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1.
Bioorg Med Chem ; 27(1): 188-195, 2019 01 01.
Artigo em Inglês | MEDLINE | ID: mdl-30522900

RESUMO

A series of ferrocene appended chalcone allied triazole coupled organosilatranes (FCTSa 7-FCTSa 12) were synthesised with the aim of amalgamating the pharmacological action of the constituting moieties into a single molecular scaffold. All the synthesised silatranes were well characterized by various spectroscopic techniques like IR, 1H NMR, 13C NMR and elemental analysis. Organosilatranes were then evaluated for their biological alacrity against bacterial and fungal strains compared with the standard drugs Rifampicin and Amphotericin B respectively. The ferrocene conjugates were found to be only moderately effective against the tested microbes. However, the organosilatranes conceded excellent efficacy against parasite G. lamblia with FCTSa 11 arraying the leading results. On the other hand against another parasite T. vaginalis, FCTSa 8 has emerged as an outstanding composite. Further, Total Antioxidant Assay (TAA) with 2,2'-azino-bis-3-(ethylbenzothiazoline-6-sulphonic acid) revealed FCTSa 10 to be the best claimant for radical scavenging activity. Along these lines, introducing some different substituents in the synthesised hybrids may act as a useful strategy for increasing the biological profile of the drugs.


Assuntos
Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Chalconas/farmacologia , Compostos Ferrosos/farmacologia , Compostos de Organossilício/farmacologia , Triazóis/farmacologia , Anti-Infecciosos/síntese química , Anti-Infecciosos/química , Antioxidantes/síntese química , Antioxidantes/química , Bactérias/efeitos dos fármacos , Células CACO-2 , Candida/efeitos dos fármacos , Chalconas/síntese química , Chalconas/química , Compostos Ferrosos/síntese química , Compostos Ferrosos/química , Giardia lamblia/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana , Compostos de Organossilício/síntese química , Compostos de Organossilício/química , Testes de Sensibilidade Parasitária , Triazóis/síntese química , Triazóis/química , Trichomonas vaginalis/efeitos dos fármacos
2.
J Sci Food Agric ; 98(13): 5129-5133, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-29635793

RESUMO

BACKGROUND: The present investigation reports the stimulating effects of different substituted alkyl silatranes (3a-3e) on the early seedling growth of wheat (Triticum aestivum) and maize (Zea mays). Seeds of these plants were exposed to six different concentrations (0, 10, 50, 100, 200 and 500 µmol L-1 ). The results revealed that different substitutions (3a-3e) had different effects on root and shoot elongation. Silatranes (3a-3e) were synthesized employing microwave irradiation by a solvent-mediated transesterification reaction, thereby reducing reaction times from several hours under conventional reflux conditions to 15 min under microwave irradiation. RESULTS: It was of interest that the effect of these silatranes did not show a dose-dependent relationship but an optimum concentration, which was 100 µmol L-1 for maize and 200 µmol L-1 for wheat. γ-Aminopropyl silatranes (3b and 3e) gave the best results in maize, whereas γ-chloropropyl silatrane (3a) was most efficient for wheat at these optimum concentrations. CONCLUSION: All the synthesized silatranes were effective in promoting root and shoot growth of wheat and maize. Furthermore, an efficient green microwave methodology was successful for the synthesis of silatranes. These observations pave the way for silatranes as efficient plant growth regulators for crops. © 2018 Society of Chemical Industry.


Assuntos
Compostos Bicíclicos Heterocíclicos com Pontes/farmacologia , Compostos de Organossilício/farmacologia , Reguladores de Crescimento de Plantas/farmacologia , Raízes de Plantas/crescimento & desenvolvimento , Brotos de Planta/crescimento & desenvolvimento , Triticum/efeitos dos fármacos , Zea mays/efeitos dos fármacos , Compostos Bicíclicos Heterocíclicos com Pontes/síntese química , Compostos de Organossilício/síntese química , Reguladores de Crescimento de Plantas/síntese química , Raízes de Plantas/efeitos dos fármacos , Brotos de Planta/efeitos dos fármacos , Triticum/crescimento & desenvolvimento , Zea mays/crescimento & desenvolvimento
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