Triazole derivatives R 0280Synthesis of Some 3-(Arylalkylthio)-4-alkyl/aryl-5-(4-aminophenyl)-4H-1,2,4-triazole Derivatives and Their Anticonvulsant Activity. -The synthesis of the title triazoles (VI) is aimed at investigating antimicrobial and antimycobacterial properties in addition to their anticonvulsant activities. The primary amino group in (VI) is masked to observe the contribution of this function to pharmacological activity. Protective activities in the maximal electroshock (MES) test as well as in the subcutaneous pentylenetetrazole (sc PTZ) test are shown by triazoles (VIa) and (VIb). The novel triazoles are devoid of antibacterial and antimycobacterial activity. Triazoles (VIc) and (VIII) display marginal activity against M. tuberculosis H37. -(KUECUEKGUEZEL, I.; KUECUEKGUEZEL, G. S.; ROLLAS, S.; OETUEK-SANIS, G.; OEZDEMIR, O.; BAYRAK, I.; ALTUG, T.; STABLES, J. P.; Farmaco 59 (2004) 11, 893-901; Dep. Pharm. Chem., Fac. Pharm., Marmara Univ., Haydarpasa, TR-81010 Istanbul, Turk.; Eng.) -H. Hoennerscheid 12-136
imino--4-thiazolidinon-5-ylidene]-5-substituted/nonsubstituted 1H-Indole-2-ones and Investigation of Their Structure-Activity Relationships. -Several novel promising compounds such as (III) for the title pharmacological activities are synthesized. The activity of (IIIc) is close to that of cefuroxime sodium against Staphylococcus epidermidis ATCC 12228. The preparation of the starting materials (I) is also given. -(ALTINTAS*, H.; ATES, O.; UYDES-DOGAN, B. S.; ALP, F. I.; KALELI, D.; OEZDEMIR, O.; BIRTEKSOEZ, S.; OETUEK, G.; SATANA, D.; UZUN, M.; Arzneim.-Forsch. 56 (2006) 3, 239-248; Dep. Pharm. Chem., Fac. Pharm., Univ. Istanbul, Beyazit, TR-34452 Istanbul, Turk.; Eng.) -K. Schneider 30-137
Synthesis and Pharmacology of New Dithiocarbamic Acid EstersDerived from Phenothiazine and Diphenylamine.-Fourteen new esters such as (III) and (V) are synthesized and tested for antihistaminic and anticholinergic activities. The compounds show no significant anticholinergic activity. Esters (IIIc) and (Vc) exhibit moderate antihistaminic activity. In general, diphenylamines (V) are more active than phenothiazines (III). -
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