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Therapeutic Use of Carbonic Anhydrase Inhibitors and Their Multiple Drug Interactions
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Andrea Angeli, Claudiu T. Supuran
The systemic carbonic anhydrase inhibitor, acetazolamide (1), was initially discovered as a diuretic agent (Supuran, 2008; Neri and Supuran, 2011) and introduced in 1954 into ophthalmology as a treatment for glaucoma and, since then, has been widely used for this purpose. At first, its clinical use as diuretic drug is limited to development of metabolic acidosis (Kassamali and Sica, 2011). However, this feature can afford some potential clinical benefit for disease states such as metabolic alkalosis (Faisy et al., 2010; Mazur et al., 1999) nephrolithiasis (Sterrett et al., 2008), rhabdomyolysis (Subbaramaiah et al., 2010; Davidov et al., 2006), contrast-induced nephropathy (CIN) (Pakfetrat et al., 2009), sleep apnea (Nakayama et al., 2002; Angeli and Supuran, 2018), and high-altitude erythropoiesis (Leaf and Goldfarb, 2007; Richalet et al., 2008). In subsequent years the systemic side effects of acetazolamide led to the development of new CAIs such as brinzolamide 3 and dorzolamide 4 (Fig. 3.2) with their high water solubility are administered via the topical route directly into the eye, making them less prone to drug-drug interactions and systemic side effects (Carta et al., 2012; Masini et al., 2013).
Synthetic and anti-cancer activity aspects of 1, 3, 4-thiadiazole containing bioactive molecules: A concise review
Published in Journal of Sulfur Chemistry, 2021
Vincent A. Obakachi, Babita Kushwaha, Narva Deshwar Kushwaha, Sithabile Mokoena, Ab Majeed Ganai, Tabasum Khan Pathan, Werner E. van Zyl, Rajshekhar Karpoormath
The display of interesting pharmacological properties of 1,3,4-thiadiazole heterocyclic compounds is considered to be due to N2C2S moiety, its lack of toxicity, in vivo stability, and high aromaticity [19]. Furthermore, the ability of the ‘hydrogen binding domain’ and the ‘two-electron donor mechanism’ allows the use of 1,3,4-thiadiazole as one of the latent molecules in a variety of marketed products, such as Methazolamide (Carbonic anhydrase inhibitor), Acetazolamide (for glaucoma), Desaglybuzole (anti-diabetic) [20], Cephazolin, Filanesib, Litronesib etc. as presented in (Figure 2) with their respective frameworks and activities that have been approved. The synthesis and evaluation of the chemical properties and biological activities of the novel 1,3,4-thiadiazole embedded analogues have accelerated over the years. In addition, the number of research studies on this moiety has also increased significantly in recent years. This review aims to capture a recent synthetic approaches and anticancer activities published in the literature, based on the compound's value in medicinal chemistry.
Synthesis, characterization, and pharmacological evaluation of the proton transfer salts of 2-aminobenzothiazole derivatives with 5-sulfosalicylic acid and their Cu(II) complexes
Published in Journal of Coordination Chemistry, 2018
Halil Ilkimen, Yasemin Tekşen, Cengiz Yenikaya, Irem Turhan, Tuncay Tunç, Musa Sari
2-Aminobenzothiazole (abt), 2-amino-6-ethoxybenzothiazole (EtOabt), and 5-sulfosalicylic acid dihydrate (H3ssa) and their simple metal complexes are well known for their biological activities, such as anti-microbial, anti-fungal, anti-inflammatory, analgesic, anthelmintic, anti-ulcer, anti-tumor, and carbonic anhydrase inhibitor properties [1–8]. 2-Aminobenzothiazole and its derivatives in most cases act as monodentate ligands which coordinate to metal ions through the nitrogen [4,9] or sulfur [10,11] of the ring or amino group [12,13]; on the other hand, there are several works on 2-aminobenzothiazole complexes in which the nitrogen [14,15] or sulfur [16] with the amino group participate in coordination. The H3ssa ligand involves three functional groups, –SO3H, –COOH, and –OH, which can be partly or fully deprotonated in five forms, fabricating many novel architectures [17].