In this era of sporadic advancement in science and technology, a substantial amount of intervention is being set in motion to reduce health-related diseases. Discoveries from researchers have pinpointed the usefulness of heterocyclic compounds, amongst which benzothiazepine (BTZ) derivatives have been synthesized for their various pharmacological activities. This also contributes to their undeniable application in therapeutic medicine for the development of efficacious drugs. BTZs are compounds with a benzene ring fused with a thiazepine ring. This work contains several methods that have been used to synthesize 1,3-, 1,4-, 1,5-, and 4-1-benzothiazepine derivatives. In addition, up-to-date information about the crucial pharmacological activities of BTZ derivatives has been reviewed in this present study to appreciate their druggable potential in therapeutic medicine for drug development. Drug design and development have further been simplified with the implementation of computer aided approaches to predict biological interactions which can help in the design of several derivatives. Hence, the structural activity relationship (SAR), ADMET and the molecular docking studies of BTZ derivatives were discussed to further establish their interactions and safety in biological systems. This present work aims to expound on the reported chemistry and pharmacological propensity of BTZ moiety in relation to other relevant moieties to validate their potential as excellent pharmacophores in drug design and development.

在这个科学技术零星进步的时代，正在启动大量干预措施以减少与健康相关的疾病。研究人员的发现明确了杂环化合物的用途，其中合成的苯并噻氮 (BTZ) 衍生物具有多种药理活性。这也有助于它们在治疗医学中用于开发有效药物的不可否认的应用。BTZ 是苯环与硫氮杂环稠合的化合物。这项工作包含多种用于合成 1,3-、1,4-、1,5- 和 4-1-苯并硫氮杂衍生物的方法。此外，本研究回顾了有关 BTZ 衍生物关键药理活性的最新信息，以了解它们在药物开发治疗药物中的成药潜力。通过实施计算机辅助方法来预测有助于设计多种衍生物的生物相互作用，药物设计和开发得到了进一步简化。因此，讨论了 BTZ 衍生物的结构活性关系 (SAR)、ADMET 和分子对接研究，以进一步确定它们在生物系统中的相互作用和安全性。目前的工作旨在阐述 BTZ 部分与其他相关部分相关的化学和药理学倾向，以验证它们在药物设计和开发中作为优秀药效团的潜力。