Design and Microwave Assisted Synthesis of Coumarin Derivatives as PDE Inhibitors.
نویسندگان
چکیده
Coumarins appended to benzimidazole through pyrazole are designed and synthesized using microwave irradiation. These compounds were analyzed for phosphodiesterase (PDE) inhibition indirectly by motility pattern in human spermatozoa. Some of the synthesized compounds, namely, 5d, 5e, 5f, 5g, 5h, and 5k, have exhibited potent inhibitory activity on PDE.
منابع مشابه
Synthesis novel bis-Coumarin derivatives as potential acetylcholinestrase inhibitors: An in vitro, molecular docking, and molecular dynamics simulations study
Alzheimer's disease is an irreversible and progressive brain disorder that slowly destroys memory and thinking skills and ultimately the ability to do the simplest things and can lead to death. Cholinesterases (ChEs) play an important role in controlling cholinergic transmission, and subsequently, by inhibiting CHEs, acetylcholine levels in the brain are elevated. Coumarins have been shown to e...
متن کاملMicrowave-Assisted Three Component Cyclocondensation Reaction: A Facile Synthesis of Highly Functionalized Cyclohexene Derivatives
Microwave-assisted three component cyclocondensation reactions of aldehydes, amides and dienophiles in the presence of acetic anhydride and para-toluenesulfonic acid as a catalyst to afford the highly substituted cyclohexene derivatives, in relatively good yields after several minutes are reported.
متن کاملMicrowave-assisted synthesis and antioxidant properties of hydrazinyl thiazolyl coumarin derivatives
UNLABELLED BACKGROUND Coumarin derivatives exhibit a wide range of biological properties including promising antioxidant activity. Furthermore, microwave-assisted organic synthesis has delivered rapid routes to N- and O-containing heterocycles, including coumarins and thiazoles. Combining these features, the use of microwave-assisted processes will provide rapid access to a targeted coumarin...
متن کاملMicrowave Assisted Multi-component Synthesis of 4Hchromene Derivatives by Nano-coconut Shell-BF3 as a New Heterogeneous Catalyst
Microwave assisted reactions have gained considerable attention, due to versatility and reduction ofsolvent and reaction time. The reaction of a nano-coconut shell and boron tri-fluoride in diethylether solvent resulted in preparation of nano-coconut shell-BF3 as a catalyst. The nano-coconutshell-BF3 catalyst has been characterized by fourier transform infrared spectroscopy (F...
متن کاملMicrowave assisted synthesis of [4, 5-e] [1, 3, 4]thia- diazin-7-yl] hydrazine Derivatives
New pyrimido [4, 5-e] [1, 3, 4]thia- diazin-7-yl] hydrazines were synthesized via the cyclocondensation of alkyl-2-phenylhydrazinecarbodithioates as a binucleophile with 5-bromo-2,4-dichloro-6-methylpyrimidine as a bielectrophile , and replacement of C-7 chloro atom by hydrazine in ethanol as the solvent . This method has advantages over methods currently described in the literature for the con...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
- International journal of medicinal chemistry
دوره 2016 شماره
صفحات -
تاریخ انتشار 2016