The process of rational drug designing together with serendipity has played
an important role in the search for new drugs, for example, in neurotherapeutics the
dopaminergic dysfunction of Parkinson’s disease, the dopaminergic hyperfunction of
schizophrenia and the acetylcholine deficit in patients suffering from Alzheimer’s
disease (AD). AD is the most common form of dementia which is a group of disorders
that impairs mental functioning. The aim of this chapter is 1) to analyze some examples
of discoveries in AD related disorders based on some serendipitous hypotheses and
rational drug design approach such as structure based drug designing, ligand based drug
designing and multi-target-directed ligand approach ii) to study the drug targets such as
AChE, BACE-1, Tau protein for treating AD iii) to design second-generation agents
with improved efficacy and safety iv) to illustrate the complexity of problems that have
to be overcome for successful targeting and v) to study drug delivery and intercellular
characterization of the blood brain barrier.
Keywords: Alzheimer’s disease, blood brain barrier, disease modifying drugs,
multi-target-directed ligand, rational drug design, serendipity, symptomatic drugs.
