Abstract
Several new pyrazole, pyridine, [1,2,4]triazolo[1,5-α]pyrimidine, benzimidazo[1,2-a]pyrimidine and 1,2,4-triazolo[3,4-c][1,2,4]triazine derivatives incorporating a thiophene moiety were synthesized from (E)-ethyl 5-(3-(dimethylamino)acryloyl)-4-phenyl-2-(phenylamino)thiophene-3-carboxylate (1). The structures of the newly synthesized compounds were confirmed by IR, 1H-, 13C-NMR, mass spectral data and elemental analysis. The antibacterial and antifungal activities of all the synthesized compounds were evaluated. The results indicated that compounds 9, 12, and 19 were found to be more potent than the standard drug Amphotericin B against Aspergillus fumigates. Additionally, compound 12 exhibited higher activity than the standard drug Amphotericin B against Syncephalastrum racemosum.
Highlights
The synthesis and study of thiophene derivatives have been of interest due to their facile synthesis and broad spectrum of biological and pharmacological activities
A literature survey indicated that heterocyclic compounds containing thiophene ring were found to exhibit wide range of biological activities, such as antioxidant [1], anti HIV [2], anesthetic [3], bactericidal [4], antifungal [5], anti-inflammatory [1,6], antitubercular [7], and antitumor [8,9,10] activities
The aforementioned facts stimulated our interest for the synthesis of novel heterocyclic compounds containing thiophene ring utilizing enaminone 1 [18] as a key precursor to fulfill our objectives
Summary
The synthesis and study of thiophene derivatives have been of interest due to their facile synthesis and broad spectrum of biological and pharmacological activities. Enaminones are versatile starting materials for the synthesis of fused ring systems. These synthons were reacted with several nucleophilic and electrophilic reagents to construct new heterocyclic systems [16,17]. The aforementioned facts stimulated our interest for the synthesis of novel heterocyclic compounds containing thiophene ring utilizing enaminone 1 [18] as a key precursor to fulfill our objectives.
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