عنوان المقالة:تحضير وتشخيص وتقييم مضاد للالتهاب لبعض المشتقات الجديده لـ ۲-(۳-فلوروبايفنيل-٤-يل)حامض البروبانويك SYNTHESIS, CHARACTERIZATION AND ANTI-INFLAMMATORY EVALUATION OF SOME NEW 2-(3-FLUOROBIPHENYL-4-YL) PROPANOIC ACID DERIVATIVES
Ahmed W. Naser , Ahmed J. Al-Musawi , Ammar A. Fadhil and Nada N. Al-Shawi
الملخص الانجليزي
Different new compounds derived from 2-(3-flourobiphenyl-4-yl)
propanohydrazide [2] as starting material were synthesized. Reaction [2] with maleic
anhydride, succinic anhydride and phthalic anhydride gave the corresponding
cyclicimides [3a-c]. The hydrazone derivatives [4a-d] were obtained by condensation of
compound [2] with 2,4-dimethoxybenzaldehyde, 4-(N,N-dimethylamino)benzaldehyde,
3-hydroxybenzaldehyde and 2-hydroxybenzaldehyde. The cyclization of [2] with CS2
in
presence potassium hydroxide and hydrazine hydrate gave 1,2,4-triazole compound [5],
that condensation either with 2,4-dimethoxybenzaldehyde, 4-(N,N-dimethyl amino)
benzaldehyde, 3-hydroxybenzaldehyde and 2-hydroxybenzaldehyde to give the
corresponding Schiff-bases [6a-d]. The cyclization of hydrazone derivatives [4a-d] with
phenyl isocyanate, maleic anhydride, succinic anhydride and phthalic anhydride gave the
corresponding aza-β-lactams [7a-d], oxazepine [8,9,10 a-d]. The structures of new
compounds are supported by FT-IR, 1H-NMR and 13C-NMR. Compounds [3c], [4c],
[8d], [7d] and [4b] were evaluated in vivo for their anti-inflammatory activity comparable
to the standard drug flurbiprofen. Compound 2-(2-hydroxyphenyl)-3-[2-(3-
fluorobiphenyl-4-yl)] propan- amido-2,3-dihydro-1,3-oxazepine-4,7-dione [8d] showed
anti-inflammatory activity more than the standard drug flurbiprofen, in the egg-albumin
induced paw edema in rats.
تاريخ النشر
01/04/2017
الناشر
International Journal of Pharmaceutical Sciences and Research
احمد جعفر قاسم الموسوي | Ahmed Jaafar Qasim Al-Musawi | 7205