Synthesis of novel heterocyclic compounds containing 1, 5-benzodiazepine (original) (raw)

Benzodiazepines, from the pharmacological standpoint, are very interesting molecules. Numerous studies have demonstrated anxiolytic effect on the human nervous system. They are used in the therapeutic field 1 and have important biological activities, particularly the 1,4-and 1,5-benzodiazepines 2. Benzodiazepines are also used as anticonvulsant agents 3 , anti-inflammatory and analgesic 4 , antidepressive of the central nervous system 5 and antibacterial 6. For instance, Valium (diazepam) is marketed as a sedative and noveril (dibenzepin) as an antidepressive. The strategy of using benzodiazepines essentially depends on the knowledge of their pharmacokinetics that can take advantage of their "qualities" but also to avoid some of their "side effects". In addition, benzodiazepines are the most powerful anticonvulsant substances known so far: they are able of antagonize, common amongst animal, convulsions induced by a wide variety of chemical substances e.g., isoniazid, picrotoxin, strychnine, pentetrazole. On the other hand, they are less effective in protecting seizures due to electric shock 7. Synthesis of 1,5-benzodiazepines structures were made from different lactones, such as tetronic acid, 4-hydroxy coumarin, demidone and dehydroacetic acid 8. It therefore seemed interesting to carry on further research by investigating the reactivity of the dehydroacetic acid and its derivatives which are susceptible to serve as starting material for the synthesis of other heterocyclic compounds such as benzodi