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1.
Pakistan Journal of Pharmaceutical Sciences. 2018; 31 (3 Supp.): 1067-1074
em Inglês | IMEMR | ID: emr-198718

RESUMO

Hypertension is one of cardiovascular disease that is not sufficiently prevented and controlled at both hospital and community levels. Hypertension resulted in significant morbidity and mortality. The benz-imidazole ring is very important pharmacophore in modern drug discovery. The substituted benzimidazoles are the important for medicinal research. Researchers have reported that substituted Benzimidazoles are the structural isosteres of nucleotides, and easily allow them to interact with the different biopolymers, possess pharmacological activity especially antihypertensive activity. Angiotensin II Receptor Antagonists/Blockers [ARBs] compete with angiotensin II at the receptor site and block the contractile effect of angiotensin II in all vascular smooth muscles. Among all Angiotensin II Receptor Antagonists/Blockers [ARBs], Telmisartan, Milfasartan and many others have benzimidazole ring in their structure. In this study Angiotensin II Receptor Antagonists/Blockers [ARBs] have been prepared. Synthesized compounds were characterized by physical data and FTIR spectroscopic technique. Synthesized compounds studied were finally screened for their antihypertensive activity by tail cuff method of measurement of blood pressure by NIBP apparatus [None Invasive Blood Pressure] using Chart 5.0 software. The compounds synthesized were 2-[3-nitrophenyl]-1Hbenzimidazole [1a], 3-[1H benzimidazol-2-yl]aniline [1b] and 5-[1H-benzimidazol-2-yl]-2-methoxyphenol [1c]. The synthesized compounds have shown antihypertensive activity by taking Losartan as lead compound

2.
Pakistan Journal of Pharmaceutical Sciences. 2018; 31 (4 [Supp.]): 1463-1467
em Inglês | IMEMR | ID: emr-199536

RESUMO

Thallium has been shown to significantly influence various tissues of living organisms; Exposure to Thallium can disturb mitochondrial function, degenerate neurons, and interfere with the function of critical metabolic enzymes and co-enzymes. Glutathione [GSH] an essential biomarker is considered a key factor in harnessing the thallium toxicity. In the present study the interaction of Thallium [Thallium Chloride] and glutathione was investigated spectro- photometrically in aqueous media. The renowned Elman's experimental protocol was followed at a wavelength of 412nm for Glutathione quantification in each sample. The pH of each sample was maintained at 7.6 using Phosphate buffer during the entire course of the experiment. A concentration as well as time dependent depletion of glutathione after exposure to various concentration of Thallium metal was observed, revealing chemical interaction between the metal and glutathione. The exact mechanism of interaction of Thallium and glutathione is still to be investigated. However, this piece of research suggests that a decrease in the concentration of Glutathione may be due to Thallium-GSH abduct or oxidize glutathione [GSSG] formation. This study was performed in-vitro as a model of in vivo

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