Synthesis, Characterization, Lethal dose (LD50) and In vivo Acute Oral Toxicity Studies of a Novel 1,5-Benzothiazepine Derivatives

Abstract

Background: Since they've numerous bioactivities, the 1, 5-benzothiazepines are enormous seven-member heterocyclic nitrogen and sulphur compounds in healing improvement. The maximum famous sort of 1,4-thiazepines are 1,5-benzothiazepines. The 1,5-benzothiazepine derivatives are of specific relevance for lead discovery because it has been located that they may be lively towards numerous objectives from numerous families.A benzene ring and a diazepine ring integrate to shape benzodiazepines (BZD, BDZ, BZs), a own circle of relatives of depressive drugs now and again stated as "benzos" or "benzos". They are advertised as a remedy for seizures, sleeplessness, and tension problems. 1,5-Benzothiazepines have inspired the improvement of some of artificial strategies for his or her synthesis and chemical changes because of their usefulness in pharmacological research.

Aim of Study: With the use of different dosages (10, 100, 1000, 1600, 2900, and 5000 mg/kg p.o. route), an unique series of the chosen 1,5-benzothiazepine derivatives were produced and tested for in vivo safety pharmacological tests (acute toxicity LD50).

Materials and methods: Completion of chemical response become monitored with the aid of using skinny layer chromatography on silica gel G covered plates and very last compounds had been purified with the aid of using recrystallisation with methanol. The chemical shape of synthesized had been prominent with the aid of using FTIR, 1H-NMR, Mass and elemental analysis. The LD50 of novel 1,5-benzothiazepine derivatives decided with the aid of using acute poisonous magnificence approach as consistent with OECD 423 guidelines.

Results and discussion: In the results of the spectral study, all the compounds showed characteristic peak in FTIR and ¹H-NMR spectroscopy. Compounds containing chlorine moiety show [M+2]⁺ peak in mass spectrum. The result of in vivo acute oral toxicity studies showed that the compounds 6c1, 6e2 and 6e3 were toxic to mice and cause death at dose of 1600 and 2900 mg/kg body weight of live mice and LD50 of compounds 6c1: 4786 mg/Kg, 6e2: 2542 mg/kg and 6e3: 2039 mg/kg respectively.