Cytotoxic and antimicrobial activities of some novel heterocycles employing 6-(1,3-diphenyl-1H-pyrazol-4-yl)-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile

Abstract

A pyrimidinethione derivative namely, 6-(1,3-diphenyl-1H-pyrazol-4-yl)-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile, was readily synthesized and reacted with carbon electrophiles in an attempt to synthesize selected fused heterocycles. The reactivity of 6-(1,3-diphenyl-1H-pyrazol-4-yl)-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile was investigated towards selected nitrogen nucleophiles. Thiation and hydrolysis reactions of the tetrahydropyrimidine derivative were investigated. Antitumor and antimicrobial activity evaluation of some of the synthesized products exhibited promising results.

Synthesis and cytotoxicity against tumor cells of pincer N-heterocyclic ligands and their transition metal complexes

“…14,15 The pyrazole scaffold is a privileged pharmacophore encountered in many chemical compounds conrmed to be associated with various biological assets such as anti-inammatory, 16 antimicrobial and anticancer properties. 17,18 Furthermore, many compounds bearing a pyridine moiety have been identied to be biologically active [19][20][21][22] and therapeutically relevant in medicinal chemistry and to display versatile biological activities including antibacterial and anticancer activities. 18,23 In view of their biological signicant activity, the combination of pyrazole and pyridine moieties may lead to the synthesis of a new class of therapeutical active compounds, and is thus very much attractive.…”

Tyrosine-Derived Novel Benzoxazine Active in a Rat Syngenic Mammary Tumor Model of Breast Cancer

“…1,4-Benzoxazinone “G” inhibits the coagulation serine proteases factor Xa, thrombin and factor VIIa, and compound “H” possesses a dual antithrombotic action, exhibiting both thrombin inhibitory and fibrinogen receptor antagonistic activities. Apart from benzoxazine derivatives, some other skeletons showed anti-breast cancer activity in the MCF-7 cell line (pyrimidinethione derivatives, pyrrolone derivatives, quinazolinone derivatives, 1,3-diphenylpyrazole derivatives, 1,3-diphenylpyrazolyltetrahydropyrimidine derivatives, Chromone–Pyrazole)…”

Evaluation of some new heterocycles bearing 2‐oxoquinolyl moiety as immunomodulator against highly pathogenic avian influenza virus (H5N8)

“…In turn, furan‐2(3 H )‐ones are of considerable interest as they are versatile key materials for synthesis of a variety of heterocycles having a diverse of pharmacological applications [8–18]. Furthermore, quinolin‐2(1 H )‐ones are of fascinating interest according to their role in natural products and their pharmacological effects [19–27]. The present work deals with synthesis of quinolin‐2(1 H )‐one‐based heterocycles, for example, pyrrolone, pyridazinone, oxadiazole, and triazole derivatives, to enhance the antiviral activity and selectivity toward highly pathogenic avian influenza virus (H 5 N 8 ).…”