Medicinal chemistry is a very important and useful tool insuring effective development of new drugs. There are many synthetic and natural substances containing pyrrole moiety with significant activity, which have became a target molecule for new "drug-like" compounds. To better understand of rationalized drug design the importance of some terms and processes playing an essential role in modern pharmacy (e.g. pro-drugs, in silico prediction, molecular modelling, bioisosterism) were emphasized and the main classes of drugs in Poland and UE and alkaloids with pyrrole ring in its structure (neuroleptics, non-steroidal anti-iflammatory, nootropic, inhibitory-angiotensin converting enzyme and antiemetic drugs, adrenolytics, statins, drugs used in the treatment of insomnia, migraine, Parkinson disease and erection disorders) were reviewed as well.

Keywords: pro-drugs, in silico prediction, molecular modelling, bioisosterism, drugs containing pyrrole moiety.