Synthesis and Antimicrobial Evaluation of (1‐(2‐(Benzyloxy)‐2‐oxoethyl)‐1<i>H</i>‐1,2,3‐triazol‐4‐yl)methyl Benzoate Analogues

Kaushik, C. P.; Pahwa, Ashima; Kumar, Devinder; Kumar, Ashwani; Singh, Dalbir; Kumar, Krishan; Luxmi, Raj

doi:10.1002/jhet.3209

Cited by 14 publications

(14 citation statements)

References 31 publications

(27 reference statements)

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“…Dataset: All the synthesized triazoles (1a-1t) with antimicrobial activities reported previously [26] were considered for present QSAR study. The dataset was split into training (20 compounds) and test (05 compounds) sets in a random manner.…”

Section: Methodsmentioning

confidence: 99%

“…The resulted QSAR models were evaluated using different parameters suggested in literature [29]. [26]. Norfloxacin and fluconazole were used as reference drugs for antibacterial and antifungal strains, respectively.…”

Section: Methodsmentioning

confidence: 99%

“…It helps to envisage the biological spectrum of newly designed compounds from structural and electronic parameters, contributing for the drug discovery processes. Encouraged from above considerations, for the development of effective microbicidal substituted 1,2,3-triazoles [23][24][25], herein, we describe the QSAR studies of 20 ester linked 1,4-disubstituted 1,2,3-triazoles (1a-1t) possessing antimicrobial activities reported earlier [26].…”

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confidence: 99%

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QSAR Studies on Microbicidal Activity of Disubstituted 1,2,3-Triazoles having Ester Linkages

Kaushik¹,

Pahwa²,

Kumar³

et al. 2018

Asian J. Chem.

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Over the past few years, continuous emergence of resistance in microorganisms along with side effects towards existing antimicrobials has become major health concern for the community. Various types of infections are increasing day by day due to these multidrug resistant bacteria and fungi. Owing to this, design and development of new structural leads has become major challenge for medicinal researchers. This justifies the attempt for synthesis of new, effective and safer antibacterial and antifungal agents with novel mode of action to combat newer microbial infections [1,2]. Triazoles correspond to class of bioactive heterocycles and have been recognized as key structural entity in several molecules of pharmaceutical importance [3]. These scaffolds reflected their role as antibacterial [4,5], antifungal [6], anti-HIV [7], anticancer [8,9], antitubercular [10,11], anticonvulsant [12], antiallergic [13], antioxidant [14], antiviral [15], antimalarial [16] agents etc., in the field of medicinal chemistry. Inspite of the pharmaceutical applications, these triazole derivatives also found to possess industrial importance as optical brighteners, dyestuffs, photostabilizers, agrochemicals and corrosion inhibitors [17,18]. In the past, various synthetic approaches have been developed for the synthesis of 1,2,3triazoles, however, Cu(I) catalyzed cycloaddition between

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Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

mentioning

confidence: 99%

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QSAR Studies on Microbicidal Activity of Disubstituted 1,2,3-Triazoles having Ester Linkages

Kaushik¹,

Pahwa²,

Kumar³

et al. 2018

Asian J. Chem.

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“…Among the analogs, 37 with electronegative nitro group substitution at para position next to ester nucleus with MIC value of 0.0142 μmol/mL showed the best antifungal activity, whereas electropositive substitution of methyl at para position resulted in decreased activity. [65] At the same pace, Kaushik et al synthesised 1,4-disubstituted-1,2,3triazole analogs comprising thioether and ester linkages and evaluated for their antifungal activity against Candida albicans. Among all the derivatives, 38 was most active with MIC value of 0.0138 μmol/mL.…”

Section: 23-triazole Derivatives Containing Ester Linkagementioning

confidence: 99%

1,2,3‐Triazole Derivatives as an Emerging Scaffold for Antifungal Drug Development against Candida albicans: A Comprehensive Review

