Pharmacological significance of triazole scaffold

Kharb, Rajeev; Sharma, Prabodh Chander; Yar, Mohammad Shahar

doi:10.3109/14756360903524304

Cited by 469 publications

(254 citation statements)

References 151 publications

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“…Oxazolidinones that contain a benzodioxin moiety (50) were synthesized by Ebner s group and their antimicrobial activity was tested. [115] The MIC against S. aureus was determined to be 2-3 mg mL À1 for one of the compounds.…”

Section: Antifungal and Antibacterialsmentioning

confidence: 99%

“…[118] Type and position of the cationic moieties as well as nature of the aromatic substituents, influenced the in vitro antiprotozoal activities of these compounds against Trypanosoma brucei rhodesiense, Plasmodium falciparum, and Leishmania donovani, and their cytotoxicity for mammalian cells. A few congeners displayed antitrypanosomal IC 50 values below 10 nm. Most of the dications were more potent against P. falciparum than pentamidine (IC 50 = 58 nm), and some analogues were more active than artemisinin (IC 50 = 6 nm).…”

Section: Antifungal and Antibacterialsmentioning

confidence: 99%

“…[159] The most promising compound displayed an IC 50 for cytotoxicity in vitro of (3.8 AE 0.3) nm and an IC 50 for nicotinamide adenine dinucleotide (NAD) depletion of (3.0 AE 0.4) nm.…”

Section: Antifungal and Antibacterialsmentioning

confidence: 99%

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Click Chemistry: 1,2,3‐Triazoles as Pharmacophores

Agalave

Maujan

Pore

2011

Chemistry An Asian Journal

1,149

508

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The copper(I)-catalyzed 1,2,3-triazole-forming reaction between azides and terminal alkynes has become the gold standard of click chemistry due to its reliability, specificity, and biocompatibility. Applications of click chemistry are increasingly found in all aspects of drug discovery; they range from lead finding through combinatorial chemistry and target-templated in vitro chemistry, to proteomics and DNA research by using bioconjugation reactions. The triazole products are more than just passive linkers; they readily associate with biological targets, through hydrogen-bonding and dipole interactions. The present review will focus mainly on the recent literature for applications of this reaction in the field of medicinal chemistry, in particular on use of the 1,2,3-triazole moiety as pharmacophore.

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Section: Antifungal and Antibacterialsmentioning

confidence: 99%

Section: Antifungal and Antibacterialsmentioning

confidence: 99%

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Click Chemistry: 1,2,3‐Triazoles as Pharmacophores

Agalave

Maujan

Pore

2011

Chemistry An Asian Journal

1,149

508

View full text Add to dashboard Cite

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“…Triazole ring derivatization lies on the 'bioisosterism phenomenon' in which oxygen of oxadiazole nucleus is replaced with the nitrogen of triazole analogue 27 . Triazole derivatives are the therapeutically fascinating drug candidates including antifungal 28 , antioxidant 29 , antibacterial 30 , insecticidal 31 , anti-inflammatory 15 , antineoplastic 32 , antiviral 33 , sedatives 34 , anticonvulsant 35,36 , anti-histaminic 27,32 , antitumor 37 , and CNS stimulants 38 etc.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antioxidant Evaluation of Novel Phenothiazine Linked Substitutedbenzylideneamino-1,2,4-Triazole Derivatives

Maddila

Momin

Gorle

et al. 2015

J. Chil. Chem. Soc.

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A series of novel 5-((10H-phenothiazin-10yl)methyl)-4-(substitutedbenzylideneamino)-4H-1,2,4-triazole-3-thiol derivatives (6a-i) have been synthesized from compound (1) through a multi-step reaction. The key intermediate (5) afforded a series of title compounds (6a-i) on condensation with various suitable aldehydes in the presence of H 2 SO 4 . The structures of novel compounds were characterized based on their elemental analysis, IR, 1 H-NMR, 13 C-NMR and MS spectral data. All these novel compounds were screened for their in vitro antioxidant activity by employing nitric oxide, hydrogen peroxide, and DPPH radical scavenging assays. The compounds 6d, 6e and 6i demonstrated potent antioxidant activity as these contain the electron-releasing groups.

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“…antidepressant, anti inflammatory, anti oxidant anti convulsant and anticancer [6][7][8]. Furthermore, Schiff base derivatives of [1, 2,4] triazoles have been identified having diverse pharmacological properties, like antifungal, antimicrobial, anticancer, antioxidant, anticonvulsant and anti-tubercular activities [9][10][11][12].…”

mentioning

confidence: 99%

Triazole substituted phthalocyanines and their electrochemical properties

Bayrak

2017

Hittite J. Sci. Eng.

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P hthalocyanines (Pcs) can be used many different applications such as gas sensors, electrochromic devices, photovoltaic cells and photodynamic therapy (PDT), due to their 18-π planar conjugate electron system [1][2][3][4]. Therefore synthesizing Pcs having different groups play a vital role in promoting these high technologies.These macrocyclic compounds are ideal building blocks for applications when they are modified with groups in the desired properties. For this reason, substitution of Pcs either on peripheral/nonperipheral or axial positions has vital importance for their utilizations. Furthermore, the solubility of Pc derivatives plays a critical role in order to use in all those applications. Phthalocyanines that unsubstituted are not soluble in common organic solvents due to the aggregation. These compounds can be made soluble in organic solvents by integration of substituents in the periphery/non-periphery of Pc core, thus increasing their electrochemical and catalysis applications. [5]. 1,2,4-Triazole derivatives are one of the key organic compound class have an important functions in biological applications. It's known that some of 1,2,4-triazoles exhibit biological trenchancy e.g. antifungal, anti microbial, anti viral, anti tubercular,

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Pharmacological significance of triazole scaffold

Cited by 469 publications

References 151 publications

Click Chemistry: 1,2,3‐Triazoles as Pharmacophores

Click Chemistry: 1,2,3‐Triazoles as Pharmacophores

Synthesis and Antioxidant Evaluation of Novel Phenothiazine Linked Substitutedbenzylideneamino-1,2,4-Triazole Derivatives

Triazole substituted phthalocyanines and their electrochemical properties

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