Synthesis and characterization of 4-((5-bromo-1H-pyrazolo [3,4-b]pyridin-3-yl)amino)-N-(substituted)benzenesulfonamide as Antibacterial, and Antioxidant Candidates

Abstract

A series of novel 5-Bromo-3-iodo-1H-pyrazolo [3,4-b]pyridine linked various sulfonamide derivatives 8a-8j poly functionalized were designed and synthesized in moderate to good yield. A starting with iodination of 5-with the reaction of various sulfonamide derivatives 7a-7j via copper catalyzed coupling reaction produced targeted compounds8a-8j. The isolated compounds were accepted by spectral and elemental analysis. The compounds 8a,8c,8d, and 8i were excellent active against Gram-positive and gram-negative bacterial strain compare to streptomycin standard drug. All synthesized compounds showed moderate to good antioxidant properties with used DPPH and Superoxide radical scavenging assay, Compounds 8c, 8g, and 8i exerted significant antioxidant scavenging activity for the DPPH radical.

Synthesis and characterization of 4(3-(4-Fluorophenyl)2-methyl-1-(4-(sulfonamidesubtituted)phenyl)-4-oxoazitidin-2-yl)-3-methyl-1-(p-tolyl)-1H-pyrazol-5(4H)One as Antibacterial, and Antioxidant Candidates

“…The in vitro agar well diffusion method was used also described in our previous research 5 . Plates of ager well are finished by sterile cork borer (6mm diameter) and inoculated with the bacteria (two Gram-negative MTCC No.8558 Enterobacter aerogens, Escherichia coli MTCC No.1610, and two Gram-positive Micrococcus luteus MTCC No.11948 and Bacillus cereus MTCC No.8558) investigated all solids compounds dissolved in DMSO (because not inhibition) and get a concentration 1000µg/ml was directly encumbered into well of agar plates which inoculated for 37 ºC for 24 hours.…”

“…In our previous reported study 5 , we have seen that in vitro free radical scavenging antioxidant activity of all the synthesized derivatives 5a-5r was investigated by 2,2'-diphenyl-1-picrylhydrazyl (DPPH) assay which was calculated by percentage (%) Inhibition As shown in below Table 2.…”

“…Also, other derivatives showed good to moderate inhibition. According to our preceding report studied 5 The compounds 5a-r examined for Superoxide anion scavenging activity were analyzed at different concentrations 0.00 µg/ml, 200 µg/ml, 400 µg/ml, and 600 µg/ml which were calculated for IC50 values mentioned in below Table 3. Compounds 5c, 5i, and 5o considered high scavenging activity.…”

“…[1][2] Sulfonamides a well-known distinct class of versatile groups has an intensively considered the first drugs used for protective and chemotherapeutic activity against numerous supplementary pharmacological activities, especially as Antibacterial and Antifungal, Cyclooxygenase-2(COX-2), Carbonic anhydrase inhibitors (CAIs), Anti-HIV, Antioxidant, type II diabetes, Anti-malarial, treating male erectile dysfunction, Antituberculosis, etc. 3,4,5,6,5,7,8,9,10 At Present-days a large number of Schiff bases known even as Imine or azomethines synthesized from groups of sulfonamides have received extensive attention as an excellent synthon for various fused ring transformations and examined as various biological action. 11,12,13 The function of the 2-Azetidinone (β-lactam) framework was recognized as a unique structural synthetic target nucleus and an important contribution in the pharmaceutical research world for the reason that of their most attractive antibacterial drugs globally marketing (above 65%).…”

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“…, Antimalarial [13], cysteine protease [14], hypoglycemic [15], influenza [16], Antioxidant [5], [17][18][19], anti tuberculosis [20][21][22], etc. Beside the azitidine, another small fused 4-membered 'N' containing heterocyclic ring having carbonyl group at second position therefore also known as βlactam and 2-azitidinone is one of the most potent pharmacophores showed famous drugs as cephalosporins, carbapenems, penicillin, monobactams, clavulanic acid, etc [23].…”