Incorporation of an adamantyl group in prototypical soluble expoxide hydrolase (sEH) inhibitors afforded improved enzyme potency. We explored replacement of the adamantyl group in unsymmetrical ureas and amides with substituted aryl rings to identify equipotent and metabolically stable sEH inhibitors. We found that aryl rings, especially those substituted in the para position with a strongly electron withdrawing substituent, afforded enzyme IC(50) values comparable to the adamantyl compounds in an ether substituted, unsymmetrical N,N'-diaryl urea or amide scaffold.
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http://dx.doi.org/10.1016/j.bmcl.2009.05.102 | DOI Listing |
Biomol Concepts
January 2025
Division of Pharmacology, School of Medical and Life Sciences, Sunway University, No. 5, Jalan Universiti, Bandar Sunway, 47500 Selangor Darul Ehsan, Malaysia.
Seaweeds have been utilized as food, fodder, fertilizer, and medicine since ancient times; nevertheless, they have received only a little attention. In the current work, we extracted the sulfated polysaccharide from a marine source and investigated its anti-arthritic potential . The isolated and freeze-dried polysaccharide was tested for acute oral toxicity based on OECD 423.
View Article and Find Full Text PDFAfr J Prim Health Care Fam Med
December 2024
Department of Anaesthesiology, Pharmacology and Therapeutics, Faculty of Medicine, University of British Columbia, Vancouver.
In older adults with type 2 diabetes (T2DM), tight glycaemic control (HbA1c 7%) can result in more harm than benefit, especially when using insulin or sulfonylureas. Older adults are at higher risk for adverse drug events, especially hypoglycaemia, which may cause falls, confusion and hospitalisations. This Therapeutic Letter evaluates the risks of tight glycaemic control in older adults with T2DM, focusing on deprescribing diabetes medications in those over 65, especially those with multimorbidity and polypharmacy.
View Article and Find Full Text PDFMedComm (2020)
February 2025
Chronic kidney disease (CKD) is a disease that affects more than 850 million people. Acute kidney injury (AKI) is a common cause of CKD, and blocking the AKI-CKD transition shows promising therapeutic potential. Herein, we found that butyrolactone I (BLI), a natural product, exerts significant nephroprotective effects, including maintenance of kidney function, inhibition of inflammatory response, and prevention of fibrosis, in both folic acid- and ureteral obstruction-induced AKI-CKD transition mouse models.
View Article and Find Full Text PDFStem Cells Int
January 2025
Transplant Research Center, Shiraz University of Medical Sciences, Shiraz, Iran.
Renal dysfunction due to ischemia-reperfusion injury (IRI) is a common problem after kidney transplantation. In recent years, studies on animal models have shown that exosomes derived from mesenchymal stem cells (MSC-Exo) play an important role in treating acute kidney injury (AKI) and promoting tissue repair. The microneedle patch provides a noninvasive and targeted delivery system for exosomes.
View Article and Find Full Text PDFHeliyon
January 2025
Department of Surgery and Obstetrics, Faculty of Veterinary Science, Bangladesh Agricultural University, Mymensingh, 2202, Bangladesh.
Electrosurgery (ES) offers a promising alternative to conventional steel scalpel surgery (SSS), providing superior hemorrhage control and efficient tissue dissection with minimal invasiveness. Given the limited literature, this study aims to compare the clinical efficacy of ES with that of SSS in bovine umbilical herniorrhaphy. Fourteen crossbred male calves with reducible umbilical hernias, aged less than one month and weighing 25-47 kg, were randomly assigned to two experimental groups: group A (ES) and group B (SSS), each containing seven calves.
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