Synthesis and in vivo anti-ulcer evaluation of some novel piperidine linked dihydropyrimidinone derivatives

Abstract

Dihydropyrimidinone derivatives containing piperidine moiety were synthesised in a good yield. All the compounds were confirmed by elemental analysis and spectral data. Anti-ulcer activity of novel dihydropyrimidinone-piperidine hybrids (1–18) was evaluated. Among them, four compounds (3, 8, 11 and 15) were found to be most active in 80% ethanol-induced ulcer experimental animal model. All the potent compounds were further evaluated for anti-ulcer activity by different in vivo anti-ulcer models to study the effect of compounds on anti-secretory and cytoprotective activities. All the active compounds inhibited the formation of gastric ulcers and increased the formation of gastric mucin secretion. Compound 15 was found to be the most potent compound of the series as anti-ulcer agent. Additional experimental studies on lead compound 15 will result in a new class of orally active molecule for anti-ulcer activity.

A One-Pot Biginelli Synthesis and Characterization of Novel Dihydropyrimidinone Derivatives Containing Piperazine/Morpholine Moiety

“…The eight protons of morpholine moiety were observed as triplets at δH 3.20–3.22 ppm with coupling constant ( J = 4.7 Hz) for four protons and another triplet at δH 3.72–3.82 with coupling constant ( J = 4.6 Hz) for four protons. The H-4 and =CH protons of dihydropyrimidinone moiety were observed at δH 5.32–6.08 and 7.79–8.24 ppm, respectively [ 37 , 38 , 39 ]. 13 C NMR spectra confirmed the presence of all carbon atoms of compounds ( 1 – 20 ).…”

Electrochemical properties of non-peripherally and peripherally tetra-[(1-benzylpiperidine-4-yl)oxy] substituted phthalocyanines

“…For compounds containing the piperidine ring system in their chemical structure, many pharmacological activities such as antibacterial, antifungal, anticancer, antioxidant, antiulcer, and renin inhibitor have been reported [18][19][20][21][22][23][24]. In addition, the electrochemical properties of many groups of compounds containing piperidine rings have been examined and it has been reported that they show very different electrochemical properties [25][26][27].…”