Synthesis, antimalarial activity, structure–activity relationship analysis of thieno-[3,2-b]benzothiazine S,S-dioxide analogs

Synthesis and Characterization of Immobilized Lipase on Fe3O4 Nanoparticles as Nano biocatalyst for the Synthesis of Benzothiazepine and Spirobenzothiazine Chroman Derivatives

“…To investigate the efficacy and the generality of the catalyst, a variety of benzothiazepine and spirobenzothiazine chroman derivatives were synthesized by threecomponent reaction between coumarin-3-carboxylic acid derivatives (1), amino benzothiol (2) and alkyl isocyanide derivatives (3) in the presence of (0.025 g) NBC at room temperature in ethanol and dioxane, according to Schemes 2 and 3. The products were obtained in excellent yields with high purity and in short reaction times, in comparison with previous reports (Table 2) [44].…”

“…In continuation of our general interest in the synthesis of heterocyclic compounds through MCRs in the presence of nanocatalysts [35][36][37], a new approach for the synthesis of 1,4-benzo-thiazepine, spirobenzothiazine chroman derivatives and some novel derivatives of these compounds was investigated, utilizing three-component reaction of coumarin-3-carboxylic acids (1), 2-aminobenzothiol (2) and isocyanides (3) in the presence of immobilized lipase (from ANL as a new source) on Fe 3 O 4 nanoparticles (Fe 3 O 4 NPs@lipase) as an active nano biocatalyst (NBC) at ambient temperature (Schemes 2 and 3). Based on this, first magnetic nanoparticles Fe 3 O 4 were prepared by the method which has been reported in literature [38].…”

“…Benzothiazepine structure is so multifunctional that a great number of known drugs such as dithiazem, clentiazem, and thiazesim possess such structure [1]. Benzothiazines also demonstrate widespread medicinal properties such as antimicrobial [2], antimalarial [3], and anti-inflammatory medications [4].…”

Synthesis and antimicrobial activity of structurally flexible heterocycles with the 1,4-thiazine heterosystem

“…In addition, 4H-1,4-benzothiazine derivatives have been shown to exhibit wide-ranging biological activities, such as anticancer, antifungal, antagonistic, antioxidant, antihypertensive, analgesic, cardiovascular, antibacterial, antimalarial, and antimicrobial, etc. [8][9][10][11][12][13][14][15][16][17][18][19][20][21]. 1,4-Benzothiazines have also been reported as new antiallergic and antirheumatic agents.…”

Anti-HIV activity of new pyrazolobenzothiazine 5,5-dioxide-based acetohydrazides

“…The oxicam family of nonsteroidal anti-inflammatory drugs (NSAIDs) is in use for the treatment of various kinds of inflammatory disorders (Olkkola et al, 1994;Katzmann, 1990;Hadadzadeh et al, 2012;Balfour et al, 1996). Various other derivatives of benzothiazine family have been reported as antimicrobial (Abbas and Farghaly, 2010), antimalarial (Barazarte et al, 2008), antiinflammatory (Gannarapu et al, 2014), anti-tumor/anticancer agents (Coughlin et al, 1995;Abbas and Farghaly, 2010;Zięba et al, 2013;Peng et al, 2011;Kamel et al, 2010;Coughlin et al, 1995), antiviral (Aslam et al, 2014a, b) and acetylcholinesterase inhibitors (Aslam et al, 2014c).…”