All of the synthesized compounds were found potent hMAO-A inhibitors in in vitro screening tests. Only one of the in vivo tested three compounds, (3-(2-hydroxy-5-methylphenyl)-5- p-tolyl-4,5-dihydropyrazol-1-yl)(pyridin-4-yl) methanone indicated significant antidepressant activity. This article opens a window for further development of new pyrazoline and hydrazone derivatives as antidepressant agents.
Amaç: Bu çalışmada öncelikle şalkonlar ve bu şalkon türevlerinin hidrazitler ile reaksiyonu sonucu halka kapanması ile oluşan 4,5-dihidro-1H-pirazol yapısındaki bileşikler sentez edilmiş ve sentezlenen tüm bileşiklerin antimikrobiyal ve antitüberküler etkileri araştırılmıştır.Gereç ve Yöntem: Benzaldehit ve asetofenon türevlerinin alkali ortamda metanol içindeki reaksiyonuyla elde edilen şalkonların, hidrazit türevleri ile etanol içindeki reaksiyonu sonucu 4,5-dihidro-1H-pirazol türevleri elde edilmiştir. Sentezlenen bu bileşiklerin antimikrobiyal etkileri mikrodilüsyon yöntemiyle, antitüberküler etkileri ise mikroplaka alamar mavisi deneyi ile saptanmıştır.Sonuç ve Tartışma: Comparing E. coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, Pseudomonas aeruginosa izolat (gentamisine dirençli) ve Candida albicans'a karşı 4,5-dihidro-1H-pirazol yapısındaki bileşiklerin şalkonlardan daha etkili olduğu bulunmuştur. Staphylococcus aureus'a karşı ise şalkonlar 4,5-dihidro-1H-pirazol türevlerinden daha etkili bulunmuştur. Staphylococcus aureus izolat (MRSA)
Research in experimental epilepsy models and clinical investigations on epilepsy patients have provided important evidence that neuroinflammation has an effective role in epilepsy pathophysiology. Particularly, the effects of neuroinflammation-related pathways and mediators in the epileptogenesis process have been the subject of intensive research, and the elucidation of these processes has become important for the development of antiepileptogenic therapies and epileptogenic biomarkers. As a result of these studies, many pathophysiological processes have been determined and antiepileptogenic therapeutic targets have been defined. In this review, the main mechanisms involved in neuroinflammation in the epileptogenesis process are addressed and potential targets are reviewed focusing on developing antiepileptogenic therapy.
A series of hydrazone derivatives were synthesized to investigate antifungal, antimicrobial and antitubercular activities. These activities were investigated against Escherichia coli, Escherichia coli isolate, Pseudomonas aeruginosa, Pseudomonas aeruginosa isolate (resistant to gentamicin), Staphylococcus aureus, Staphylococcus aureus isolate (MRSA), Enterococcus faecalis, Enterococcus faecalis isolate (VRE), Candida albicans, Candida krusei and Mycobacterium tuberculosis. Among the synthesized compounds B23 had the best activity against Candida albicans with 16 µg/mL MIC value and B24 had the best activity against Staphylococcus aureus isolate (MRSA) with 16 µg/mL MIC value. The most effective compound against Mycobacterium tuberculosis is found to be E9 with 32 µg/mL MIC value, a chalcone derivative. However, all compounds were determined as ineffective against Escherichia coli and Escherichia coli isolate.
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