Singh

Sharma

et al. 2023

Chemistry & Biodiversity

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Candida infections are most prominent among fungal infections majorly target immunocompromised and hospitalized patients and cause significant morbidity and mortality. Candida albicans is the notorious and most prevalent among all pathogenic Candida strains. Its emerging resistance toward available antifungal agents making it hard to tackle and emerging as global healthcare emergency. Simultaneously, 1,2,3-triazole nucleus is a privileged scaffold that is gaining importance in antifungal drug development due to being a prominent bioactive linker and isostere of triazole based antifungal class core 1,2,4-triazole. Numerous reports have been updated in scientific literature in last few decades related to utilization of 1,2,3-triazole nucleus in antifungal drug development against Candida albicans. Present review will shed light on various preclinical studies focused on development of 1,2,3-triazole derivatives targeting Candida albicans along with brief highlight on clinical trials and newly approved drugs. Structure-activity relationship has been precisely discussed for each architect along with future perspective that will help medicinal chemists in design and development of potent antifungal agents for tackling infections derived from Candida albicans.

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“…1,2,3‐Triazoles, a class of five‐membered nitrogen heterocyclic compound present in a variety of biologically active molecules (Figure 1). 1,4‐Disubstituted 1,2,3‐triazoles have naturally endowed with a great number of biological activities such as antiviral, [ 14 ] antimicrobial, [ 15–19 ] antimalarial, [ 20 ] antitubercular, [ 21 ] antidiabetic, [ 22 ] anti‐allergic, [ 23 ] anti‐HIV, [ 24,25 ] and so forth. Moreover, a significant number of 1,2,3‐triazoles have also been reported with exceptional anticancer activities.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of chalcone precursor via Cu(I) catalyzed 1,3‐dipolar reaction of functionalized acetylene and pyrazole embedded dipole

Manju

Kalluraya

Asma

et al. 2020

Journal of Heterocyclic Chem

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A new class of functionalized pyrazole bearing 1,2,3-triazole has been synthesized via Cu(I) mediated 1,3-dipolar cycloaddition of pyrazole bearing azide with various aromatic/heteroaromatic bearing terminal dipolarophile (acetylene). Structures of the newly synthesized compounds were explicated by analytical and spectral analysis. All the newly synthesized compounds were evaluated for their in-vitro antibacterial and antioxidant activity. Among the synthesized compound, triazole bearing 2,5-thiazolidinone 5b (20 ± 0.70) and triazole bearing thiocarboamide 5e (19 ± 0.70) showed good antibacterial activity against Escherichia coli and Pseudomonas aeruginosa, respectively. The newly synthesized compounds further tested for their ability to bleach DPPH radical using DPPH scavenging assay. Among the synthesized compounds 1,2,3-triazole bearing 2,5-thiazolidinone 5b (58.81%) exhibited good DPPH scavenging activity compared to the rest of the compounds. From the X-ray and Hirshfield analysis, it was observed that compound 3, crystallizes in a triclinic crystal system with a P-1 space group. The major intercontacts present in these molecules are H…H (39.7%), C…H (23.9%), N…H (20.3%).

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Synthesis and Antimicrobial Evaluation of (1‐(2‐(Benzyloxy)‐2‐oxoethyl)‐1H‐1,2,3‐triazol‐4‐yl)methyl Benzoate Analogues

Cited by 14 publications

References 31 publications

QSAR Studies on Microbicidal Activity of Disubstituted 1,2,3-Triazoles having Ester Linkages

QSAR Studies on Microbicidal Activity of Disubstituted 1,2,3-Triazoles having Ester Linkages

1,2,3‐Triazole Derivatives as an Emerging Scaffold for Antifungal Drug Development against Candida albicans: A Comprehensive Review

Synthesis of chalcone precursor via Cu(I) catalyzed 1,3‐dipolar reaction of functionalized acetylene and pyrazole embedded dipole

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