Synthesis, characterization and pharmacological evaluation of certain sulfonamide containing heterocyclic motifs

Design, Synthesis, Antimicrobial Evaluation and in Silico Studies of Eugenol‐Sulfonamide Hybrids

“…Numerous sulfonamide‐based compounds have been used to develop potent lead substances with better efficacy and less toxicity [11] . Indeed, bioactive molecules possessing the sulfonamide group have been reported to demonstrate potent properties such as antibacterial, [12] antifungal, [13] antiviral, [14] antiparasitic, [15] and anti‐inflammatory properties [16] amongst others. Pharmacological properties of eugenol have been extensively highlighted, especially involving its antibacterial and antifungal properties [17–22] .…”

Thiophene‐containing compounds with antimicrobial activity

“…In this series, sulfonamides 304 (X = O or S) (Figure 36) had broad antibacterial activity (they were approximately three times less potent than cefaclor against S. aureus , E. coli and P. aeruginosa ) and antifungal activity (they were approximately eleven times less potent than ketoconazole against A. niger and more than 25 times less potent than ketoconazole against C. albicans ), while the antimicrobial activity of the remaining three thiophenes in the series was poor. In the second report, [ 278 ] 1‐(benzazol‐2‐ylmethyl)‐substituted bis(sulfonamides) 305 (Figure 36) were prepared through the reaction of the 3,4‐bis(thiophenesulfonamide)‐substituted pyrrolidin‐1‐ylacetic acid with ring‐substituted ortho ‐phenylenediamines, 2‐aminophenols or 2‐aminothiophenols. Generally, compounds 305 having chloro, bromo or nitro as substituent R were more active than candidates with R = H, CH 3 or OCH 3 against all the microbial strains employed in the study, irrespective of the nature of the benzazole moiety.…”

“…In this series, sulfonamides 304 (X = O or S) (Figure 36) had broad antibacterial activity (they were approximately three times less potent than cefaclor against S. aureus, E. coli and P. aeruginosa) and antifungal activity (they were approximately eleven times less potent than ketoconazole against A. niger and more than 25 times less potent than ketoconazole against C. albicans), while the antimicrobial activity of the remaining three thiophenes in the series was poor. In the second report, [278] 1-(benzazol-2-ylmethyl)-substituted bis(sulfonamides) 305 Bis(sulfonamides) having a 2-phenylbenzoxazole core have been reported as antibacterial agents in a different paper. [279] Depending on the position of the 5-chlorothiophen-2-sulfonylamino pharmacophore (either as a benzoxazole substituent or as a phenyl substituent), two parallel series of unsymmetrical bis(sulfonamides) have been developed.…”

Acyl pyrazole sulfonamides as new antidiabetic agents: synthesis, glucosidase inhibition studies, and molecular docking analysis

“…Among the heterocyclic compounds that contain nitrogen and sulfur, sulfonamide derivatives with a pyrazole moiety hold a privileged position in organic chemistry ( Kołaczek et al, 2014 ; Khan et al, 2016 ; Dhameja and Gupta, 2019 ; Faisal et al, 2019 ). They not only act as anticonvulsants ( Abdul-Gafoor, 2016 ; Abdelgawad et al, 2018 ; Mishra et al, 2018 ), anti-stress and anxiogenics ( Channar et al, 2018 ; Saha and Pal, 2020 ), antitumor ( Channar et al, 2018 ), antiviral ( Badampudi et al, 2014 ; Kołaczek et al, 2014 ; Kumar et al, 2015 ; Mustafa et al, 2022 ), antimicrobial, anticholinesterase ( Mumtaz et al, 2019 ; Ghosh et al, 2020 ; Verma et al, 2020), antiulcer ( Khan et al, 2018 ), and antimalarial ( Thillainayagam et al, 2020 ) but also exhibit a variety of enzyme inhibition properties ( Mumtaz et al, 2019 ; Bayrak, 2022 ; Chalkha et al, 2022 ; Mustafa et al, 2022 ). Additionally, some of the pyrazole-containing sulfonamide derivatives have been tested against α -glucosidase ( Shu et al, 2016 ; Azimi et al, 2021 ).…”