Summary of structure-activity relationships (SARs)课件.pptVIP

What structural elements are necessary for activity? Removing the oxide bridge (and hydrogenating double bond, removing one alcohol) produces levorphanol, which has enhanced analgesic properties over morphine. Surprisingly, its mirror image still has antitussive properties, but no analgesic properties Methylating the phenolic hydroxyl group improves this antitussive activity Dextromethorphan (DM or DXM) is an antitussive drug that is found in many over-the-counter cold and cough preparations, usually in the form of dextromethorphan hydrobromide. It is also commonly taken above the recommended dosage by users seeking its dissociative effect. The FDA has approved dextromethorphan for over-the-counter sale as a cough suppressant. A combination of dextromethorphan and quinidine has been shown to alleviate symptoms of easy laughing and crying (pseudobulbar affect) in patients with amyotrophic lateral sclerosis and multiple sclerosis.[3] Dextromethorphan is being investigated as a possible treatment for pain associated with fibromyalgia, a chronic rheumatological organic fatigue disorder.[4] Dextromethorphan is also useful in breaking addictions to narcotics and other habit-forming drugs (including nicotine), since it is an inhibitor of many of the brain receptors involved in narcotic action on the brain. For this purpose, DXM is more effective when combined with an oxidase inhibitor, which suppresses its inactivation and increases its half-life; thus it increases the concentration of DXM in the circulating blood and extends its effective duration.[5] Meperidine Pethidine (INN) or meperidine (USAN) (also referred to as: isonipecaine; lidol; pethanol; piridosal; Algil?; Alodan?; Centralgin?; Demerol?; Dispadol?; Dolantin?; Dolargan? (in Poland);[1] Dolestine?; Dolosal?; Dolsin?; Mefedina?) is a fast-acting opioid analgesic drug. In the United States, it is more commonly known as meperidine or by its brand name Demerol.[2]Pethidine is indicated for the treatment of moderate