Synthesis, Analgesic, Anti-inflammatory and Antibacterial Activities of Some Novel 2-Methyl-3-substituted Quinazolin-4-(3H)-ones

Abstract

A series of novel 2-methyl-3-substituted quinazolin-4-(3H)-ones have been synthesized by treating (2-methyl-4-oxo-3H-quinazolin-3-yl)dithiocarbamic acid methyl ester with different amines, the starting material dithiocarbamate was synthesized from anthranilic acid. The compounds synthesized were investigated for analgesic, anti-inflammatory and antibacterial activities. All the test compounds exhibited significant activity, the compounds VA2, VA3 and VA4 shown more potent analgesic activity, and the compounds VA3 and VA4 shown more potent anti-inflammatory activity than the reference compound diclofinac sodium.

Synthesis, Analgesic, Anti-inflammatory and Antibacterial Activities of Some Novel 2-Butyl-3-substituted Quinazolin-4-(3H)-ones

“…Quinazolines and condensed quinazolines exhibit potent antimicrobial 1) and central nervous system (CNS) activities like analgesic, 2) anti-inflammatory 3) and anticonvulsant 4) activities. In view of these facts and to develop our earlier reported 2-phenyl-3-substituted quinazolines, 5) 2,3-disubstituted quinazolines, 6) 2-methyl-3-substituted quinazolin-4-(3H)-ones 7) and 2-methylthio-3-substituted quinazolin-4-(3H)-ones 8) that exhibited good analgesic and anti-inflammatory activities, in the present study we aimed to synthesize some 2-butyl-3-substituted quinazolin-4(3H)-ones. The title compounds were synthesized by nucleophilic substitution of (2-butyl-4-oxo-3H-quinazolin-3-yl)dithiocarbamic acid methyl ester with different amines.…”

Synthesis, Analgesic, Anti-inflammatory and Antibacterial Activities of some Novel 2-Methylthio-3-Substituted Quinazolin-4-(3H)-ones

“…Quinazolines and condensed quinazolines exhibit potent antimicrobial 1) and CNS activities like analgesic, 2) anti-inflammatory 3) and anticonvulsant 4) activities. In view of these facts and to develop our earlier reported 2-phenyl-3-substituted quinazolines, 5) 2,3-disubstituted quinazolines 6) and 2-methyl-3-substituted quinazolin-4-(3H)-ones 7) that exhibited good analgesic and anti-inflammatory activities, in the present study we aimed to synthesize some 2-methylthio-3-substituted quinazolin-4(3H)-ones. The title compounds were synthesized by nucleophilic substitution of (2-methylthio-4-oxo-3H-quinazolin-3-yl)dithiocarbamic acid methyl ester with different amines.…”

Reactions of organolithium reagents with quinazoline derivatives

“…56,70 The synthesis of quinazoline derivatives has attracted the attention of chemists and has importance in medicinal chemistry because of the pharmacological applications for this heterocyclic ring system. [71][72][73][74][75][76][77][78][79][80][81] Also, quinazoline derivatives are important intermediates in the synthesis of a variety of valuable heterocyclic compounds. [82][83][84][85][86] Therefore, methods for the syntheses and/or modification of this ring system are always of interest.…”