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Biocatalyzed Synthesis of Antidiabetic Drugs
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Glitazones, PPAR-γ agonists, are one of the earlier drugs used for treatment of T2DM (Nanjan et al., 2018). Ciglitazone (2a, Fig. 11.11) was discovered by Takeda in 1982, but rapidly discontinued (Gale, 2001). Troglitazone 2b was approved by FDA for T2DM in 1997, but after 6 weeks of its launch by Glaxo Welcome was withdrawn due to hepatotoxicity, and finally retired in 2000 (Nanjan et al., 2018). There are three marketed TZDs: pioglitazone (2c, Actos™ or Glustin™, Takeda Pharma USA and Eli Lilly), rosiglitazone (2d, Avandia™, GlaxoSmithKline), and lobeglitazone (2e, Duvie™, Chong Kun Dang), whose chemical structures are shown in Fig. 11.11. There are concerns about cardiovascular risks associated to rosiglitazone 2d, so that FDA placed some restrictions on it use, while EMA (European Medicine Agency) recommended its suspension from the market (Nanjan et al., 2018). On the other hand, the risk of developing bladder cancer associated to the use of pioglitazone 2c has been also reported (Shukla and Kalra, 2011). Lobeglitazone 2e was approved by the Ministry of Food and Drug Safety of Korea in 2013 (Lee et al., 2015), although the postmarketing surveillance is planned to finish in 2019. Chemical structure of glitazones.
Outdoor Air Pollution
Published in William J. Rea, Kalpana D. Patel, Reversibility of Chronic Disease and Hypersensitivity, Volume 4, 2017
William J. Rea, Kalpana D. Patel
Other data that may prove helpful in weighing the merits of the schools of oxidative shielding versus OS are the results of clinical trials in which a therapy recommended by the shielding school, for example, diet and exercise (which is known to stimulate ROS234), is directly compared with conventional medical intervention. When this is done in type 2 diabetes and its prodromal metabolic syndrome, diet and exercise are categorically superior to the best drug intervention. A recent meta-analysis of 13 clinical trials involving 3907 subjects found that the odds ratio for disease improvement with diet and exercise was 3.8 (95% CI = 2.5−5.9), but the odds ratios for disease improvement with drug treatment was 1.6 (95% CI = 1.0−2.5).235 Diet and exercise can actually cure early type 2 diabetes while simultaneously reducing the risk of heart disease. In contrast, common drug interventions such as the thiazolidinedione insulin-sensitizing drug rosiglitazone will decrease diabetes, but increase the risk of heart failure.236
Lipase-Mediated Biocatalysis as a Greener and Sustainable Choice for Pharmaceutical Processes
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2020
Monika Sharma, Tanya Bajaj, Rohit Sharma
Peroxisome proliferator-activated receptors (PPARs) agonists are involved in the metabolic regulation of lipid and lipoprotein, blood glucose, and abdominal adiposity. They are classified as a, β, and γ subtypes. PPAR alpha agonists primarily act by decreasing the serum triglyceride levels and increasing high-density lipid cholesterol (HDLc) levels. They also tend to improve glucose tolerance in type 2 diabetic patients, whereas the PPAR gamma agonists also called the insulin sensitizers such as pioglitazone and rosiglitazone affect the type 2 diabetes patients by improving the insulin sensitivity, glucose tolerance and decreasing blood glucose levels.
Implications of peroxisome proliferator-activated receptor gamma (PPARY) with the intersection of organophosphate flame retardants and diet-induced obesity in adult mice
Published in Journal of Toxicology and Environmental Health, Part A, 2022
Gwyndolin M. Vail, Sabrina N. Walley, Ali Yasrebi, Angela Maeng, Thomas J. Degroat, Kristie M. Conde, Troy A. Roepke
PPARγ is expressed within subpopulations of neurons termed neuropeptide Y (NPY) and proopiomelanocortin (POMC) neurons within the arcuate (ARC) nucleus of the hypothalamus. These neurons act as integral central regulators of ingestive behavior and energy expenditure (Garretson et al. 2015; Sarruf et al. 2009). Highlighting the importance of PPARγ in these pathways, Garretson et al. (2015) reported that centrally administered rosiglitazone induced ingesting and hoarding behaviors in male mice and hamsters that is abolished with targeted knockout of PPARγ within POMC neurons (Stump et al. 2016). In addition, brain-specific PPARγKO mice also exhibit resistance to diet-induced obesity (Lu et al. 2011).
Ni@zeolite-Y nanoporous; a valuable and efficient nanocatalyst for the synthesis of N-benzimidazole-1,3-thiazolidinones
Published in Green Chemistry Letters and Reviews, 2018
Mehdi Kalhor, Soodabeh Banibairami, Seyed Ahmad Mirshokraie
By having nitrogen and sulfur atoms in a five-membered ring, 1,3-Thiazolidin-4-ones are belonging to heterocyclic compounds that can be found as a core structure in the natural and synthetic pharmaceutical, agricultural compounds and displaying a broad spectrum of biological activities (1, 2). Also, some important derivatives of thiazolidinone, such as Rosiglitazone and Pioglitazone, are known marketed drugs with hypoglycemic action to treat diabetes (Scheme 1) (3).