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Int. J. Mol. Sci. 2014, 15(9), 16500-16510; doi:10.3390/ijms150916500

Synthesis, Anticonvulsant, Sedative and Anxiolytic Activities of Novel Annulated Pyrrolo[1,4]benzodiazepines

1
Medicinal Chemistry Laboratory, Gunapati Venkata Krishnareddy Biosciences Private Limited, Plot No. 28A, Industrial Development Area Nacharam, Hyderabad 500076, India
2
Chemistry Division, Institute of Science and Technology, Jawaharlal Nehru Technological University, Kukatpally, Hyderabad 500085, India
3
School of Pharmacy, China Medical University, Taichung 40402, Taiwan
4
Department of Anatomy, School of Medicine, China Medical University, Taichung 40402, Taiwan
5
Department of Chinese Pharmaceutical Sciences and Chinese Medicine Resources, China Medical University, Taichung 40402, Taiwan
6
Research Center for Chinese Herbal Medicine, China Medical University, Taichung 40402, Taiwan
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Received: 14 August 2014 / Revised: 5 September 2014 / Accepted: 9 September 2014 / Published: 18 September 2014
(This article belongs to the Section Biochemistry, Molecular and Cellular Biology)
View Full-Text   |   Download PDF [707 KB, uploaded 18 September 2014]   |  

Abstract

Four new pentacyclic benzodiazepine derivatives (PBDTs 1316) were synthesized by conventional thermal heating and microwave-assisted intramolecular cyclocondensation. Their anticonvulsant, sedative and anxiolytic activities were evaluated by drug-induced convulsion models, a pentobarbital-induced hypnotic model and an elevated plus maze in mice. PBDT 13, a triazolopyrrolo[2,1-c][1,4]benzodiazepin-8-one fused with a thiadiazolone ring, exhibited the best anticonvulsant, sedative and anxiolytic effects in our tests. There was no significant difference in potency between PBDT 13 and diazepam, and we proposed that the action mechanism of PBDT 13 could be similar to that of diazepam via benzodiazepine receptors. View Full-Text
Keywords: benzodiazepine; thiadiazolone; pyrimidinone; cyclocondensation; anticonvulsant; sedative; anxiolytic benzodiazepine; thiadiazolone; pyrimidinone; cyclocondensation; anticonvulsant; sedative; anxiolytic
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Sorra, K.; Chen, C.-S.; Chang, C.-F.; Pusuluri, S.; Mukkanti, K.; Wu, C.-R.; Chuang, T.-H. Synthesis, Anticonvulsant, Sedative and Anxiolytic Activities of Novel Annulated Pyrrolo[1,4]benzodiazepines. Int. J. Mol. Sci. 2014, 15, 16500-16510.

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