Synthesis and characterization of new imidazolidineiminothione and bis-imidazolidineiminothione derivatives as potential antimicrobial agents

Abstract

A series of new imidazolidineiminothiones (2-4) and bis-imidazolidineiminothiones (5) were synthesized through the cycloaddition reaction of N-arylcyanothioformamides (1) with some electrophilic reagents. Structure of imidazolidineiminothione derivatives were established based on spectroscopic IR, 1 H NMR, 13 C NMR, MS and elemental analyses data. These compounds were screened for their antibacterial and antifungal activities. Among the synthesized compounds, imidazolidineiminothione derivative 3a showed about 25% less potent effect than Ampicillin against S. epidermidis and B. subtilis (MIC, 0.49 μg/mL) and about 50 % less potent effect than Amphotericin B against A. clavatus and G. Candidum. Bisimidazolidineiminothione derivative 5a was equipotent to the Gentamycin in inhibiting the growth of N. gonorrhoeae (MIC, 0.49 μg/mL), and displayed 50% less active than Amphotericin B against A. clavatus.

Sulfaguanidine Hybrid with Some New Pyridine-2-One Derivatives: Design, Synthesis, and Antimicrobial Activity against Multidrug-Resistant Bacteria as Dual DNA Gyrase and DHFR Inhibitors

“…Activation of T lymphocytes, natural killer, and macrophage cells mainly produce the cytokines that have immunomodulatory potential and plays a vital role in the immune response process by assisting the expulsion of abnormal cells [ 50 ]. In view of the above observations and in continuation of our program on the medicinal chemistry that demonstrated biological activity [ 51 , 52 , 53 , 54 , 55 , 56 , 57 , 58 , 59 , 60 ]. We report herein the synthesis of the versatile hitherto unknown 2-pyridone and chromeno-[3,4-c] pyridine derivatives containing the sulfaguanidine moiety in a single molecular framework; the rational study design is presented in Figure 1 .…”

“…Antibiotics 2021, 10, x FOR PEER REVIEW 3 of 31 the expulsion of abnormal cells [50]. In view of the above observations and in continuation of our program on the medicinal chemistry that demonstrated biological activity [51][52][53][54][55][56][57][58][59][60].…”

Synthesis and Evaluation of Antibacterial and Antifungal Activities of 1,3-Disubstituted-4-thioxoimidazolidin-2-one Derivatives

“…The aim of the present investigation is to synthesize series of imidazolidineiminothiones was bearing various substituent at N- (1) and others at N- (3). The antibacterial and antifungal activities of these derivatives were measured.…”

“…[2] Imidazolidineiminothione derivatives and their related heterocycles exhibit interesting pharmacological effects such as antibacterial, antifungal antiviral and antitumor agents. [3][4][5][6][7] Bacterial infection and fungal infection are among the widespread and serious diseases. To overcome these serious diseases, the discovery of new types of antimicrobial agents is a very important task.…”

Synthesis, Spectral Characterization and Pharmacological Evaluation of Novel Thiazole-Oxoindole Hybrid Compounds as Potential Anticancer Agents

“…Molecular hybridization is a valuable structure modification approach that comprises the incorporation of two or more pharmacophores into single entity. In view of the importance of thiazole and isatin derivatives and as part of our continued interest [28][29][30][31] in developing new active therapeutic agent (hybrid drug). We herein report the synthesis of novel thiazole based isatin sulphonamide.…”