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Recent Developments in Therapies and Strategies Against COVID-19
Published in Hanadi Talal Ahmedah, Muhammad Riaz, Sagheer Ahmed, Marius Alexandru Moga, The Covid-19 Pandemic, 2023
Misbah Hameed, M. Zia-Ul-Haq, Marius Moga
The thiazolidinediones are known as glitazones after ciglitazone, the prototypical drug of this class. These are heterocyclic compounds with a five-membered C3NS ring. The group was introduced in the late 1990s and is used in the treatment of diabetes mellitus type 2. Thiazolidinedione has shown efficiency against pulmonary disease induced by respiratory syncytial virus (RSV) or H1N1 influenza infection; however, their role in COVID-19 treatment is still not explored [72]. Thiazolidinediones upregulate ACE2 receptor, which is a binding target for COVID-19 virus in host cells. More studies and clinical trials are needed to establish any efficacy of this group against COVID-19 disease.
Medical Therapies
Published in Nazar N. Amso, Saikat Banerjee, Endometriosis, 2022
Simone Ferrero, Fabio Barra, Giulio Evangelisti, Matteo Tantari
Thiazolidinediones target peroxisome proliferator-activated-γ (PPAR-γ) receptors, which are involved in cell growth, angiogenesis and have anti-inflammatory activity (159). In the animal model, the treatment with rosiglitazone, pioglitazone, and ciglitazone reduced growth of established endometriotic implants in comparison to controls (159–162).
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 Troglitazone 2b was approved by FDA for T2DM in 1997, but after 6 weeks of its launch by Glaxo Welcome was withdrawn due to hepatotoxicity, and finally retired in 2000 (Nanjan et al., 2018).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.
Protein tyrosine phosphatase 1B (PTP1B) inhibitors as potential anti-diabetes agents: patent review (2015-2018)
Published in Expert Opinion on Therapeutic Patents, 2019
Hidayat Hussain, Ivan R Green, Ghulam Abbas, Sergazy M Adekenov, Wahid Hussain, Iftikhar Ali
Tetrazole scaffold chemistry has a wide range of applications for medicinal chemistry and in the agriculture fields. These scaffolds have been widely used in pharmaceuticals in the form of carboxylic acid surrogates and lipophilic spacers. Literature surveys showed that tetrazole analogs often possess a wide range of biolgical properties viz., antidiabetic, antimicrobial, anticancer, anti-inflammatory, analgesic, antitubercular, and antihyperlipidimic effects [63]. Interestingly, there are a number of drugs having the tetrazole group that have been approved by the FDA for various diseases [63,64]. Moreover, 5-membered heterocycles have a long history in producing antidiabetic compounds viz, thiazolidinedione analogs such as ciglitazone, pioglitazone, AD-5061, and AD-5075 have demonstrated very potent in vitro and in vivo antidiabetic and related effects. Moreover Wy-49,322 was the first hypoglycemic agent which has the trazole ring [65].
Thiazolidinedione drugs in the treatment of type 2 diabetes mellitus: past, present and future
Published in Critical Reviews in Toxicology, 2018
Melissa A. Davidson, Donald R. Mattison, Laurent Azoulay, Daniel Krewski
A class of TZDs was first discovered in the 1970s but it was not until the mid-1990s, after the early development of the fibrate drugs (agonists of the α PPAR subtype) and after TZD drugs such as ciglitazone, pioglitazone, and troglitazone had begun clinical development, that it was discovered that TZDs exerted insulin-sensitizing effects through direct activation of PPARs, specifically the γ subtype (Colca et al. 2014b). Since that time, it has been discovered that dependent upon cell type or binding site, TZDs act as synthetic agonists or antagonists of PPARs, a subfamily of nuclear receptors comprised of α, β/δ, and γ isoforms (Lehmann et al. 1995; Nuclear Receptors Nomenclature Committee 1999). Like other nuclear receptors, PPARs are comprised of distinct functional domains which are potential targets for modulation of signaling cascades (Ahmadian et al. 2013), including a ligand-binding domain (Moras and Gronemeyer 1998), a highly conserved DNA-binding domain (Poulsen et al. 2012), and a transactivation domain that allows for ligand-independent activation (Werman et al. 1997). After ligand binding, PPARs undergo specific conformational changes that allow for the differential recruitment of protein coactivators (Willson et al. 2001). As ligands differ in their ability to interact with coactivators, they can induce a number of diverse biologic and metabolic responses (Poulsen et al. 2012; Ahmadian et al. 2013).
Pioglitazone improves skeletal muscle functions in reserpine-induced fibromyalgia rat model
Published in Annals of Medicine, 2021
Fatma E. Hassan, Hader I. Sakr, Passant M. Mohie, Howayda Saeed Suliman, Ayman Saber Mohamed, Mohamed H. Attia, Dalia M. Eid
TZD’s have been tested for their anti-inflammatory effects on different mice and rat models. In one study, ciglitazone showed improvement of inflammatory process with peritonitis experimental sepsis rat model [42]. While pioglitazone improved adjuvant-induced arthritis (AIA) in rat models [43]. Also, pioglitazone protects against diabetic vascular complications independent from the decrease in blood sugar by decreasing atherosclerosis via different mechanisms [44]. Pioglitazone improved retinopathy in mice models through decreasing inflammation and neovascularisation in the retina in diabetic mice by decreasing TNF-alpha through stimulation of adiponectin, a known natural anti-inflammatory mediator [45].