Antiinflammatory agent

Aspinn possesses a number of properties that make it an often recommended drug It is an analgesic effective m relieving headache pain It is also an antiinflammatory agent providing some relief from the swelling associated with arthritis and minor injuries Aspinn IS an antipyretic compound that is it reduces fever How aspmn does all this was once a mystery but is now better understood and will be discussed m Section 26 6 Each year more than 40 million lb of aspirin is produced m the United States a rate equal to 300 tablets per year for every man woman and child... 

ANALGESICS,ANTIPYRETICS,AND ANTIINFLAMMATORY AGENTS] (Vol2) Buprenorphme [52485-79-7]... 

Progress in the field received further impetus with the development of synthetic steroids exhibiting activities far greater than that of the natural hormones. The synthesis of 9 a-fluorocortisol (3), described in 1953 by Fried and Sabo (3), opened the way for development of many more highly active antiinflammatory agents, and indeed some of today s most active antiinflammatory agents (ca 1997) bear some resemblance to this 9a-fluorinated steroid. 

Acylated Corticoids. The corticoid side-chain of (30) was converted iato the cycHc ortho ester (96) by reaction with a lower alkyl ortho ester RC(OR )2 iu benzene solution ia the presence of i ra-toluenesulfonic acid (88). Acid hydrolysis of the product at room temperature led to the formation of the 17-monoesters (97) ia nearly quantitative yield. The 17-monoesters (97) underwent acyl migration to the 21-monoesters (98) on careful heating with. In this way, prednisolone 17a,21-methylorthovalerate was converted quantitatively iato prednisolone 17-valerate, which is a very active antiinflammatory agent (89). The iatermediate ortho esters also are active. Thus, 17a,21-(l -methoxy)-pentyhdenedioxy-l,4-pregnadiene-liP-ol-3,20-dione [(96), R = CH3, R = C Hg] is at least 70 times more potent than prednisolone (89). The above conversions... 

Analgesics. Four examples of antiinflammatory agents are Sulindac [38194-50-2] based on a monofluoro indene derivative diflunisal... 

Few appHcations for fluoronaphthalenes and related polycycHc stmctures have materialized. The fused-ring bicycHc, suHndac [38194-50-2] a monofluorinated indene-3-acetic acid, is used as an antiinflammatory agent. 

See Analgesics, antipyretics, and antiinflammatory agents Chemotherapeutics, anticancer Immunotherapeutic agents. 

A new generation of antiinflammatory agents having immunosuppressive activity has been developed. The appearance of preclinical and clinical reports suggest that these are near entry to the pharmaceutical market. For example, tenidap (CP-66,248) (12) has been demonstrated to inhibit IL-1 production from human peripheral blood monocytes in culture (55). Clinically, IL-1 in synovial fluids of arthritic patients was reduced following treatment with tenidap. Patients with rheumatoid or osteoarthritis, when treated with tenidap, showed clinical improvement (57,58). In addition to its immunological effects, tenidap also has an antiinflammatory profile similar to the classical NSAIDs (59). Other synthetic inhibitors of IL-1 production are SKF 86002 (20) andE-5110 (21) (55). 

Synthetic Derivatives of Indoles as Pharmaceuticals. Thousands of indole derivatives have been prepared and evaluated as potential pharmaceuticals (32). Of those which have been put into use perhaps the most important are the nonsteroidal antiinflammatory agent indomethacin [53-86-1] (10) (33) and the p-adrenergic blocker pindolol [13823-86-9] (11) (34). 

From 1981 to 1995 other dmgs switched to OTC were the antifiingal preparations containing micona2ole nitrate [22832-87-7] (7) and clotrima2ole [23593-75-1] (8) the antiinflammatory agent ibuprofen [15687-27-1] (9) and the histamine H2-receptor antagonists famotidine [76824-35-6] (10) and cimetidine [51481-61-9] (11). 

Nonsteroidal Antiinflammatory Drugs. Nonsteroidal antiinflammatory dmgs (NSAIDs) include, among the numerous agents of this class, aspirin (acetylsaflcyhc acid), the arylacetic acids indomethacin and sulindac, and the arylpropionic acids, (5)-(147) and (R)-(148) ibuprofen, (5)-(149) and (R)- (150), flurbiprofen naproxen (41), and fenoprofen (see Analgesics, antipyretics, and antiinflammatory agents Salicylic acid and related compounds). 

Many 1,2,3,5-benzenetetrol derivatives are used mediciaaHy. For example, khellin [82-02-0] (65), which is a naturally occurring benzopyranone, is used as a coronary vasodilator and bronchodilator (233). Derivatives of khellin are effective local anesthetics and antiarrythmics (234). Similarly, amine derivatives (68) that are prepared from khellinone oxime (66) exhibit hypnotic, sedative, anticonvulsant, antiinflammatory, cardiac analeptic, diuretic, and antiulcerous activity (235) (see Analgesics, antipyretics, and antiinflammatory agents). 

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