Design, Synthesis and Biological Evaluation of Novel N-Pyridyl-Hydrazone Derivatives as Potential Monoamine Oxidase (MAO) Inhibitors

A new series of N-pyridyl-hydrazone derivatives was synthesized by using a simple and efficient method. The final compounds obtained were screened for their inhibitory potency against monoamine oxidase (MAO) A and B. The newly synthesized compounds 2a–2n specifically inhibited monoamine oxidases, displaying notably low IC50 values. Compounds 2i and 2j, with a CF3 and OH group on the 4-position of the phenyl ring, respectively, showed considerable MAO-A and MAO-B inhibitory activities. Compounds 2k, 2l and 2n, with N-methylpyrrole, furan and pyridine moieties instead of the phenyl ring, were the most powerful and specific inhibitors of MAO-A, with IC50 values of 6.12 μM, 10.64 μM and 9.52 μM, respectively. Moreover, these active compounds were found to be non-cytotoxic to NIH/3T3 cells. This study supports future studies aimed at designing MAO inhibitors to obtain more viable medications for neurodegenerative disorders, such as Parkinson’s disease

Synthesis of some new hydrazone derivatives containing benzothiazole moiety

Hydrazones are important classes of compounds found in many synthetic products. Due to their importance in synthetic chemistry, the present article reports the synthesis of a new series of ten compounds based on the coupling of 2-[2(3H)-benzothiazolone-3-yl]acetylhydrazine and 2-(1,3- benzothiazol-2-yl)sulphanylacetylhydrazine with different aldehydes. The structures of the synthesized compounds were confirmed by elemental analyses, IR, 1H-NMR, 13C-NMR and FAB+-MS spectral data

BAZI N-(BENZOTİYAZOL-2-İL)-2-(4H-[1,2,4]TRİAZOL-3- İLSÜLFANİL)ASETAMİDLERİN SENTEZİ VE BUNLARIN ANTİMİKROBİYAL AKTİVİTELERİ

Bu çalışmanın amacı, yeni benzotiyazolil-amid türevlerini sentezlemek ve bunların antimikrobiyal aktivitelerini araştırmaktır. N-(benzotiyazol-2-il)-2-kloroasetamidler ile uygun 4H-[1,2,4]triazol-2tiyonların reaksiyona sokulmasıyla N-(Benzotiyazol-2-il)-2-(4H-[1,2,4]triazol-3-ilsülfanil) asetamid türevleri hazırlanmıştır. Sentezlenen bileşiklerin kimyasal yapıları elemental analiz, IR, 1H-NMR, 13CNMR ve FAB+-MS spektral verileri ile aydınlatılmıştır. Bunların antimikrobiyal aktiviteleri Escherichia coli (NRRL B-3008), Staphylococcus aureus (ATCC 6538), Pseudomonas aeruginosa (ATCC 27853), Proteus vulgaris (NRRL B-123), Salmonella typhimurium (ATCC 13311), Methicillin-resistant Staphylococcus aureus (MRSA) (clinic isolate), Candida albicans (NRRL Y-12983) ve Candida parapsilosis’e (NRRL Y-12696) karşı araştırılmıştır. Sonuçlar test edilen tüm bileşiklerin, test organizmalarına karşı inaktif olduğunu gösterd

BAZI N-(BENZOTİYAZOL-2-İL)-2-(4H-[1,2,4]TRİAZOL-3- İLSÜLFANİL)ASETAMİDLERİN SENTEZİ VE BUNLARIN ANTİMİKROBİYAL AKTİVİTELERİ

Bu çalışmanın amacı, yeni benzotiyazolil-amid türevlerini sentezlemek ve bunların antimikrobiyal aktivitelerini araştırmaktır. N-(benzotiyazol-2-il)-2-kloroasetamidler ile uygun 4H-[1,2,4]triazol-2tiyonların reaksiyona sokulmasıyla N-(Benzotiyazol-2-il)-2-(4H-[1,2,4]triazol-3-ilsülfanil) asetamid türevleri hazırlanmıştır. Sentezlenen bileşiklerin kimyasal yapıları elemental analiz, IR, 1H-NMR, 13CNMR ve FAB+-MS spektral verileri ile aydınlatılmıştır. Bunların antimikrobiyal aktiviteleri Escherichia coli (NRRL B-3008), Staphylococcus aureus (ATCC 6538), Pseudomonas aeruginosa (ATCC 27853), Proteus vulgaris (NRRL B-123), Salmonella typhimurium (ATCC 13311), Methicillin-resistant Staphylococcus aureus (MRSA) (clinic isolate), Candida albicans (NRRL Y-12983) ve Candida parapsilosis’e (NRRL Y-12696) karşı araştırılmıştır. Sonuçlar test edilen tüm bileşiklerin, test organizmalarına karşı inaktif olduğunu gösterd

Design, Synthesis and Biological Evaluation of Novel N-Pyridyl-Hydrazone Derivatives as Potential Monoamine Oxidase (MAO) Inhibitors

A new series of N-pyridyl-hydrazone derivatives was synthesized by using a simple and efficient method. The final compounds obtained were screened for their inhibitory potency against monoamine oxidase (MAO) A and B. The newly synthesized compounds 2a–2n specifically inhibited monoamine oxidases, displaying notably low IC50 values. Compounds 2i and 2j, with a CF3 and OH group on the 4-position of the phenyl ring, respectively, showed considerable MAO-A and MAO-B inhibitory activities. Compounds 2k, 2l and 2n, with N-methylpyrrole, furan and pyridine moieties instead of the phenyl ring, were the most powerful and specific inhibitors of MAO-A, with IC50 values of 6.12 μM, 10.64 μM and 9.52 μM, respectively. Moreover, these active compounds were found to be non-cytotoxic to NIH/3T3 cells. This study supports future studies aimed at designing MAO inhibitors to obtain more viable medications for neurodegenerative disorders, such as Parkinson’s disease