Conformationally restricted GABA analogs: from rigid carbocycles to cage hydrocarbons.

摘要: GABA was discovered to play an important role as the major inhibitory neurotransmitter in adult mammalian CNS 60 years ago. The conformational flexibility of is for its biological function, it has been found bind different receptors with conformations. In effort increase lipophilicity and reduce itself, a polycyclic or cage hydrocarbon framework can be introduced into 3D structure order better control binding. This article explores available synthetic methods, properties activity carbocyclic (cyclopropanes, cyclobutanes cyclohexanes) (adamantane others) hydrocarbons - analogs conformationally rigid carbon skeletons.