On conformation analysis, molecular graphics, fentanyl and its derivatives.

Abstract

In 1680, Thomas Sydenham noted that ‘Among the remedies which it has pleased Almighty God to give man to relieve his sufferings, none is so universal and so efficacious as opium’. After Friedrich Serturner in the beginning of the 19th century isolated an opium alkaloid which he called morphine after the Greek god Morpheus, and following the invention of the syringe and the hollow needle in the fifties of the 19th century, the controlled administration of morphine became possible. Imagine the terror of a patient in the first half of the 19th century subjected conscious to the saw and the knife! In fact, during the Lister Lecture in memory of the first Baron Lister, pioneer of antiseptic surgery, Spinks [1] recalled the reputation for quick surgery of James Syme, who allegedly performed a mid-thigh amputation in nine sec-onds, including the patient’s left testicle and the forefinger of the chief assistant! Ever since the introduction of morphine in clinical practice it has been recognized that morphine has a number of side-effects such as addiction potential, tolerance and respiratory depression, which prompted the quest for new opiates lacking these side-effects. This quest went over heroine which was introduced in 1890 as a non-addictive morphine derivative, to meperidine and methadone, the latter two being purely synthetic compounds.