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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-amine derivatives were prepared. Several of these compounds were screened for antiinflammatory, analgesic, antipyretic and ulcerogenic activities. 相似文献
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In this study, eight new 1-(2-benzoxazolinone-6-yl)-2-(4-arylpiperazine-1-yl)ethanol and -propanol derivatives have been prepared. Their structures have been elucidated by IR- and 1H-NMR-spectra and by elementary analysis. The analgesic activities of these compounds, using modified Koster's test have been investigated. 1-(5-Chloro-3-methyl-2-benzoxazolone-6-yl)-2-[4-(2-methoxyphenyl)p iperazine-1- yl]ethanol has been found more active than O-acetyl-salicylic acid, respectively. 相似文献
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E. V. Shchegol’kov O. G. Khudina L. V. Anikina Ya. V. Burgart V. I. Saloutin 《Pharmaceutical Chemistry Journal》2006,40(7):373-376
1,2,3-Triketone 2-(antipyrin-4-yl)hydrazones were synthesized via the azo-coupling reactions of 1,3-diketones with 2-(antipyrin-4-yl)diazonium
chloride. The fluoroalkyl-containing hetarylhydrazone enters into cyclocondensation with hydrazines at the 1,3-dicarbonyl
fragment to yield 3-tetrafluoroethyl derivatives of pyrazole. It was found that 1,2,3-triketone 2-(antipyrin-4-yl)hydrazones
and N-(2-hydroxyethyl)-substituted pyrazole exhibit analgesic activity comparable with that of their structural analog analgin
(metamizole sodium), but do not possess antipyretic properties. In contrast, N-phenyl-substituted pyrazole did not exhibit
analgesic properties but produced a certain antipyretic effect four hours after pyrogenic administration. Fluoroalkyl-containing
compounds are less toxic substances than nonfluorinated 2-(antipyrin-4-yl)hydrazone and analgin.
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 40, No. 7, pp. 27 ‣ 29, July, 2006. 相似文献
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D. N. Ismatov U. M. Azizov M. K. Nurullaeva S. I. Iskandarov 《Pharmaceutical Chemistry Journal》1991,25(7):498-502
Translated from Khimiko-farmatsevitcheskii Zhurnal, Vol. 25, No. 7, pp. 56–59, July, 1991. 相似文献
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N. Najafi M. Pirali R. Dowlatabadi M. Bagheri N. Rastkari M. Abdollahi 《Pharmaceutical Chemistry Journal》2005,39(12):641-643
Several new N-(2,3-dihydro-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl)-2-carboxamides have been synthesized and characterized
with respect to acute toxicity (LD50), analgesic and antiinflammatory properties (formalin-and carrageenan-induced foot edema models), and interaction with morphine-induced
antinociception in mice. The new compounds were prepared by acyl coupling of 2-aminobenzophenones with α-(benzotriazol-1-yl)-N-acylglycines
followed by displacement of the benzotriazole ring with ammonia and cyclization of the resulting monoacyl aminals. The LD50 of the synthesized compounds exceeds 1000 mg/kg. Three compounds produced significant analgesic action in doses 100–150 μg/kg
in the early (painful) phase of the formalin test and potentiated the morphine-induced antinociception in this test. The synthesized
drugs neither showed antinociception in the second (inflammatory) phase of the formalin test nor decreased the carrageenan-induced
foot edema growth. Thus, the synthesized compounds produce analgesic action but do not possess antiinflammatory properties.
The analgesic activity is probably due to the interaction with μ-and δ-opioid receptors.
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 39, No. 12, pp. 21–23, December, 2005. 相似文献
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In an attempt to ascertain the pharmacological basis of the use of the marketed traditional drug Taverniera abyssinica A. Rich. (Amharic name Dingetegna), crude extracts as well as purified substances of this plant were tested for their antipyretic and analgesic properties. Antipyretic activity was determined on rats made hyperthermic by yeast injection and analgesic activity was determined by the hot plate, as well as the acetic acid induced writhing, methods. The study showed that the plant possesses significant antipyretic and analgesic activities. 相似文献
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M.T. GARCÍIA-LOPEZ R. GONZALEZ MUNNIZ R. HERRANZ H. BRAVO J.R. NARANJO J. Del RÍIO 《Chemical biology & drug design》1985,26(2):174-178
N-Phosphoryl dipeptides derived from Phe-Ala, Phe-Ala-NH2 and Phe-Gly-NH2 were synthesized and their analgesic activity was evaluated in mice. Intracere-broventricular administration of P-Phe-Ala-NH2 produced a 100-fold increase in the analgesic potency of Phe-Ala and led to a potentiation and prolongation of the analgesic effect of the exogenously administered Met-enkephalin. 相似文献
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N A Mokhort 《Farmakologiia i toksikologiia》1987,50(3):94-96
In experiments on rats with different models of pathology it was demonstrated that a new non-steroidal anti-inflammatory drug pyrimidant exerts pronounced anti-inflammatory, analgesic and antipyretic effects. In some cases its activity exceeds that of indomethacin, brufen, butadione, mefenamic acid, sodium salicylate. 相似文献
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目的:应用大鼠及小鼠研究赖氨匹林的抗炎、镇痛及解热作用。方法:用大鼠足跖肿胀研究抗炎作用,用小鼠醋酸扭体法及热板法测定镇痛作用,用鲜酵母法测定解热作用。结果:赖氨匹林对大鼠足跖肿胀有明显抑制作用,最大抑制率为80%(P<0.01)。小鼠醋酸扭体法测得镇痛ED50=72±23mg/kg,对鲜酵母致大鼠体温升高有明显抑制作用。小鼠半数致胃溃疡剂量UD50=0.18±0.06mmol/kg,是阿司匹林的2.4倍。结论:赖氨匹林具有和阿司匹林相当的解热、镇痛和抗炎作用,而对胃肠道的毒副作用比阿司匹林小。 相似文献