The novel scaffold 1,2,4-benzothiadiazine-1,1-dioxide: a review

Synthesis and molecular docking studies of novel tricyclic and angular tetracyclic benzothiadiazines via sp3‐C‐Hactivation as potential colon cancer inhibitors

“…Benzothiadiazines and their derivatives have been established as versatile pharmacological agents [1] and are prevalent in natural products, pharmaceuticals [2], materials [3], and agricultural chemicals [4]. Many of them are in clinical use and trials.…”

“…Many of them are in clinical use and trials. Figure 1 shows some examples of the biological activities of 1,2,4‐benzothiadiazine‐1,1‐dioxide as antimicrobial [5], antiviral [6], antihypertensive [7], antidiabetic [8], anticancer [9], and KATP channel activators [10]. Many benzothiadiazines are currently in clinical use, they include rutaecarpine, bendroflumethazine, and triazolobenzothiadiazine ‐benzothiazole as shown in Figure 2.…”

Efficient Synthesis of Fused Heterocycles Incorporating Pyrazole/Thiadiazine or Pyrazole/Thiadiazepine Fragments Using N‐Chlorosulfonyltrihaloacetimidoyl Chlorides

“…The sulfonamide pharmacophore group is widely used to modify biological activity and is present in a number of drugs. Recent reviews have summarized the advances in the biological applications of heterocyclic compounds containing 1,2,4‐thiadiazine dioxides [1,2] . Pyrazole derivatives have demonstrated remarkable biological activities, including anti‐inflammatory, analgesic, antimicrobial, and anticancer properties [3,4] .…”

“…Recent reviews have summarized the advances in the biological applications of heterocyclic compounds containing 1,2,4-thiadiazine dioxides. [1,2] Pyrazole derivatives have demonstrated remarkable biological activities, including anti-inflammatory, analgesic, antimicrobial, and anticancer properties. [3,4] Similarly, thiadiazines have exhibited diverse pharmacological profiles, such as antimicrobial, antitumor, antiviral, and anticonvulsant activities.…”

Ir(III)-Catalyzed Dual C–H Activation of 2-Aryl Phthalazinediones and 3-Aryl-2H-benzo[e][1,2,4]thiadiazine-1,1-dioxides for the Construction of Spiro-Fused Cyclic Frameworks

“…On the other hand, benzothiadiazine-1,1-dioxides have been identified as remarkably important heterocyclic systems that are found in many drugs and pharmaceuticals . They are found to exhibit potent antimicrobial, antiviral, antihypertensive, antidiabetic, and anticancer properties and adenosine triphosphate (ATP)-sensitive potassium channel openers . Indeed, some of them are useful for the treatment of early stages of Alzheimer’s disease (Figure ).…”