Boosting the antimicrobial performance based on new fused spirothiazolidine framework analogs

Abstract

New spiro[cyclohexane-1,2'-thiazolo[4,5-b]pyridine derivatives (3–23) were investigated. Then there is in vitro antimicrobial potency against possible organisms Staphylococcus aurous ATCC-47,077, Bacillus cereus ATCC-12228, Escherichia coli ATCC-25922, Salmonella typhiATCC-15566, and Candida albicans ATCC-10231 were tested utilizing commercially available antibiotics ampicillin as a reference drug. A preliminary antimicrobial test represented that derivatives: (Aldoses) 3'-(4-fluorophenyl)-5'-(methyleneamino)-7'-(p-tolyl)-3'H-spiro[cyclohexane-1,2'-thiazolo[4,5-b]pyridine]-6'-carbonitrile (16–19) and (Acetyl aldoses) 3'-(4-fluorophenyl)-5'-(methyleneamino)-7'-(p-tolyl)-3'H-spiro [cyclohexane-1,2'-thiazolo[4,5-b]pyridine]-6'-carbonitrile (20–23) exhibited higher antifungal, and antibacterial performance with minimum inhibitory concentrations values of (39–67 µg/ml) toward all pathogenic strains compared to common reference drug ampicillin.

Synthesis of Functionalized 2′,5‐Oxo‐spiro[furan‐2,3′‐indoline]‐3‐carboxylate Derivatives as Antiproliferative Agents: ADMET Studies, and Molecular Docking against P2Y12 Inhibitors

“…Briefly, the MW of all the synthesized spirooxindole‐oxofuran was less than 500 Daltons, whereas the number of HBDs and HBAs for 4 a – d was recorded at the desirable thresholds of less than 5 and 10, respectively. The numbers of rotatable bonds were also found to be 4 or 5 for 4 a – d falling within the permissible threshold of less than 5 [12,13] …”

“…The numbers of rotatable bonds were also found to be 4 or 5 for 4 a-d falling within the permissible threshold of less than 5. [12,13] Considering the potential of hydrophilicity in drug distribution pattern, analysis of Log P has widely been used to assess the permeability of a drug candidate, whereas, the TPSA is used as the measure of the polarity and trans-membrane transport of compounds. [14,15] Our results showed that all the synthesized spirooxindole-oxofuran ( 4 a-d These values for the TPSA for all the newly synthesized spirooxindole-oxofuran (4 a-d) were similar to that reported in the previously published reports.These properties signify the fact that the newly synthesized spirooxindole-oxofuran qualify Scheme 1.…”

Antibacterial and Anticandidal Activity of the Nanostructural Composite of a Spirothiazolidine-Derivative Assembled on Silver Nanoparticles

“…It can be seen from the results in Table 1 and Table 2 and Figure 4 that the biological activity of P16 toward most bacteria and candida strains was high. This may be related to the fused pyridine ring with spirothiazolidine in the chemical structure of P16 , which this likely played an important role in enhancing the biological activity [ 37 ]. Moreover, nucleophilic groups (NH 2 , CN) and the presence of electron-donating groups (CH 3 , hexadecyl) likely also resulted in the high degree of biological activity of P16 [ 37 ].…”

“…This may be related to the fused pyridine ring with spirothiazolidine in the chemical structure of P16 , which this likely played an important role in enhancing the biological activity [ 37 ]. Moreover, nucleophilic groups (NH 2 , CN) and the presence of electron-donating groups (CH 3 , hexadecyl) likely also resulted in the high degree of biological activity of P16 [ 37 ]. These results indicate that P16 favored the dispersion of AgNPs and improved their biocompatibility.…”

“…Simple spirothiazolidines have been shown to inhibit metalloprotease, giving rise to their use in the management of malaria infections [ 28 ]. Derivatives of spirothiazolidine have also been shown to have good antioxidant [ 29 ], anticancer [ 30 ], antihyperglycemic, antidiabetic [ 31 ], anti-inflammatory [ 32 , 33 ], anticonvulsant [ 34 , 35 , 36 ], and antimicrobial activities [ 37 ]. In this respect, nanomaterials have been receiving increased attention in recent years.…”