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

International Journal of Molecular Sciences

Kumaraswamy Sorra²  Chien-Shu Chen¹  Chi-Fen Chang⁵  Srinivas Pusuluri²  Khagga Mukkanti³  Chi-Rei Wu⁴ 

[1] School of Pharmacy, China Medical University, Taichung 40402, Taiwan; E-Mail:;Medicinal Chemistry Laboratory, Gunapati Venkata Krishnareddy Biosciences Private Limited, Plot No. 28A, Industrial Development Area Nacharam, Hyderabad 500076, India; E-Mails:;Chemistry Division, Institute of Science and Technology, Jawaharlal Nehru Technological University, Kukatpally, Hyderabad 500085, India; E-Mail:;Department of Chinese Pharmaceutical Sciences and Chinese Medicine Resources, China Medical University, Taichung 40402, Taiwan;Department of Anatomy, School of Medicine, China Medical University, Taichung 40402, Taiwan; E-Mail:

关键词: benzodiazepine;    thiadiazolone;    pyrimidinone;    cyclocondensation;    anticonvulsant;    sedative;    anxiolytic;   

DOI  :  10.3390/ijms150916500

来源: mdpi

【 摘 要 】

Four new pentacyclic benzodiazepine derivatives (PBDTs 13–16) 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.

【 授权许可】

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© 2014 by the authors; licensee MDPI, Basel, Switzerland.