Synthesis of Some Novel Thiazolo[3,2‐a]pyrimidine and Pyrimido[2,1‐b][1,3]thiazine Derivatives and their Antimicrobial Evaluation

Abstract

A 2‐(2‐Mercapto‐4‐(4‐phenoxyphenyl)‐6‐(thiophen‐2‐yl)‐1,6‐dihydropyrimidin‐5‐yl) acetic acid was used as a reactive key precursor to design various pyrimidine derivatives such as thiazolo[3,2‐a]pyrimidines and pyrimido[2,1‐b][1,3]thiazines. The chemical structures of the newly synthesized products were confirmed by their elemental analyses and spectral data (IR, 1H NMR, 13C NMR, and mass spectra). The antibacterial and antifungal activities of some of the synthesized products were also evaluated, and it was found that compounds 3, 5, 9, and 11 exhibited potent activity against tested microorganisms in comparison with standard drugs.

Recent Development of Pyrimidine‐Containing Antimicrobial Agents

“…(Table 3) Tetrazolopyrimidine attached to the pyrazole was a new structural type that could increase antibacterial activity. Besides, Behalo et al [42] prepared several novel thiazolo [3,2a]pyrimidines with potent activity against Streptococcus sp., B. subtilis, E. coli, A. niger and C. albicans compared to reference streptomycin and ketoconazole, which indicated that pyrimidine derivatives with thiazole or isoxazole moiety (compounds 69 and 70) ( Figure 12) were essential for enhancing antimicrobial activity.…”

Facile synthesis of quinazoline, oxazine and triazole derivatives as potential antimi-crobial agents based on isothiocyanate moiety

“…In addition ,is othiocyanates are a class of organic compounds with well-known potent pharmaceutical applications [18,19] and are very popular in drug discovery [20][21][22] On the basis of these experiences and in continuation of our ongoing interest in the design of bioactive heterocyclic molecules [23][24][25][26][27], the present work involves a facilesynthesis of a series of five and six-membered heterocyclic compounds as triazole, quinazoline, thiazolidine and oxazine derivatives using 2-(4-phenoxybenzoyl)benzoyl is othiocyanate(2).…”

Green synthesis, cytotoxicity and antimicrobial activities of some new pyrazolines, pyrimidines and naphthyridines based on 1,3-di(thien-2-yl)prop-2-en-1-one using choline chloride-urea mixture as a deep eutectic solvent

“…In addition, pyrimidine derivatives are an important group of heterocyclic compounds that possess wide range of pharmacological properties, which include their uses as antimicrobial [17][18][19][20], anticancer [21][22][23][24][25], antitumor [26], antioxidant [27], anti-inflammatory [28] and antiviral [29].In view of these observations and in continuation to our ongoing interest in the design of bio-active heterocyclic molecules [30][31][32][33][34][35], the present work involves synthesis of chalcone derivatives using choline chloride-urea mixture as a deep eutectic solvent and construct a series of new heterocyclic molecules that have remarkable biological activities.…”