Evaluation of selective human MAO inhibitory activities of some novel pyrazoline derivatives

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Atıf İçin Kopyala

Salgin-Goksen U., Yabanoglu-Ciftci S., ERCAN A., Yelekci K., UÇAR G., Gokhan-Kelekci N.

JOURNAL OF NEURAL TRANSMISSION, cilt.120, sa.6, ss.863-873, 2013 (SCI-Expanded)

• Yayın Türü: Makale / Tam Makale
• Cilt numarası: 120 Sayı: 6
• Basım Tarihi: 2013
• Doi Numarası: 10.1007/s00702-013-0980-6
• Dergi Adı: JOURNAL OF NEURAL TRANSMISSION
• Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
• Sayfa Sayıları: ss.863-873
• Anahtar Kelimeler: 2-Pyrazoline, 2-Benzoxazolinone, Chalcone, Monoamine oxidase inhibitory activity, Molecular docking, HUMAN MONOAMINE-OXIDASE, 1-ACETYL-3,5-DIPHENYL-4,5-DIHYDRO-(1H)-PYRAZOLE DERIVATIVES, B INHIBITORS, DISEASE, ANTIBACTERIAL, CATALYSTS, BINDING, POTENT
• Hacettepe Üniversitesi Adresli: Evet

Özet

A series of 1-[2-((5-methyl/chloro)-2-benzoxazolinone-3-yl)acetyl]-3,5-diaryl-4,5-dihydro-1H-pyrazole derivatives were prepared by reacting 2-((5-methyl/chloro)-2-benzoxazolinone-3-yl)acetylhydrazine with appropriate chalcones. The chemical structures of all compounds were confirmed by elemental analyses, IR, H-1 NMR and ESI-MS. All the compounds were investigated for their ability to selectively inhibit monoamine oxidase (MAO) by in vitro tests. MAO activities of the compounds were compared with moclobemide and selegiline and all the compounds were found to inhibit human MAO-A selectively. The inhibition profile was found to be competitive and reversible for all compounds by in vitro tests. Among the compounds examined, compounds 5ae, 5af and 5ag were more selective than moclobemide, with respect to the K (i) values experimentally found. In addition, the compound 5bg showed MAO-A inhibitor activity as well as moclobemide. A series of experimentally tested compounds (5ae-5ch) were docked computationally to the active site of the MAO-A and MAO-B isoenzyme. The AUTODOCK 4.01 program was employed to perform automated molecular docking.