Synthesis and bioassay of azolyl benzothiazine carboxamides

Recent Advances in Synthesis and Medicinal Evaluation of 1,2‐Benzothiazine Analogues

“…Inspired by this work, Sankar group have prepared new derivatives by making use of compound 88 and appropriate derivative of azolyl amines 89 – 91 a – c to produce the compounds 84 a – c , 85 a – c and 86 a – c (Figure 21 and Scheme 15). [65—66] The compounds 84 a – c were found to possess higher antioxidant properties than 85 a – c which is in turn more active than the compounds 86 a – c . The compounds 84 b and 85 b were found to have greater activity than ascorbic acid (IC 50 (Mean±SD)=33.38±0.84 μg/ml) (reference).…”

“…Chen group have designed new derivatives of benzothiazines [70] to explore their inhibiting capacities against ALR2. On treating compound 9 [66] with HCl under reflux conditions to obtain 2 H ‐1,2‐benzothiazin‐4(3 H )‐one 1,1‐dioxide ( 110 ), which is further transformed into N ‐substituted ketone compounds 111 . The compounds 111 on reacting with methyl 2‐(triphenylphosphoranylidene) to give 2‐[2‐benzyl 1,1‐dioxido‐2 H ‐1,2‐benzothiazine‐4(3 H )‐ylidene]carboxylic acid methyl esters 113 and subsequent reaction of 113 with aqueous sodium hydroxide engendering 116 a – f and subjecting 113 to saturated acids followed by hydrogenation with Pd/C to delivered 115 a – d (Scheme 17).…”

“…The remarkable features of these heterocycles can be witnessed by their large number of publications (1782) and citations (11592) in recent times. Here in this review, therapeutic applications of 1,2‐benzothiazines in the arena of anti‐inflammatory, [23–37] anticancer, [38–56] antimicrobial, [57–62] antioxidant, [56,58,63–66] antidiabetic, [67–74] nor‐A efflux pump inhibitor, [75] antiepileptic, [76] anti‐arthritis, [77] anti‐HIV‐1, [78–81] alkaline phosphate inhibitors, [82] anti‐monoamine oxidase, [83] anti‐11β‐hydroxysteroid dehydrogenase, [84–85] calpain‐1 inhibitors, [86–87] and hepatitis virus‐C [88–89] along with their corresponding synthesis have been visualized. The prominence attained by derivatives of thiazole [90–91] and thiazine [15,92] lead researchers to construct medications like alpelisib and prochlorperazine maleate and a lot more (Figure 1).…”

“…During our contemplation on this paper, we get to know that combination of two structurally different but biologically and medicinally active scaffolds can lead to revolutionary hike in their potency when compare to their individual influence. For instance, combination of 1,2‐benzothiazine with pharmaceutically active derivatives of quinolones, [64] piprazine, [36–37,54,56,62] azoyls, [65–66] and pyrazoles [58,72,75,78–81,83,88–89] lead to even more active compounds which makes the researchers job easier to invent superior drug candidate. Also, performance of 1,2‐benzothiazines increases when they exist in complex forms with metals like Copper (II), Zinc (II), Nickel (II), Cobalt (II) and Ruthenium (III), [50–53] with enhanced pharmacokinetics and reduces side effects.…”