Abstract
The objective of our work is to make a pharmacological study of molecules derived from 4-phenyl-1,5-benzodiazepin-2-one carrying long chains so that they have a structure similar to surfactants, with the benzodiazepine as a hydrophilic head and a carbon chain as a hydrophobic tail. First, we studied the acute toxicity of the above mentioned 4-phenyl-1,5-benzodiazepin-2-one derivatives. This study was conducted according to OECD 423 guidelines in female mice and revealed that these compounds are nontoxic. We then assessed the psychotropic effects of our products on the central nervous system (CNS). The results obtained show that 4-phenyl-1,5-benzodiazepin-2-one has no sedative effect at therapeutic doses of 100 and 200 mg/kg. On the other hand, its long-chain derivatives possess them. Moreover, all these products have no cataleptic and hypnotic effects at the doses studied. But at 100 mg/kg, these compounds all have the ability to significantly prolong the hypnotic effect of thiopental sodium.
Highlights
Terence Nguema Ongone,1,2 Redouane Achour,1 Mostafa El Ghoul,1 Latifa El Ouasif,1 Khalid Taghzouti,3 Meryem El Jemli,2 Yahia Cherrah,2 Katim Alaoui,2 and Amina Zellou2
Kanyonga et al [3] conducted a study of the acute toxicity of 4-phenyl-1,5-benzodiazepin-2-one. ey showed that the lethal dose 50% (LD50) is 1617.08 mg/kg
We have shown that 4-phenyl-1,5benzodiazepin-2-one does not have catatonigenic and hypnotic effects on the central nervous system (CNS) at therapeutic doses of 100 and 200 mg/kg
Summary
Terence Nguema Ongone ,1,2 Redouane Achour, Mostafa El Ghoul, Latifa El Ouasif, Khalid Taghzouti, Meryem El Jemli ,2 Yahia Cherrah, Katim Alaoui, and Amina Zellou. Academic Editor: Berend Olivier e objective of our work is to make a pharmacological study of molecules derived from 4-phenyl-1,5-benzodiazepin-2-one carrying long chains so that they have a structure similar to surfactants, with the benzodiazepine as a hydrophilic head and a carbon chain as a hydrophobic tail. All these products have no cataleptic and hypnotic effects at the doses studied. This part of the chemistry allows the synthesis of bioactive molecules used in the pharmaceutical industry for the preparation of drugs In this family, benzodiazepines have been shown to be pharmacologically important since they exert anxiolytic, analgesic, anticonvulsant, antidepressant, cataleptic, hypnotic, myorelaxant, and sedative [1,2,3] effects on the central nervous system (CNS). The literature reports a large number of works showing that, in the pharmaceutical field, the surfactants can carry hydrophilic and hydrophobic active ingredients of the drugs into the cells; they can protect them and significantly reduce their toxicity [7]
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