Synthesis, characterization and antibiotic evaluation of various biologically active derivatives of 4-Alkylpyrimidine-5-carbonitrile

Thanki, P.; Hingrajiya, D.; Modha, J.; Vadgama, J.

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Current Chemistry Letters

ISSN 1927-730x (Online) - ISSN 1927-7296 (Print) Quarterly Publication Volume 12 Issue 3 pp. 537-544 , 2023

Synthesis, characterization and antibiotic evaluation of various biologically active derivatives of 4-Alkylpyrimidine-5-carbonitrile Pages 537-544 Download PDF

Authors: Pragna H. Thanki, Dhaval V. Hingrajiya, Jayesh J. Modha, Jalpa H. Vadgama

DOI: 10.5267/j.ccl.2023.3.002

Keywords: Pyrimidine Analogs, Biologically active, Pharmacophoric Groups, Antibacterial, Antibiotic Evaluation

Abstract: Extensive research work has been published on Tetrahydro and Dihydropyrimidine derivatives. Pyrimidine-5-Carbonitrile and its analogs have demonstrated a large number of activities. Some 6-Halogenosubstituted pyrimidine analogs have also been reported to be biologically active to a certain extent, but the literature survey reveals not much report on 6-alkylated pyrimidine derivatives. Targeting enhancement in biologically useful properties of a lead molecule through the association of it with active pharmacophoric groups or molecules is a conventional method in pharmaceutical research. With an aim to explore a better useful Dihydropyrimidine derivative, a newer 4-Alkylated-1,6-dihydropyrimidine analog (1) has been prepared. The lead molecule (1) has further been converted to amine derivative (2), hydrazino derivative (3) tri substituted s-triazinyl derivative (4), sulphonamide (5), Schiff’s base (6), a thiazolidinones (7), and 2-Azetidinones (8) respectively using various methods. Compounds 2, 4, 5, and 7 showed 50% and 8 showed 100% bacterial inhibition at 32μg/mL in single-point bacterial inhibition against various bacterial strains.

How to cite this paper

 Thanki, P., Hingrajiya, D., Modha, J & Vadgama, J. (2023). Synthesis, characterization and antibiotic evaluation of various biologically active derivatives of 4-Alkylpyrimidine-5-carbonitrile.Current Chemistry Letters, 12(3), 537-544.

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