Journal article Open Access

EFFECT OF CATALYST ON SYNTHESIS OF 1, 5- BENZODIAZEPINE DERIVATIVES AND EVALUATION OF THEIR PHARMACOLOGICAL ACTIVITY

N. Siva Subramanian*, Ch. Malathi Suvarna, Pavan Kumar. Sara, Elender. G

1,5-Benzodiazepines are psychoactive drugs Benzene ring and Diazepine ring fusion, widely used as hypnotics, sedatives and in several Central Nervous System disorders. 1,5-Benzodiazepines are regularly used because of their nature of exhibiting pharmacological effects with minimal effect on patient performance. Derivatives of 1, 5- benzodiazepines were synthesized using the catalysts like Formic Acid and Glacial Acetic Acid, characterized by spectral studies using 1H-NMR Spectroscopy, Mass Spectroscopy, and FT-IR Spectroscopy. The results showed that the percentage yield of the reaction involving Formic acid as a catalyst is higher when compared to that of the Glacial Acetic Acid as catalyst. This indicates that the acidic nature of formic acid is enhancing the cyclization process thus producing higher percentage yield. Hence the use of stronger acid as a catalyst is enhancing the cyclization. The pharmacological activity of synthesized compounds are screened using animal models for muscle relaxant property and catatonic activity and are showing significant effect when compared with the standard drug diazepam. When compared the compound- A which is a derivative of acetone and 1, 2- diaminobenzene is showing more activity than the rest of synthesized compounds. Thus the study shows that the use of strong acid as a catalyst is increasing the yield of the 1,5-Benzodiazepines in synthesis of pharmacologically active derivatives.

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