SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME NEWER 3-N-ARYL AMINO ACETAMIDO THIENOPYRIMIDINONE DERIVATIVES
Ramamurthy Subbayan* and Jayachandran Egambaram
ABSTRACT
Compounds containing thiophene and pyrimidine constitute major class of drugs with wide spectrum of biological activities. Many thienopyrimidinone analogs are also found to exhibit significant therapeutic value. Thus a new series of Thieno[2,3-d]-pyrimidin(3H)-4-ones have been synthesized and characterized. Starting from cycloheptanone and ethyl cyanoacetate the intermediate 2-Amino-3-carbethoxy-4, 5-penta methylene thiophene was prepared. This compound was acetylated and then condensed with hydrazine hydrate to yield the key intermediate 3-Amino -2-methyl-5, 6-pentamethylene thieno (2, 3-d) pyrimidin(3H)-4-one. This compound was chloro acetylated and then the active chlorine was replaced with aryl amino nucleophiles to get the title compounds. The title compounds have been purified and characterized by MP, TLC, IR, 1H NMR, Mass spectral data and elemental analysis. The compounds were screened for in vitro antibacterial and antifungal activities. It was observed that the compounds containing electron withdrawing groups showed significant activity. These compounds can be further exploited to get the potent lead compounds.
Keywords: Synthesis, Thieno [2,3-d]-pyrimidin(3H)-4-one, ,Characterization, Antibacterial, Antifungal.
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