ChemInform Abstract: Synthesis and Biological Evaluation of Nimesulide Based New Class of Triazole Derivatives as Potential PDE4B Inhibitors Against Cancer Cells.

Mareddy, Jyoti; Nallapati, Suresh Babu; Anireddy, Jaya Shree; Devi, Yumnam Priyadarshini; Mangamoori, Lakshmi Narasu; Kapavarapu, Ravikumar; Pal, Sarbani

doi:10.1002/chin.201420125

Cited by 4 publications

(3 citation statements)

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“…antitumoral [8,9] . anticancer [10][11][12] ,antityrosinase [13] , and antiinflammatory [14] activities. Notable drugs based on the 1,2,3-triazole scaffold include Rufinamide, an anticonvulsant, Cefatrizine, an antibiotic, and Tazobactam, an antifungal agent.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and antibacterial screening of some new 1'2'3 -triazole derivatives from dapsone

Hasan Mohammed Marhoon,

Ezzat Hussein Zimam

2024

J. K. Chem. Sci.

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In our relentless pursuit of developing innovative antibacterial derivatives, we have successfully generated and evaluated a novel series of 1,2,3-triazole derivatives derived from azo dapsone. The synthesis process commenced with the fusion of the dapsone core with the triazole framework, establishing a solid foundation for our synthetic endeavors. Subsequently, the azo dapsone nucleus underwent functionalization using sodium azide, resulting in the creation of an azide derivative (B). To synthesize the desired end 1,2,3-triazoles, a click reaction was employed, combining the azide compound with triple bond derivatives. The structures of all the synthesized compounds were meticulously characterized through the utilization of advanced techniques such as Nuclear Magnetic Resonance (NMR) and Infrared (IR) spectroscopy. Following the successful synthesis and characterization, our focus shifted to evaluating the in vitro antibacterial activity of these compounds against two significant bacterial strains: the gram-positive bacterium Staphylococcus aureus and the gram-negative bacterium Escherichia coli. Among the compounds synthesized, one compound in particular, designated as (H2), exhibited exceptional potency against Staphylococcus aureus with a minimal inhibitory concentration (MIC) of 25 μg/mL, surpassing the activity of all other prepared compounds. Similarly, compound (H1) displayed remarkable efficacy against Escherichia coli with an MIC of 22 μg/mL, outperforming the other end compounds. These findings demonstrate the tremendous potential of our synthetic approach in generating dapsone derivatives with enhanced antibacterial activity. Our research represents a significant step forward in the development of novel and potent antibacterial agents.

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Section: Introductionmentioning

confidence: 99%

Synthesis and antibacterial screening of some new 1'2'3 -triazole derivatives from dapsone

Hasan Mohammed Marhoon,

Ezzat Hussein Zimam

2024

J. K. Chem. Sci.

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“…[4][5][6][7] 1,2,3-Triazole systems the ability of hydrogen bond formation, dipoledipole and π stacking interactions, stable to reduction and oxidation. 8 1,2,3-triazoles are present in many of the drugs like theTazobactum,Carboxyamidotriazole and Ru namide etc.The triazoles arereported to have the anticancer 9,10 , antitubercular 11 , antifungal 12,13 antibacterial 14,15 , antiviral 16,17 and antiobesity 18,19 and anti-diabetic 20 properties.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, in-silico based virtual screening,anti-cancer potential of novel1,2,3-triazole-thiadiazole hybrid derivatives as Aurora kinase A (ARK-A) and Extracellular regulated kinase 2 (ERK2) dual inhibitors

