No abstract

It is to demonstrate that a heterocyclic derivatives acts as magic moiety in antagonizing numerous undesirable diseases. Intact the 1,5-Benzothiazepine is a six member benzene ring condensed to a hetero seven member ring shows a various pharmacological properties in the field of medicine. The Material and methods: molecular design for the depicted compounds is identified for its ADME properties and drug likeliness is studied using "Mcule" a software tool available online. Further the selected compounds are prepared in wet lab, a series of substituted Benzothiazepine are prepared by cyclo condensation of α-unsaturated ketones (chalcones) with O-amino thiophenol , β under the influence of glacial acetic acid. Structural characterization and anti-inflammatory (by Protein in-vitro denaturation inhibition) and anti-oxidant (by H O scavenging activity) activity are performed with slight revising the 2 2 procedure. From the obtain result the docking process made on target Leukotriene-C4 synthase (LTC4S) enzyme need for synthesis of leukotriene C4 from arachidonic acid to produce inflammatory response on bronchial asthma and another target Peroxisome proliferator-activated receptor alpha (PPARA) need for metabolism of TG and fatty acid to generate energy, cholesterol and LDL synthesis. Some of the compound code BTP-3 and BTP-5 shows Results: appreciable ligand-target interaction with glide score of-11.2 and-10.8 G, kcal/mol on PDB-2uuh (LTC4S) Δ compound BTP-5 and BTP-2 shows glide score of-11.8 &-10.8 G, kcal/mol on PDB-1kkq (PPARA) target. All Δ compounds shows good probability of physico-chemical property as per "Lipinski rule of five Compound BTP-5, 6 ". and 7 shows significant activity studies on anti-inflammatory and anti-oxidant activity as compared with in-vitro standard drug as show in respective histogram. 1, 5-Benzothiazepine derivatives shows a prominent Conclusion: activity by and model, from this it is considered as potent pharmacophore moiety for drug in-silico in-vitro development studies and used for evaluation studies by standard methods.