• Archives of Pharmacal Research
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• 제24권3호
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• pp.180-189
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• 2001

A new series of pyridazine, pyrazoles, pyrazolidine-3,5-dione, Semicarbazide, thiosemicarbazides, hydantoin, thiohydantoins, 1,2,4-triazoles, S-triazolo[3,4-b]-1,3,4-thiadiazoles incorporated indirectly into salicylamide moiety at position 2 were synthesized. Also the synthesis of novel series of 3-salicylamido-2-hydroxypropyl-amino derivatives were prepared. Several of these compounds were screened for antiinflammatory, analgesic, antipyretic and ulcerogenic activities.

• Archives of Pharmacal Research
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• 제7권2호
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• pp.127-132
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• 1984

Systematic pharmacological astudies on pipeline have revealed that this compound elicited diverse pharmacological activities; CNS depressant activity characterized by antagonism against electo shock seizure and by muscle relaxant activity in mice; antipyretic activity in tyyhoid vaccinated rabbits; analgesic activity as evaluated by tail-clip pressure and writhing syndrome in mice; antiinflammatory activity in carrageenin-induced edema in rats.

• 약학회지
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• 제23권1호
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• pp.11-16
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• 1979

Benorylate and ethoxybenzamide have been used alone or in combination as an analgesic, antipyretic and antiinflammatory agent. We investigated the significance of the differences of analgesic activities between single and concurrent administration of benorylate and ethoxybenzamide and lorazepam in mice and also antipyretic activity between single and concurrent administration of benorylate and ethoxybenzamide in rats. 1). Concurrent administration of each half dose of benorylate and ethoxybenamide showed much inhibiting effect on the acetic acid-induced writhing syndrome of mice than the above drug alone, and the some increased analgesic response by hot plate method. 2). The synergistic and analgesic effect of combined administration of benorylate and lorazepam was found to be significant. 3). Antipyretic effect of half-dose combined administration of benorylate and ethoxybenzamide on the rat pyrexia induced by yeast(s.c.) and T.T.G. (i.v.) was shown to be similar to the effect of each drug.

• 생약학회지
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• 제26권1호
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• pp.66-73
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• 1995

'Gyejakjimo-Tang(桂芍知母湯)', which is composed of Cinnamon bark(桂枝), Peony root(芍藥), Anemarrhena root(知母) and other seven herbs, is described as antipyretic, diuretic and analgesic prescription in traditional medical literatures including Geumgwe-Yoryak(金櫃要略). So it is being used in the treatment of gout clinically in oriental region. As the results of the pharmacological and biochemical trials of the prescription, it was found to have antiinflammatory and significant analgesic effects indicated by carrageenin edema, dye permeabilities and writhing behavior. And it potentiated the output of uric acid in blood and the increase of uric acid in urine of alcohol-toxicated rats, which mean the decrease of uric acid level only by excretion procedure. But the prescription didn't show any effects on the activities of adenine/guanine deaminase, purine nucleoside phosphorylase, xanthine oxidase or uricase, which are related with formation and metabolism of uric acid.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1997년도 추계학술대회
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• pp.47-50
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• 1997

Drug development began with the finding of biologically active compounds which are obtained by chemical synthesis or from natural sources. The advent of Combinatorial Chemistry is recognized as a strategy which has a potential to change the methodology of research and development(R&D) of new drugs. Drug development has been carried out with diverse strategies. In the past several decades a variety of new methodology have been introduced in R&D. Random screening of accumulated synthetic samples which had been synthesized for development of other drugs led to the discovery of new drugs. The typical examples are anti-asthma drug trimethoquinol and calcium antagonist diltiazem. (herbesser). In particular the latter drug has been used as a calcium antagonist worldwide, however it was first synthesized to find new tranquilizer and this is the reason why diltiazem has benzodiazepam skeleton. The random screening contributed in the finding of new drugs were carried out with whole animal test and it is a standard methodology in R&D of new drugs. Aspirin is the first synthetic non-steroidal antiinflammatory drug(NSAID) and has been used for more than one hundred years. It is the first example of drug developed from natural product. Salicin is the main constituent of willow bark which had been used in Europe for a long time to treat arthritis and aspirin was developed from salicin. Most of NSAID used clinically were developed from the structure of aspirin, however it took 70 years to clarify why aspirin exhibits its antiinflammatory, analgesic and antipyretic activities. The target of aspirin is cyclooxygenase(COX)which is the first enzyme involved in arachidonate cascade leading to the production of prostaglandins(PG) and thromboxan(TX). Side effect of aspirin causing ulcer in stomach is rather serious problem, since aspirin is so popular drug easily obtained in drug store(OTP). This problem is now going to be solved by a new finding on COX, which have two different types, one is constitutionally expressed COX 1 in almost all organs and the other is inducible COX 2. COX 2 is the responsible enzyme in inflammation etc and now the search of COX 2 specific inhibitors is the target of R&D of next generation NSAID.