Bontha,

Edigi,

Dokala

et al. 2023

Med Chem Res

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As part of our ongoing efforts to produce promising cytotoxic agents, the novel compounds, 5-(4-(diethylamino)-2-((1-substitutedphenyl-1H-1,2,3-triazol-4-yl)methoxy)phenyl)-1,3,4-thiadiazol-2yl)pyrrolidine-2,5-dione derivatives (9a-l) were developed, synthesised, and characterized using several analytical techniques, including 1 H NMR, 13 C NMR, and LC-MS. New series of 1,2,3-triazole and thiadiazole molecular hybrids synthsized were evaluated for their anticancer activity against human oesophageal carcinoma cell line KYSE-450 and human pancreatic carcinoma cell line MIA PaCa-2 cells. The compounds 9b, 9i, 9j, and 9l exhibited potential cytotoxic activity against KYSE-450 and MIAPaCa-2 cells, according to cytotoxic evaluation data. Compound 9j had greater anti-cancer potential relative to the standard employed across all compounds evaluated. The remaining compounds exhibited moderate to weak anti-proliferative potential. In-vitro kinase inhibition of compound 9j was signi cantly more effective against both ARK-1 and ERK-2 enzymes, indicating its dual inhibition potential. Docking analysis culminated that 9k, 9j, and 9i have substantial docking scores with the ARK-1 receptor, indicating the presence of strong binding a nities. Signi cant binding interactions between molecules 9j and 9h and the ERK-2 receptor suggest an inhibitory effect. Hence the compounds are promising dual inhibitors of ARK-A/ERK2.

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“…have reported a series of fluconazole‐based mimics accommodate 1,3,4‐oxadiazole and 1,2,3‐triazole moieties and showed that the analogues exhibited significant antifungal activity with MIC 80 ≤ 0.125 μg/mL [27a]. Recently, we have synthesized 1,2,3‐triazole‐etodolac hybrids, etodolac‐pyridazones, and 1,2,3‐triazole‐nimesulides and investigated as anticancer agents .…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Biological Evaluation of New Ibuprofen‐1,3,4‐oxadiazole‐1,2,3‐triazole Hybrids

Rayam

Polkam

Kummari

et al. 2018

Journal of Heterocyclic Chem

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A new hybrid polydentate template comprising distinctive pharmacophoric groups, namely, ibuprofen, 1,3,4‐oxadiazole, and 1,2,3‐triazole linked through a thioether bridge was achieved by one‐pot synthesis by exploring multicomponent Cu‐catalyzed “click chemistry” approach. The target structures were characterized by NMR, IR, and LC‐Mass. The X‐ray analysis of 2‐(1‐(4‐isobutylphenyl)ethyl)‐5‐(((1‐(3‐nitrophenyl)‐1H‐1,2,3‐triazol‐4‐yl)methyl)thio)‐1,3,4‐oxadiazole (8a) confirmed the assigned structure. The in vitro antibacterial and anticancer activity of these compounds revealed that 2‐(1‐(4‐isobutylphenyl)ethyl)‐5‐(((1‐phenyl‐1H‐1,2,3‐triazol‐4‐yl)methyl)thio)‐1,3,4‐oxadiazole (8b) demonstrated more potent antibacterial activity against Gram‐negative strains (Escherichia coli and Pseudomonas aeruginosa) and 2‐(((1‐(2,4‐dimethylphenyl)‐1H‐1,2,3‐triazol‐4‐yl)methyl)thio)‐5‐(1‐(4 isobutylphenyl)ethyl)‐1,3,4‐oxadiazole (8e) exhibited anticancer activity with IC50 of 27.50 and 31.03 μg/mL against HeLa and MCF‐7 cell lines, respectively.

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ChemInform Abstract: Synthesis and Biological Evaluation of Nimesulide Based New Class of Triazole Derivatives as Potential PDE4B Inhibitors Against Cancer Cells.

Cited by 4 publications

References 1 publication

Synthesis and antibacterial screening of some new 1'2'3 -triazole derivatives from dapsone

Synthesis and antibacterial screening of some new 1'2'3 -triazole derivatives from dapsone

Synthesis, in-silico based virtual screening,anti-cancer potential of novel1,2,3-triazole-thiadiazole hybrid derivatives as Aurora kinase A (ARK-A) and Extracellular regulated kinase 2 (ERK2) dual inhibitors

Synthesis and Biological Evaluation of New Ibuprofen‐1,3,4‐oxadiazole‐1,2,3‐triazole Hybrids

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