Synthesis, Anti‐Inflammatory Activity, and COX‐1/2 Inhibition Profile of Some Novel Non‐Acidic Polysubstituted Pyrazoles and Pyrano[2,3‐c]pyrazoles
Sign Up to like & getrecommendations! Published in 2017 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.201700025
Abstract: The synthesis and evaluation of the anti‐inflammatory activity of some structure hybrids comprising basically the 5‐hydroxy‐3‐methyl‐1‐phenyl‐4‐substituted‐1H‐pyrazole scaffold directly linked to a variety of heterocycles and functionalities, or annulated as pyrano[2,3‐c]pyrazoles, is described. According to the… read more here.
Keywords: anti inflammatory; cox inhibition; cox; activity ... See more keywords
Synthesis and discovery of pyrazolo-pyridine analogs as inflammation medications through pro- and anti-inflammatory cytokine and COX-2 inhibition assessments.
Sign Up to like & getrecommendations! Published in 2019 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2019.103484
Abstract: This article briefs about the efforts taken to synthesis, characterize and develop (E)-5-methyl-2-phenyl-3-(thiophen-2-yl)-7-(thiophen-2-ylmethylene)-3,3a,4,5,6,7-hexahydro-2H-pyrazolo[4,3-c]pyridine and their analogs. In the two-step reaction, the first step is the synthesis of (3Z,5E)-1-methyl-3,5-bis(thiophen-2-ylmethylene)piperidin-4-one derivatives (3a-l) by stirring the mixture of… read more here.
Keywords: anti inflammatory; pyrazolo pyridine; cox inhibition; pyrazolo ... See more keywords
Effects of endothelin receptor blockade and COX inhibition on intestinal I/R injury in a rat model: Experimental research.
Sign Up to like & getrecommendations! Published in 2020 at "International journal of surgery"
DOI: 10.1016/j.ijsu.2020.08.061
Abstract: BACKGROUND Intestinal ischemia is a highly morbid and mortal condition with no specific treatment. The present study aimed to investigate the effects of cyclooxygenase (COX) inhibition synchronized with nitric oxide (NO) release and endothelin (ET)… read more here.
Keywords: receptor blockade; treatment; endothelin receptor; intestinal injury ... See more keywords
Identification of plant metabolite classes from Waltheria Indica L. extracts regulating inflammatory immune responses via COX-2 inhibition.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of ethnopharmacology"
DOI: 10.1016/j.jep.2020.113741
Abstract: ETHNOPHARMACOLOGICAL RELEVANCE Waltheria Indica L. is traditionally used in Africa, South America and Hawaii to treat pain, anemia, diarrhea, epilepsy and inflammatory related diseases. AIM OF THE STUDY This study aimed to identify extraction parameters… read more here.
Keywords: waltheria indica; inhibition; cox inhibition; concentration ... See more keywords
Endothelium-dependent and cyclooxygenase-dependent cutaneous vasodilatation is blunted in young men with hypertensive parents
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Hypertension"
DOI: 10.1097/hjh.0000000000001794
Abstract: Background: Across ethnicities, offspring of hypertensive parents (OH) have higher risk of hypertension than offspring of normotensive parents (ON). Sympathetic hyperactivity and reduced nitric oxide availability have been reported in normotensive OH; but the role… read more here.
Keywords: reactive hyperaemia; hypertensive parents; perf units; blunted young ... See more keywords
Physiologically based modelling of the antiplatelet effect of aspirin: A tool to characterize drug responsiveness and inform precision dosing
Sign Up to like & getrecommendations! Published in 2022 at "PLoS ONE"
DOI: 10.1371/journal.pone.0268905
Abstract: A computational approach involving mathematical modeling and in silico experiments was used to characterize the determinants of extent and duration of platelet cyclooxygenase (COX)-1 inhibition by aspirin and design precision dosing in patients with accelerated… read more here.
Keywords: precision dosing; cox inhibition; physiologically based; drug ... See more keywords
Crystallography, Molecular Modeling, and COX-2 Inhibition Studies on Indolizine Derivatives
Sign Up to like & getrecommendations! Published in 2021 at "Molecules"
DOI: 10.3390/molecules26123550
Abstract: The cyclooxygenase-2 (COX-2) enzyme is an important target for drug discovery and development of novel anti-inflammatory agents. Selective COX-2 inhibitors have the advantage of reduced side-effects, which result from COX-1 inhibition that is usually observed… read more here.
Keywords: molecular modeling; energy; inhibition; cox ... See more keywords
COX-2 inhibition in the endothelium induces glucose metabolism normalization and impairs tumor progression
Sign Up to like & getrecommendations! Published in 2018 at "Molecular Medicine Reports"
DOI: 10.3892/mmr.2017.8270
Abstract: Previous antitumor angiogenesis strategies have focused on targeting angiogenic signals. Encouragingly, the metabolism of tumor endothelial cells (TECs) has gained attention as a therapeutic target in recent years. There is consensus that, in terms of… read more here.
Keywords: normalization; glucose metabolism; cox inhibition; tumor ... See more keywords