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Synthesis, docking studies and anti-inflammatory activity of some 2-amino-5,6,7,8-tetrahydroquinoline-3-carbonitriles and related compounds
O. I. Abd El-Salam 1, D. A. Abou El Ella 2, N. S. M. Ismail 2, M. Abdullah 3
Affiliations
Article Info
1 Applied Organic Chemistry Department, National Research Centre, Dokki, Cairo, 12622, Egypt, Email: oiel_salam@yahoo.com
2 Pharmaceutical Chemistry Department, Faculty of Pharmacy, Ain-Shams University, Cairo, Egypt
3 Research Units, Hi-Care Pharmaceutical Co., Cairo, Egypt
Abstract
A series of 2-amino-5,6,7,8-tetrahydroquinoline-3-carbonitriles 4a–c has been synthesized and reacted with various reagents. Docking studies into the catalytic site of p38 mitogen activated protein kinase (MAPK) were used to identify potential anti-inflammatory lead compounds. The anticipated lead derivative 2-(pyridin-3-yl)-5-(4-methoxyphenyl)-6,7,8,9-tetrahydropyrimido[4,5-b]quinolin-4-amine 9b was endowed with good binding energy. Also, the obtained products were evaluated for their in vivo anti-inflammatory activity as prostaglandin inhibitiors (% inhibition of edema and % inhibition of plasma PGE2 at the two dose levels were determined). The tested compounds exhibited significant anti-inflammatory activity and minor ulcerogenic effects, when compared to the reference standard indomethacin, with product 9b being of particular interest.