Thomas TobinAbstract:Toltrazuril sulfone (ponazuril) is a triazine-based Antiprotozoal Agent with clinical application in the treatment of equine protozoal myeloencephalomyelitis (EPM). In this study, we synthesized and determined the bioavailability of a sodium salt formulation of toltrazuril sulfone that can be used for the treatment and prophylaxis of EPM in horses. Toltrazuril sulfone sodium salt was rapidly absorbed, with a mean peak plasma concentration of 2400 ± 169 (SEM) ng/mL occurring at 8 h after oral-mucosal dosing and was about 56% bioavailable compared with the i.v. administration of toltrazuril sulfone in dimethylsulfoxide (DMSO). The relative bioavailability of toltrazuril sulfone suspended in water compared with toltrazuril sulfone sodium salt was 46%, indicating approximately 54% less oral bioavailability of this compound suspended in water. In this study, we also investigated whether this salt formulation of toltrazuril sulfone can be used as a feed additive formulation without significant reduction in oral bioavailability. Our results indicated that toltrazuril sulfone sodium salt is relatively well absorbed when administered with feed with a mean oral bioavailability of 52%. Based on these data, repeated oral administration of toltrazuril sulfone sodium salt with or without feed will yield effective plasma and cerebrospinal fluid (CSF) concentrations of toltrazuril sulfone for the treatment and prophylaxis of EPM and other protozoal diseases of horses and other species. As such, toltrazuril sulfone sodium salt has the potential to be used as feed additive formulations for both the treatment and prophylaxis of EPM and various other apicomplexan diseases.
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New therapeutic approaches for equine protozoal myeloencephalitis: pharmacokinetics of diclazuril sodium salts in horses.
Veterinary therapeutics : research in applied veterinary medicine, 2006Co-Authors: Levent Dirikolu, W. Karpiesiuk, Andreas F. Lehner, Charlie Hughes, William E. Woods, J. D. Harkins, J. Boyles, Alfonza Atkinson, D.e. Granstrom, Thomas TobinAbstract:Diclazuril is a triazine-based Antiprotozoal Agent which may have clinical application in the treatment of equine protozoal myeloencephalomyelitis (EPM). In this study, the use of the sodium salt diclazuril to increase the apparent bioavailability of diclazuril for the treatment and prophylaxis of EPM and various other Apicomplexan mediated diseases is described. In this study, diclazuril sodium salt was synthesized and administered to horses as diclazuril sodium salt formulations. The absorption, distribution, and clearance of diclazuril sodium salt in the horse are described. Diclazuril was rapidly absorbed, with peak plasma concentrations occurring at 8-24 hours following an oral mucosal administration of diclazuril sodium salt. The mean oral bioavailability of diclazuril as Clinacox was 9.5% relative to oral mucosal administration of diclazuril sodium salt. Additionally, diclazuril in DMSO administered orally was 50% less bioavailable than diclazuril sodium salt following an oral mucosal administration. It was also shown that diclazuril sodium salt has the potential to be used as a feed additive for the treatment and prophylaxis of EPM and various other Apicomplexan mediated diseases.
Gabriel Navarretevazquez - One of the best experts on this subject based on the ideXlab platform.
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synthesis of benzologues of nitazoxanide and tizoxanide a comparative study of their in vitro broad spectrum Antiprotozoal activity
ChemInform, 2011Co-Authors: Gabriel Navarretevazquez, Fabiola Chavezsilva, Rocio Argotteramos, Maria Del Carmen Rodriguezgutierrez, Manuel Jesus Chanbacab, Roberto Cedillorivera, Rosa Moopuc, Emanuel HernandeznunezAbstract:Two new annulated analogues (I) of the Antiprotozoal Agent nitazoxanide (NIT) and its metabolite tizoxanide (TIZ), are prepared using a short synthetic route.
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synthesis of benzologues of nitazoxanide and tizoxanide a comparative study of their in vitro broad spectrum Antiprotozoal activity
Bioorganic & Medicinal Chemistry Letters, 2011Co-Authors: Gabriel Navarretevazquez, Fabiola Chavezsilva, Rocio Argotteramos, Maria Del Carmen Rodriguezgutierrez, Manuel Jesus Chanbacab, Roberto Cedillorivera, Rosa Moopuc, Emanuel HernandeznunezAbstract:Abstract We have synthesized two new benzologues of Nitazoxanide (NIT) and Tizoxanide (TIZ), using a short synthetic route. Both compounds were tested in vitro against six protozoa ( Giardia intestinalis , Trichomonas vaginalis , Entamoeba histolytic a, Plasmodium berghei , Leishmania mexicana and Trypanosoma cruzi ). Compound 1 (benzologue of NIT) showed broad Antiprotozoal effect against all parasites tested, showing IC 50 ’s G. intestinalis. It was 10-times more active than pentamidine against L. mexicana , and it was sevenfold more potent than benznidazole versus T. cruzi . This compound could be considered as a new broad spectrum Antiprotozoal Agent.
W. Karpiesiuk - One of the best experts on this subject based on the ideXlab platform.
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Toltrazuril sulfone sodium salt: synthesis, analytical detection, and pharmacokinetics in the horse.
