Abstract
Objectives: Synthesis, characterization, and evaluation of antimicrobial activity of novel pyrimidine derivatives containing O, N, and S in the ring.
 Methods: Pyrimidine derivatives were prepared in three steps. In the first step, chalcones containing -NO2 functional group were synthesized using Claisen-Schmidt condensation of aromatic aldehydes with 2-acetyl pyridine/3-acetylpyridine in methanol in the presence of aqueous NaOH. In the second step, -NO2 group was reduced to -NH2 group. Resulting compounds containing NH2 functional group were reacted with different dichlorothienopyrimidines and dichlorofuropyrimidines in the presence of N,N-diisopropylethylamine to obtain pyrimidine derivatives.Antibacterial and antifungal activity of pyrimidine derivatives were studied in vitro.
 Results: Pyrimidine derivatives were synthesized and purified using flash column chromatography. Purity of synthesized pyrimidines was determined by high-performance liquid chromatography. Pyrimidines were characterized by elemental analysis, infrared, nuclear magnetic resonance, and mass spectral analysis. Analytical data of synthesized pyrimidines supported the proposed structures. Significant antibacterial and antifungal activity were observed in the synthesized pyrimidine derivatives.
 Conclusion: Antibacterial and antifungal activity of the newly synthesized pyrimidine derivatives will definitely inspire future researchers for the preparation of new analogs.
Highlights
Pyrimidine and its derivatives having two nitrogen atoms at 1 and 3 positions of aromatic ring are found in nature
Progress of reactions was monitored both by thin-layer chromatography (TLC) using precoated silica plate (TLC Silica gel 60 F254) and high-performance liquid chromatography (HPLC)
Vibrational frequencies are presented in cm−1. 1H nuclear magnetic resonance (NMR) spectra were recorded on Bruker Avance, DPX 300 using tetramethylsilane as an internal standard and chemical shift values are presented in δ ppm
Summary
Pyrimidine and its derivatives having two nitrogen atoms at 1 and 3 positions of aromatic ring are found in nature. Pyrimidine derivatives synthesized in laboratory are reported in literature. Antibacterial [1,2,3,4], antifungal [5,6,7], antiHIV [8], antitubercular [9], antitumor [10], antineoplastic [11], antileishmanial [12], anti-inflammatory [13,14,15], antidiabetic [16], antipyretic [17], antioxidant [18,19], antihistaminic [20], anticancer [21,22], and herbicidal [23] properties of pyrimidine derivatives are reported in literatures. Pyrimidine derivatives were found to possess potential central nervous system-depressant properties [24,25] and to act as blocker of calcium channel [26].
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