ABSTRACT

It is the promise of modern chemistry, biology, and biotechnology to the pharmaceutical industry that basic knowledge can be translated into novel and efcient drugs. However, such transfer of information is very complex and, hence, drug discovery is very expensive and time consuming, and no drugs are yet available for many disorders. Today, only several hundred distinct chemical entities exist as drug molecules (along with several thousand of their analogs) and are available on the market; most of them are low MW (typically of 300-400 Da) substances. Well-known examples from history are morphine (an ingredient of opium, known for 5000 years), aspirin (acetylsalicylic acid rst synthesized in 1853; an antianalgesic, which inhibits the enzyme cyclooxygenase), salvarsan (an antimicrobial agent that cures syphilis, introduced by Nobel Prize winner Paul Ehrlich in 1910), β-blockers (introduced in 1960s), HIV protease inhibitors (introduced in 1990s), and other well-known drugs.