Synthesis and Anti‐Inflammatory Activity of Novel (4‐Hydroxyphenyl)(2,4‐dimethoxyphenyl) Methanone Derivatives

Abstract

In the scope of the research program aiming to perform the synthesis and pharmacological evaluation of novel possible anti-inflammatory compounds, in this manuscript, we report the synthesis of novel carboxamide 9a-d and thioamide 10a-d derivatives from the benzophenone and piperidine nucleus. Variation in the functional group at the N-terminal of piperidine led to two sets of compounds, bearing the carboxamide and thioamide, respectively. The characterization of this new class of compounds was performed with (1)H-NMR, LC-MS, IR, and elemental analysis. The newly synthesized compounds were screened for their anti-inflammatory activity by carrageenan-induced foot pad oedema assay and were compared with a standard drug. All the compounds exhibited anti-inflammatory activity at the dose of 30 mg/kg p.o. with varying degree from 52 to 67% inhibition of oedema. The compounds 9d and 10d with dichloro and fluoro substitution showed more potent activity at 30 mg/kg p.o. than the standard drug.

Efficient synthesis of piperidine derivatives using dendrimer based catalytical pockets

“…Piperidine derivatives are mainly used as Insect repellents [2], selective serotonin reuptake inhibitors [3], stimulants [4], selective estrogen receptor modulators [5], vasodilators [6], etc. Piperidine and its derivatives are biologically active molecules, therapeutic agents [7], anti-hypertensive [8], anti-bacterial [8], anticonvulsant [9], and anti-inflammatory agents [10]. They are commonly used in chemical degradation reactions, such as the sequencing of DNA in the cleavage of particular modified nucleotides, and used as a base for the deprotection of Fmoc amino acids used in solid-phase peptide synthesis [11].…”

Synthesis and Antileukemic Activity of Novel 2‐(4‐(2,4‐dimethoxybenzoyl)phenoxy)‐1‐(4‐(3‐(piperidin‐4‐yl)propyl)piperidin‐1‐yl)ethanone Derivatives

“…Compounds containing piperidine moiety play an important role in the field of medicinal chemistry. Derivatives of this class possess useful biological activities such as herbicidal, insecticidal, fungicidal, bactericidal, anti-inflammatory, antihistaminic, hypotensive, anticancer, CNS stimulant and depressant, and nerve activities (16)(17)(18)(19)(20)(21)(22)(23).…”

Synthesis and Antileukemic Activity of Novel 4‐(3‐(Piperidin‐4‐yl) Propyl)Piperidine Derivatives

“…Piperidine moiety‐containing molecules play an important role in the field of medicinal chemistry. Several derivatives of this class have found such useful biological applications as fungicidal, bactericidal, anti‐inflammatory, antihistaminic, wound healing, anticancer, CNS stimulant, and depressant activities (4–10). Compounds containing amide bond substitution can alter the chemical properties, disposition, and biological activities of drugs (11).…”