Hypertension is one of the most serious health problems of the modern world with a continuous rise in the number of patients. Selective alpha(1)-adrenoreceptor antagonists though have many advantages and uses in the management of arterial hypertension, their lack of specificity at the level of alpha(1)-adr subtypes leads to multiple side effects. Existence of multiple alpha(1)-adr subtypes holds great promise for the discovery and development of more specific and selective drug molecules, targeting only one alpha(1)-adr subtype at a time and thus relative freedom from side effects. Herein, the research done on the discovery and evaluation of a variety of chemically diverse structures as selective antagonists of alpha(1)-adr and alpha(1)-adr subtypes in recent years has been reviewed.