The aim of this review is an attempt to highlight the progress in the chemistry and to present an outline of various pharmacological activities of 1,2,4-benzothiadiazine-1,1-dioxide ring. The biological activities of 1,2,4-benzothiadiazine-1,1-dioxide, for example, antimicrobial, antiviral, antihypertensive, antidiabetic, anticancer, KATP channel activators, and AMPA receptor modulators etc., are reported. Many functional groups attached to the ring are responsible for the activity of 1,2,4-benzothiadiazine-1,1-dioxide like a halo, the group at 7 and 8 positions of the ring gave active compounds. Meanwhile, other functional groups like alkyl, aryl, alkylamino, benzyl, keto, etc. at different position of 1,2,4-benzothiadiazine-1,1-dioxide ring are responsible for the activity. The review aims are to collect literature work stated by scholars on 1,2,4-benzothiadiazine-1,1-dioxide for their different therapeutic activities and report the current efforts made on this ring.