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Prem M S Chauhan - One of the best experts on this subject based on the ideXlab platform.
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synthesis and biological evaluation of new 1 2 4 triazino 5 6 b indol 3 ylthio 1 3 5 Triazines and 1 2 4 triazino 5 6 b indol 3 ylthio pyrimidines against leishmania donovani
European Journal of Medicinal Chemistry, 2010Co-Authors: Leena Gupta, Saumya Srivastava, Neena Goyal, Naresh Sunduru, Suman Gupta, Aditya Verma, Prem M S ChauhanAbstract:Abstract A series of [1,2,4]triazino[5,6-b]indol-3-ylthio-1,3,5-Triazines and [1,2,4]triazino[5,6-b]indol-3-ylthio-pyrimidines were synthesized and screened for their in vitro antileishmanial activity against Leishmania donovani. Among all, 8 compounds have shown more than 90% inhibition against promastigotes and IC50 in the range of 4.01–57.78 μM against amastigotes. Compound 5, a triazino[5,6-b]indol-3-ylthio-1,3,5-Triazine derivative was found to be the most active and least toxic with 20- & 10-fold more selectivity (S.I. = 56.61) as compared to that of standard drugs pentamidine and sodium stibogluconate (SSG), respectively.
Leena Gupta - One of the best experts on this subject based on the ideXlab platform.
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synthesis and biological evaluation of new 1 2 4 triazino 5 6 b indol 3 ylthio 1 3 5 Triazines and 1 2 4 triazino 5 6 b indol 3 ylthio pyrimidines against leishmania donovani
European Journal of Medicinal Chemistry, 2010Co-Authors: Leena Gupta, Saumya Srivastava, Neena Goyal, Naresh Sunduru, Suman Gupta, Aditya Verma, Prem M S ChauhanAbstract:Abstract A series of [1,2,4]triazino[5,6-b]indol-3-ylthio-1,3,5-Triazines and [1,2,4]triazino[5,6-b]indol-3-ylthio-pyrimidines were synthesized and screened for their in vitro antileishmanial activity against Leishmania donovani. Among all, 8 compounds have shown more than 90% inhibition against promastigotes and IC50 in the range of 4.01–57.78 μM against amastigotes. Compound 5, a triazino[5,6-b]indol-3-ylthio-1,3,5-Triazine derivative was found to be the most active and least toxic with 20- & 10-fold more selectivity (S.I. = 56.61) as compared to that of standard drugs pentamidine and sodium stibogluconate (SSG), respectively.
Michael J Lydy - One of the best experts on this subject based on the ideXlab platform.
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Joint Toxicity of Triazine Herbicides and Organophosphate Insecticides to the Midge Chironomus tentans
Archives of Environmental Contamination and Toxicology, 2005Co-Authors: L. J. Schuler, A. J. Trimble, Jason B Belden, Michael J LydyAbstract:A series of recent studies demonstrated that the Triazine herbicide atrazine, although not itself acutely toxic, potentiated the toxicity of certain organophosphate insecticides (OPs) to the midge Chironomus tentans . In the current study, a series of Triazine herbicides and Triazine herbicide degradation products were tested to determine if other Triazines potentiate OP toxicity to midges. Chlorpyrifos and diazinon were the OPs tested. Toxicity tests were conducted using a factorial design and analysis of variance to statistically determine if each Triazine had an effect on expected toxicity. Log-probit procedures were also used to evaluate the magnitude of change in median effective concentration (EC_50) values during coexposure with each Triazine. All of the Triazine herbicides tested (atrazine, simazine, cyanazine, and hexazinone) were capable of potentiating the toxicity of the OPs, whereas the degradation products ( s -Triazine, deethylatrazine, and deisopropylatrazine) had less effect. In most cases, a Triazine concentration of 100 μg/L was necessary to significantly increase OP toxicity, and higher concentrations of Triazine caused a greater degree of potentiation. Changes in EC_50 values ranged from no change to a 2.5-fold increase in toxicity. Generally, EC_50 values changed by less than a factor of 2, indicating that the effect may be of limited concern in regard to future risk assessments of OPs.
Aditya Verma - One of the best experts on this subject based on the ideXlab platform.
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synthesis and biological evaluation of new 1 2 4 triazino 5 6 b indol 3 ylthio 1 3 5 Triazines and 1 2 4 triazino 5 6 b indol 3 ylthio pyrimidines against leishmania donovani
European Journal of Medicinal Chemistry, 2010Co-Authors: Leena Gupta, Saumya Srivastava, Neena Goyal, Naresh Sunduru, Suman Gupta, Aditya Verma, Prem M S ChauhanAbstract:Abstract A series of [1,2,4]triazino[5,6-b]indol-3-ylthio-1,3,5-Triazines and [1,2,4]triazino[5,6-b]indol-3-ylthio-pyrimidines were synthesized and screened for their in vitro antileishmanial activity against Leishmania donovani. Among all, 8 compounds have shown more than 90% inhibition against promastigotes and IC50 in the range of 4.01–57.78 μM against amastigotes. Compound 5, a triazino[5,6-b]indol-3-ylthio-1,3,5-Triazine derivative was found to be the most active and least toxic with 20- & 10-fold more selectivity (S.I. = 56.61) as compared to that of standard drugs pentamidine and sodium stibogluconate (SSG), respectively.
Saumya Srivastava - One of the best experts on this subject based on the ideXlab platform.
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synthesis and biological evaluation of new 1 2 4 triazino 5 6 b indol 3 ylthio 1 3 5 Triazines and 1 2 4 triazino 5 6 b indol 3 ylthio pyrimidines against leishmania donovani
European Journal of Medicinal Chemistry, 2010Co-Authors: Leena Gupta, Saumya Srivastava, Neena Goyal, Naresh Sunduru, Suman Gupta, Aditya Verma, Prem M S ChauhanAbstract:Abstract A series of [1,2,4]triazino[5,6-b]indol-3-ylthio-1,3,5-Triazines and [1,2,4]triazino[5,6-b]indol-3-ylthio-pyrimidines were synthesized and screened for their in vitro antileishmanial activity against Leishmania donovani. Among all, 8 compounds have shown more than 90% inhibition against promastigotes and IC50 in the range of 4.01–57.78 μM against amastigotes. Compound 5, a triazino[5,6-b]indol-3-ylthio-1,3,5-Triazine derivative was found to be the most active and least toxic with 20- & 10-fold more selectivity (S.I. = 56.61) as compared to that of standard drugs pentamidine and sodium stibogluconate (SSG), respectively.