70458-49-0Relevant academic research and scientific papers
Synthetic Guaiacol Derivatives as Promising Myeloperoxidase Inhibitors Targeting Atherosclerotic Cardiovascular Disease
Premkumar, Jayaraj,Sampath, Parthasarathy,Sanjay, Rajagopalan,Chandrakala, Aluganti,Rajagopal, Desikan
supporting information, p. 1187 - 1199 (2020/05/25)
Myeloperoxidase (MPO) is known to cause oxidative stress and inflammation leading to cardiovascular disease (CVD) complications. MPO-mediated oxidation of lipoproteins leads to dysfunctional entities altering the landscape of lipoprotein functionality. The specificity of guaiacol derivatives toward preventing MPO-mediated oxidation to limit MPO's harmful effects is unknown. Diligent in silico studies were accomplished for a portfolio of compounds with guaiacol as a building block. The compounds’ activity toward MPO inhibition was also validated. The role of these chemical entities in controlling MPO-mediated oxidation of lipoproteins (LDL and HDL) was shown to agree with our approach of developing powerful MPO inhibitors. The mechanism of MPO inhibition was demonstrated to be reversible in nature. This study reveals that there is great potential for guaiacol derivatives as therapeutics for CVD by modulating lipid profiles, reducing atherosclerotic plaque burden, and subsequently optimizing cardiovascular functions.
Compounds and their use to treat diabetes and related disorders
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Page/Page column 15, (2008/06/13)
The invention relates generally to compounds described herein. More specifically, the invention relates to compounds and pharmaceutical compositions containing such compounds. Methods of the invention comprise administration of a compound of the invention
Comparative inhibitory effects of niflumic acid and novel synthetic derivatives on the rat isolated stomach fundus
Criddle,Meireles,MacEdo,Leal-Cardoso,Scarparo,Jaffar
, p. 283 - 288 (2007/10/03)
Novel derivatives of 2-[3-(trifluoromethyl)-analino]nicotinic acid (niflumic acid) were synthesized. The compounds were compared for their inhibitory effects on 5-hydroxytryptamine (5-HT)- and KCl-induced contraction of the rat fundus. The aim was to assess structure-activity relationships regarding the selectivity and potency of these compounds. Niflumic acid (1-100 μM) concentration-dependently inhibited 5-HT-induced tonic contractions with an IC50 value (concentration reducing the control contractile response by 50%, calculated from semi-log graphs) of 0.24 × 10-4 M (n = 9). In contrast, it was significantly less potent at inhibiting KCl-induced responses (IC50 = 1.49 × 10-4 M, n = 9). The methyl ester (NFAme) and amido (NFAm) analogues showed no selectivity between 5-HT- and KCl-induced contractions with IC50 values of 1.64 × 10-4 M (n = 8) and 1.87 × 10-4 M (n = 9) for 5-HT responses, and 2.61 × 10-4 M (n = 8) and 2.55 × 10-4 M (n = 7) for KCl-induced responses, respectively. Our results suggest that alteration of the carboxylic acid moiety of niflumic acid reduces the selectivity and potency of its inhibitory action on 5-HT-induced contractile responses of the rat fundus, possibly via a reduced interaction with calcium-activated chloride channels.
