The alliance of new drug, green technology and public health initiatives is essential for the eco... more The alliance of new drug, green technology and public health initiatives is essential for the ecosystem. The microwave technique is used to synthesize new drugs cognate to metronidazole. A new family of triethoxysilanes (3a–3e) was synthesized after reconnaissance with terminal alkynes (2a–2e) as an array using the Huisgen 1,3‐dipolar cycloaddition. All products were obtained in excellent yield with recovery of the catalyst as well as the solvent, and in a short time span. The design feature of these compounds is the tailoring of two unsymmetrical triazole nuclei into a single scaffold. The pharmacokinetic profiles of the triazole scaffold were analyzed using MOLINSPIRATION and ADMET toolkits, which gave promising results that prompted the investigation of these compounds for anti‐parasitic activity against parasites (Giardia lamblia and Trichomonas vaginalis) in contrast to standard drug (metronidazole). Compound 3d manifested good efficacy against both strains amongst all the synthesized triazole analogs.Highlights By using microwave methodology, a series of triazole functionalized alkynes and triazole organo silanes were synthesized. This involves tailoring of the 1,2,4‐triazole nucleus to 1,2,3‐triazole moiety. The protocol afforded excellent yield in a short time span under eco‐friendly conditions. The hybrid molecules were screened for their physicochemical properties using MOLINSPIRATION software and ADMET web server. All the synthesized compounds were investigated for their antioxidant activity, anti‐giardial and anti‐trichomonal activities. Tris triazole silane (3d) was found to be the most significant against Giardia lamblia and Trichomonas vaginalis, respectively, and this low‐price, versatile drug will hopefully lead to the eventual elimination of parasitic disease from the human population. Thermal gravimetric analysis has been performed for compounds (2a–2e) and (3a–3e).
The known silatranes have attached substituents such as hydrogen, organyl, organoxy, aminoalkyl, ... more The known silatranes have attached substituents such as hydrogen, organyl, organoxy, aminoalkyl, thioorganyl, acyloxy, halogen, pseudohalogen, and other groups; however, their functionalization with any polycyclic aromatic hydrocarbon substituent is not recognized; this creates a niche in silatrane chemistry.
Chemical contaminants such as industrial and urban by-products, pharmaceuticals, drugs metabolite... more Chemical contaminants such as industrial and urban by-products, pharmaceuticals, drugs metabolites and, plastics, are continuously found in the oceans, affecting its quality and organism's welfare. Although these compounds are found at concentrations ranged ng L-1, there is an increasing concern about the potential adverse effects of the interactions among those substances present, simultaneously, in a mixture. In the present study, specimens of sea bream (Sparus aurata) were exposed, by food, to rising concentrations of a mixture of carbamazepine, polybrominated diphenyl ether-47 and cadmium chloride, for 15 days and then, maintained, with the same control diet, without contaminants, for other 15 days. Samples of skin mucus, serum, head-kidney, liver and intestine were sampled at 0, 15 and 30 days. Cellular immune parameters were evaluated on head-kidney, as well as humoral parameters were determined on skin mucus and serum. In addition, the expression of some genes, related to immunity, was analysed on liver and intestine. Both cellular and humoral response were affected at 15 days, showing slightly signs of recovery at 30 days. Besides, the expression of immune-related genes was highly affected, suggesting the development of inflammatory processes, as well as a reduction of immune parameters. Overall, the mixture of compounds severally affected the immune system of sea bream, suggesting a lower degree of recovery. The prolonged exposure to a mixture of these compounds could entail serious change on population immunity and, eventually, promote changes on marine biota.
The alliance of new drug, green technology and public health initiatives is essential for the eco... more The alliance of new drug, green technology and public health initiatives is essential for the ecosystem. The microwave technique is used to synthesize new drugs cognate to metronidazole. A new family of triethoxysilanes (3a–3e) was synthesized after reconnaissance with terminal alkynes (2a–2e) as an array using the Huisgen 1,3‐dipolar cycloaddition. All products were obtained in excellent yield with recovery of the catalyst as well as the solvent, and in a short time span. The design feature of these compounds is the tailoring of two unsymmetrical triazole nuclei into a single scaffold. The pharmacokinetic profiles of the triazole scaffold were analyzed using MOLINSPIRATION and ADMET toolkits, which gave promising results that prompted the investigation of these compounds for anti‐parasitic activity against parasites (Giardia lamblia and Trichomonas vaginalis) in contrast to standard drug (metronidazole). Compound 3d manifested good efficacy against both strains amongst all the synthesized triazole analogs.Highlights By using microwave methodology, a series of triazole functionalized alkynes and triazole organo silanes were synthesized. This involves tailoring of the 1,2,4‐triazole nucleus to 1,2,3‐triazole moiety. The protocol afforded excellent yield in a short time span under eco‐friendly conditions. The hybrid molecules were screened for their physicochemical properties using MOLINSPIRATION software and ADMET web server. All the synthesized compounds were investigated for their antioxidant activity, anti‐giardial and anti‐trichomonal activities. Tris triazole silane (3d) was found to be the most significant against Giardia lamblia and Trichomonas vaginalis, respectively, and this low‐price, versatile drug will hopefully lead to the eventual elimination of parasitic disease from the human population. Thermal gravimetric analysis has been performed for compounds (2a–2e) and (3a–3e).
The known silatranes have attached substituents such as hydrogen, organyl, organoxy, aminoalkyl, ... more The known silatranes have attached substituents such as hydrogen, organyl, organoxy, aminoalkyl, thioorganyl, acyloxy, halogen, pseudohalogen, and other groups; however, their functionalization with any polycyclic aromatic hydrocarbon substituent is not recognized; this creates a niche in silatrane chemistry.
Chemical contaminants such as industrial and urban by-products, pharmaceuticals, drugs metabolite... more Chemical contaminants such as industrial and urban by-products, pharmaceuticals, drugs metabolites and, plastics, are continuously found in the oceans, affecting its quality and organism's welfare. Although these compounds are found at concentrations ranged ng L-1, there is an increasing concern about the potential adverse effects of the interactions among those substances present, simultaneously, in a mixture. In the present study, specimens of sea bream (Sparus aurata) were exposed, by food, to rising concentrations of a mixture of carbamazepine, polybrominated diphenyl ether-47 and cadmium chloride, for 15 days and then, maintained, with the same control diet, without contaminants, for other 15 days. Samples of skin mucus, serum, head-kidney, liver and intestine were sampled at 0, 15 and 30 days. Cellular immune parameters were evaluated on head-kidney, as well as humoral parameters were determined on skin mucus and serum. In addition, the expression of some genes, related to immunity, was analysed on liver and intestine. Both cellular and humoral response were affected at 15 days, showing slightly signs of recovery at 30 days. Besides, the expression of immune-related genes was highly affected, suggesting the development of inflammatory processes, as well as a reduction of immune parameters. Overall, the mixture of compounds severally affected the immune system of sea bream, suggesting a lower degree of recovery. The prolonged exposure to a mixture of these compounds could entail serious change on population immunity and, eventually, promote changes on marine biota.
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Papers by Cristobal Espinosa