Synthesis and psychobiological evaluation of modafinil analogs in mice
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- 作者：Arezou Lari (1)
Isaac Karimi (2)
Hadi Adibi (3)
Alireza Aliabadi (3)
Loghman Firoozpour (4)
Alireza Foroumadi (4) (5) - 关键词：Modafinil ; Wake ; promoting agent ; Narcolepsy
- 刊名：DARU Journal of Pharmaceutical Sciences
- 出版年：2013
- 出版时间：December 2013
- 年：2013
- 卷：21
- 期：1
- 全文大小：338 KB
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17. Miraghaee S, Karimi I, Becker LA: Psychobiological assessment of smoke of agarwood (Aquilaria spp.) in male rats. / J Appl Biol Sci 2011, 5:45鈥?3. - 作者单位：Arezou Lari (1)
Isaac Karimi (2)
Hadi Adibi (3)
Alireza Aliabadi (3)
Loghman Firoozpour (4)
Alireza Foroumadi (4) (5)
1. Students Research Committee, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran
2. Laboratory of Molecular and Cellular Biology, School of Veterinary Medicine, Razi University, Kermanshah, Iran
3. Novel Drug Delivery Research Center, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran
4. Drug Design and Development Research Center, Tehran University of Medical Sciences, Tehran, Iran
5. Neuroscience Research Center, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman, Iran - ISSN：2008-2231
文摘
Background and the purpose of the study Modafinil, a novel wake-promoting agent with low potential for abuse and dependence, has a reliable structure to find some novel derivatives with better activity and lower potential for abuse and risk of dependency. This study was designed to evaluate psychobiological activity of some novel N-aryl modafinil derivatives. Methods Seven novel N-aryl modafinil derivatives were synthesized through three reactions: a) preparation of benzhydrylsulfanyl acetic acid through reaction of benzhydrol with thioglycolic acid, b) formation of desired amide by adding the substituted aniline to activated acid with EDC (1-ethyl-3-(3-dimethyl amino propyl) carbodiimide). This reaction was catalyzed by HOBt (N- hydroxylbenzotriazole), and c) oxidation of sulfur to sulfoxide group with H2O2. Then, their psychobiological effect on the performance of male albino mice were compared to that of modafinil as following: wakefulness by determining the effects of derivatives on phenobarbital-induced loss of the righting reflex (LOPR); exploratory activity by measuring activity in the open field test (OFT); depression by measuring immobility time (IT) during forced swimming test (FST) and the anxiogenic and anxiolytic like effects by using elevated plus-maze test (EPM). All tests were videotaped and analyzed for the frequency and duration of the behaviors during the procedures. Conclusions 2-(Benzhydrylsulfonyl)-N-(4-chlorophenyl)acetamide (4c) showed comparable result in LOPR test. However, all analogs were found to be stimulant except 2-(benzhydrylsulfinyl)-N-phenylacetamide (4a). Also 4c led the most exploratory activity in mice among derivatives. FST results showed that 4a had the longest IT while modafinil, 2-(benzhydrylsulfinyl)-N-(3-chlorophenyl) acetamide (4b) and 2-(benzhydrylsulfinyl)-N-(4-ethylphenyl) acetamide (4d) had the shortest IT. In EPM, all derivatives showed anxiogenic-like behavior since they decreased open arms time and open arms entries and simultaneously increased close arms time.