Design, synthesis, antimicrobial activity and anticancer screening of some new 1,3-thiazolidin-4-ones derivatives

Synthesis of Multifunctionalized 2-Iminothiazolidin-4-ones and Their 2-Arylimino Derivatives

“…Among them, the 1,3-thiazolidin-4-one core has been widely explored due to its versatile biological properties. [1][2][3] In particular, 2-iminothiazolidin-4ones I (Figure 1) display antifungal, [4][5][6] anti-inflammatory, 7,8 anticonvulsant, 9,10 hypnotic, 11 and antibacterial 6,12 activities. On the other hand, pyrazole scaffolds have also been largely exploited by medicinal chemists, leading to the development of valuable bioactive compounds.…”

“…Further optimizations related to the amounts of DBU and phenyl isothiocyanate (entries 8-10) showed that the use of 3 equivalents of phenyl isothiocyanate allowed a significant improvement of the NMR yield (54%, entry 9). Afterwards, the dilution effect was examined (entries [11][12][13][14]. Optimal conditions using 0.1 M pyrazole 4c, DBU (1 equiv), and phenyl isothiocyanate (3 equiv) led to 7a in an improved 70% NMR yield and 45% isolated yield (entry 12).…”

Design and synthesis of novel lactam/thiazole derivatives having five membered thiazolyl ring and their antimicrobial activity

“…Changes in the four-membered -lactam nucleus's substituent have been demonstrated to have a substantial impact on conferring promising microbial activity [3]. B-lactam moiety exhibits outstanding antibacterial [4], antimicrobial [5], anti-inflammatory [6], anticonvulsant [7], and antitubercular effects [8]. They also inhibit enzymes and have a beneficial effect on the central nervous system.…”

Design, Synthesis, Molecular Docking, and Evaluation Antioxidant and Antimicrobial Activities for Novel 3-Phenylimidazolidin-4-One and 2-Aminothiazol-4-One Derivatives

“…For a long time, thiazole derivatives were of great interest to scientists due to their significant and numerous pharmacological activities [ 5 ]. Thiazole derivatives have shown promise as therapeutic medicines such as anticancer [ 6 ], antimicrobial [ 7 ], antidiabetic agents [ 8 ], antiviral agents [ 9 ]. The fused imidazole was designed and drug discovery because it has a tremendous synthetic versatility that permits structural modifications throughout its periphery.…”