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Triazole derivatives
Triazole derivatives R 0280Synthesis, Characterization and Antiinflammatory-Analgesic Properties of 6-(α-Amino-4-chlorobenzyl)thiazolo[3,2-b]-1,2,4-triazol-5-ols. -Thiazolotriazole derivative (IV), an active compound in naproxen series, is subjected to Michael addition with secondary amines yielding addition products (VI) in a diastereoselective fashion. Adducts (VI) show significant analgesic and anti-inflammatory activities. Within the series (acetylphenyl)piperazine (VIb) displays the highest and dose-dependent analgesic and anti-inflammatory activity without inducing any gastric lesion. -(TOZKOPARAN, B.; GOEKHAN, N.; KUEPELI, E.; YESILADA, E.; ERTAN*, M.; Arzneim.-Forsch. 54 (2004) 1, 35-41; Dep. Pharm. Chem., Fac. Pharm., Hacettepe Univ., TR-06100 Ankara, Turk.; Eng.) -H. Hoennerscheid
Activities of 6-Acyl-3-piperazinomethyl-2-benzoxazolinones. -A variety of new piperazinomethylbenzoxazolinones (VI) (16 examples) are synthesized by Mannich reaction and evaluated for their pharmacological activities. Derivative (VIa) shows analgesic and antifungal activities comparable to those of acetylsalicylic acid and fluconazole, respectively. -(GOEKHAN*, N.; ERDOGAN, H.; DURLU, N. T.; DEMIRDAMAR, R.; OEZALP, M.; Arzneim. -Forsch. 53 (2003) 2, 114-120; Dep. Pharm. Chem., Fac. Pharm., Hacettepe Univ., TR-06100 Ankara, Turk.; Eng.) -F. Santoso
The effect of molecular variation by changing the 6-acyl moiety into a 5-acyl moiety, cf. (VIII) and (XI), on the analgesic-antiinflammatory activities is investigated. The C-acylation of benzoxazolinone (III) is carried out taking advantage of the AlCl3/DMF complex used as Friedel-Crafts catalyst. The acylation proceeds with satisfactory rate and yield, only when a substrate/catalyst ratio of 11:7 is used. A classical Mannich procedure completes the reaction sequence. In vivo studies reveal that the analgesic and antiinflammatory activities of (VIIIa) and (VIIIb) are comparable to those of Aspirin and Indometacin. In spite of its potent activity, (VIIIc) is ulcerogenic. Less remarkable results are obtained with compounds (XI) bearing the acyl group at 5-position of the main ring. -(KOEKSAL, M.; GOEKHAN*, N.; KUEPELI, E.; YESILADA, E.; ERDOGAN, H.; Arch. Pharm. (Weinheim, Ger.) 338 (2005) 2-3, 117-125; Dep. Pharm. Chem., Fac. Pharm., Hacettepe Univ., TR-06100 Ankara, Turk.; Eng.) -H. Hoennerscheid 35-139
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
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