Volume 3 of Advances in Medicinal Chemistry is comprised of four chapters on diverse aspects of medicinal chemistry. Chapter 1 presents an account of a research program which was started to discover a novel antipsychotic agent with minimal side effects for the treatment, principally, of schizophrenia. Chapter 2 relates an account on the discovery of novel antithrombotic drugs based on the RGD motif through a rational design approach. Chapter 3 presents the medicinal chemistry and preclinical development surrounding sertraline, a very important serotonin reuptake drug for the treatment of endogenous depression. Finally, Chapter 4 gives a summary of a series of boronic acid-based immunosuppressants that operate via inhibition of dipeptidypeptidase IV.