Journal of Veterinary Pharmacology and Therapeutics, 2011Co-Authors: Levent Dirikolu, W. Karpiesiuk, Andreas F. Lehner, Thomas TobinAbstract:Dirikolu, L., Karpiesiuk, W., Lehner, A. F., Tobin, T. Toltrazuril sulfone sodium salt: synthesis, analytical detection, and pharmacokinetics in the Horse. J. vet. Pharmacol. Therap. 35, 265–274. Toltrazuril sulfone (ponazuril) is a triazine-based Antiprotozoal Agent with clinical application in the treatment of equine protozoal myeloencephalomyelitis (EPM). In this study, we synthesized and determined the bioavailability of a sodium salt formulation of toltrazuril sulfone that can be used for the treatment and prophylaxis of EPM in horses. Toltrazuril sulfone sodium salt was rapidly absorbed, with a mean peak plasma concentration of 2400 ± 169 (SEM) ng/mL occurring at 8 h after oral-mucosal dosing and was about 56% bioavailable compared with the i.v. administration of toltrazuril sulfone in dimethylsulfoxide (DMSO). The relative bioavailability of toltrazuril sulfone suspended in water compared with toltrazuril sulfone sodium salt was 46%, indicating approximately 54% less oral bioavailability of this compound suspended in water. In this study, we also investigated whether this salt formulation of toltrazuril sulfone can be used as a feed additive formulation without significant reduction in oral bioavailability. Our results indicated that toltrazuril sulfone sodium salt is relatively well absorbed when administered with feed with a mean oral bioavailability of 52%. Based on these data, repeated oral administration of toltrazuril sulfone sodium salt with or without feed will yield effective plasma and cerebrospinal fluid (CSF) concentrations of toltrazuril sulfone for the treatment and prophylaxis of EPM and other protozoal diseases of horses and other species. As such, toltrazuril sulfone sodium salt has the potential to be used as feed additive formulations for both the treatment and prophylaxis of EPM and various other apicomplexan diseases.
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Toltrazuril sulfone sodium salt: synthesis, analytical detection, and pharmacokinetics in the horse.
Journal of Veterinary Pharmacology and Therapeutics, 2011Co-Authors: Levent Dirikolu, W. Karpiesiuk, Andreas F. Lehner, Thomas TobinAbstract:Toltrazuril sulfone (ponazuril) is a triazine-based Antiprotozoal Agent with clinical application in the treatment of equine protozoal myeloencephalomyelitis (EPM). In this study, we synthesized and determined the bioavailability of a sodium salt formulation of toltrazuril sulfone that can be used for the treatment and prophylaxis of EPM in horses. Toltrazuril sulfone sodium salt was rapidly absorbed, with a mean peak plasma concentration of 2400 ± 169 (SEM) ng/mL occurring at 8 h after oral-mucosal dosing and was about 56% bioavailable compared with the i.v. administration of toltrazuril sulfone in dimethylsulfoxide (DMSO). The relative bioavailability of toltrazuril sulfone suspended in water compared with toltrazuril sulfone sodium salt was 46%, indicating approximately 54% less oral bioavailability of this compound suspended in water. In this study, we also investigated whether this salt formulation of toltrazuril sulfone can be used as a feed additive formulation without significant reduction in oral bioavailability. Our results indicated that toltrazuril sulfone sodium salt is relatively well absorbed when administered with feed with a mean oral bioavailability of 52%. Based on these data, repeated oral administration of toltrazuril sulfone sodium salt with or without feed will yield effective plasma and cerebrospinal fluid (CSF) concentrations of toltrazuril sulfone for the treatment and prophylaxis of EPM and other protozoal diseases of horses and other species. As such, toltrazuril sulfone sodium salt has the potential to be used as feed additive formulations for both the treatment and prophylaxis of EPM and various other apicomplexan diseases.
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New therapeutic approaches for equine protozoal myeloencephalitis: pharmacokinetics of diclazuril sodium salts in horses.
Veterinary therapeutics : research in applied veterinary medicine, 2006Co-Authors: Levent Dirikolu, W. Karpiesiuk, Andreas F. Lehner, Charlie Hughes, William E. Woods, J. D. Harkins, J. Boyles, Alfonza Atkinson, D.e. Granstrom, Thomas TobinAbstract:Diclazuril is a triazine-based Antiprotozoal Agent which may have clinical application in the treatment of equine protozoal myeloencephalomyelitis (EPM). In this study, the use of the sodium salt diclazuril to increase the apparent bioavailability of diclazuril for the treatment and prophylaxis of EPM and various other Apicomplexan mediated diseases is described. In this study, diclazuril sodium salt was synthesized and administered to horses as diclazuril sodium salt formulations. The absorption, distribution, and clearance of diclazuril sodium salt in the horse are described. Diclazuril was rapidly absorbed, with peak plasma concentrations occurring at 8-24 hours following an oral mucosal administration of diclazuril sodium salt. The mean oral bioavailability of diclazuril as Clinacox was 9.5% relative to oral mucosal administration of diclazuril sodium salt. Additionally, diclazuril in DMSO administered orally was 50% less bioavailable than diclazuril sodium salt following an oral mucosal administration. It was also shown that diclazuril sodium salt has the potential to be used as a feed additive for the treatment and prophylaxis of EPM and various other Apicomplexan mediated diseases.