Currently, a handful of FDA approved drugs are commercially available to treat Alzheimers disease (AD). Among these, Tacrine (Cognex), Donepezil (Aricept), Rivastigmine (Exelon), Galantamine (Reminyl) and Memantine (Nemenda; Forest) are either acetylcholinesterase or N-methyl-D-aspartate antagonists. These are only palliative solutions, however, and side effects remain an important concern. Clearly, the search for more potent and effacious drugs for the treatment of AD is one of the most pressing pharmacological goals, and many more drugs are either in clinical trials or are being tested in laboratories around the world, both in academia and industry. In this review, we will compare the aforementioned five drugs with several other molecules that are currently in clinical trials or are ready to go into clinical trials. These will include antioxidants, metal chelators, monoamine oxidase inhibitors, anti-inflammatory drugs, as well as other AChE and NMDA inhibitors. In addition, medicinal chemistry approaches toward designing better pharmaceuticals will be discussed.