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Chemical modification of acetaminophen：PASS assisted in vivo antiinflammatory activity of chalcones,flavanones and Schiff bases

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Journal of Chinese Pharmaceutical Sciences 2017年第8期26卷 611-620页

作者： syed misbahul hasan Shah Alam Khan Kavita Golani Jaswinder Lamba Aftab Ahmad Asif Husain Department of Pharmaceutical Chemistry School of Pharmaceutical Education and Research Jamia Hamdard (Hamdard University)New Delhi 110062 India Faculty of Pharmacy Integral University Lucknow UP 226026 India Department of Pharmacy Oman Medical College PO Box 620 Postal code-130 Muscat Sultanate of Oman Health Information Technology Department Jeddah Community College King Abdulaziz University deddah Kingdom of Saudi Arabia

In the present study,synthetic chalcones,flavanones and Schiff bases were prepared starting from paraceamol,and evaluated their anticipated anti-inflammatory *** were synthesized by reacting 3-acetyl-4-hydroxy acetanilide and aromatic aldehydes in alcoholic potassium hydroxide(KOH) solution under Claisen-Schmidt condensation *** chalcones were cyclized in the presence of piperidine in isoamyl alcohol to obtain flavonone *** bases were synthesized by condensing 3-acetyl-4-hydroxy anilines with aromatic aldehydes in the presence of *** Schiff bases were further reacted with other aromatic aldehydes in alcoholic KOH *** cheminformatics software was used to predict the anti-inflammatory activity of synthesized *** software predicted that chalcone-based Schiff bases 6a–d contained structural features that can exhibit anti-inflammatory *** the prepared derivatives of acetaminophen exhibited moderate to excellent in vivo anti-inflammatory activity in carrageenan-induced edema in rat *** the Schiff bases coupled chalcones showed good anti-inflammatory activity compared with the reference drug,*** evaluation of their therapeutic potential and safety profile is required in the future study.

关键词： p-Acetaminophen Anti-inflammatory Chalcone Flavanone

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