Abstract
New series of 2,3-disubstituted quinazolin-4(3H)- one were synthesized via the reaction of the readily obtainable 2-thioxo-3-phenyl-quinazolin-4(3H)one 1 with ethyl chloroacetate followed by hydrazinolysis to afford the hydrazide 3 which allowed to react with different electrophilic reagents such as carbon disulphide, phenyl isothiocyanate, β-diketones, anhydrides, acrylonitrile, ethyl cinnamate, dimethyl acetylene dicarboxylate, aldehydes, arylidene malononitrile and lauroyl chloride. Some of the newly synthesized compounds showed promising anti-inflammatory activity.
Highlights
Several Quinazolinone derivatives were synthesized as potential antimicrobial[1,2], anticancer[3,4,5,6,7], anti-inflamematory[8,9,10,11], and antimalarial[12] agents
Quinazolin-4(3H)one is a frequently encountered unit in natural products such as L-vasicinone[13], chrysogine[14,15] and drugs as Methaqualone[16], i.e. molecules based on quinazoline and quinazolinone exhibit a multitude of interesting pharmacological activities[17,18,19]
When the hydrazide 3 was treated with carbon disulphide in ethanolic potassium hydroxide, no combination was detected between the hydrazide 3 and the carbon disulphide and the solid separated was identified as the sulfur free compound which assigned as 3-phenyl- quinazolin-2,4(1H,3H)-dione5
Summary
Several Quinazolinone derivatives were synthesized as potential antimicrobial[1,2], anticancer[3,4,5,6,7], anti-inflamematory[8,9,10,11], and antimalarial[12] agents. Quinazolin-4(3H)one is a frequently encountered unit in natural products such as L-vasicinone[13], chrysogine[14,15] and drugs as Methaqualone[16], i.e. molecules based on quinazoline and quinazolinone exhibit a multitude of interesting pharmacological activities[17,18,19]. Aforementioned findings promoted the authors to synthesis a varieties of 2, 3-disubstituted quinazolinone derivatives via the utility of the key starting material 2-thioxo3-phenyl quinazolin 4(3H)one1[20,21]
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