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Asian Journal of Research in Pharmaceutical Science
Year : 2018, Volume : 8, Issue : 1
First page : ( 25) Last page : ( 29)
Print ISSN : 2231-5640. Online ISSN : 2231-5659.
Article DOI : 10.5958/2231-5659.2018.00006.1

Anxiolytic activity of some 2, 3-dihydrobenzo[b] [1, 4] oxazepine derivatives synthesized from Murrayanine-Chalcone

Mahapatra Debarshi Kar1,*, Shivhare Ruchi S.2, Gupta Sayan Dutta3

1Department of Pharmaceutical Chemistry, Dadasaheb Balpande College of Pharmacy, Nagpur, 440037, Maharashtra, India

2Department of Pharmaceutical Chemistry, Kamla Nehru College of Pharmacy, Nagpur, 441108, Maharashtra, India

3Department of Pharmaceutical Chemistry, Gokaraju Rangaraju College of Pharmacy, Hyderabad, 500090, Telangana, India

*Corresponding Author E-mail: dkmbsp@gmail.com

Online published on 2 June, 2018.

Abstract

Due to the fact that, Murrayanine is one of the most active compounds of the present carbazole series with a simple chemistry which facilitate multiple sites for substituting varied active groups, and their pharmacological expression thereof. Several heterocycle based hybrids of the Murrayanine were fabricated rationally by our research group. Benzoxazepine is an exhaustively applied scaffold which finds application in diverse areas of pharmacotherapeutics. Hybridizing benzoxazepine with any components has often resulted in the discovery of prospective compounds. In the present research, we designed and synthesized certain seven-membered benzoxazepine molecules by cyclizing Murrayanine-Chalcone, the starting material previously reported by our research group and explored their anti-anxiety or hypnotic effects by evaluating locomotor inhibitory potentials in Swiss albino rat. The highest locomotor inhibition was exhibited by the compound 3d containing 4-iodo substituent which may be translated therapeutically as the anti-anxiety effect. However, none of the fabricated molecules presented higher pharmacological activity than the benzodiazepine (diazepam), the standard drug. A very clear SAR could not be established from this study. The murrayanine based benzoxazepine analogs (3a-h) produced hypnosis and anxiolysis by enhancing the effect of GABA neurotransmitter at GABAA receptor, a mechanism similar to that of the benzodiazepine (diazepam). The research will further explore more potential of the hybrid seven-member candidates and will motivate researchers in developing therapeutically active as well as safe analogs in upcoming time.

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Keywords

Murraya koenigii, Murrayanine, Benzoxazepine, Chalcone, Locomotor, Heterocycle.

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