Emerging impact of triazoles as anti-tubercular agent

Sharma, Anindra; Agrahari, Anand K.; Rajkhowa, Sanchayita; Tiwari, Vinod K.

doi:10.1016/j.ejmech.2022.114454

Cited by 45 publications

(16 citation statements)

References 257 publications

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“…Although synthetically derived those compounds containing 1,2,3-triazole group have various biological activities such as anticancer [41][42][43][44] , antibacterial [45,46] , antifungal [47,48] , anti-HIV [49,50] , antituberculosis [51,52] , antioxidant [53,54] , antiproliferative [55,56] and enzyme inhibitory [57,58] , these compounds are not found in nature. Therefore, the importance of these compounds in medicinal chemistry field has become undeniable, and so 1,2,3-triazole groups have been described as a "pharmacophore group" with the meaning of the main functional group responsible for the effect of a drug compound and the synthesis of the related compound has been carried out by many scientists after that time [59] .…”

Section: Design Synthesis Properties and Applications Of 123-triazolesmentioning

confidence: 99%

Click chemistry: A fascinating, Nobel-winning method for the improvement of biological activity

Halay

Açıkbaş

2023

ACE

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Click chemistry is totally an approach consisting of efficient and reliable reactions that bind two molecular building blocks and require no complex purification techniques. The aspire of achieving molecules with the desired characteristics and behaviour is the key to the click chemistry concept. In this concept, in order to obtain 1,2,3-triazole products as diversely functionalized molecules, copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction has been widely used for years in the field of materials science, organic synthesis and the biochemistry. This review focusses on the importance of click chemistry for obtaining biologically active triazole molecules and therefore the applications of such 1,2,3-triazole derivatives in medicinal chemistry field are highlighted.

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Section: Design Synthesis Properties and Applications Of 123-triazolesmentioning

confidence: 99%

Click chemistry: A fascinating, Nobel-winning method for the improvement of biological activity

Halay

Açıkbaş

2023

ACE

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“…1,2,3‐Triazoles have also been reported to be active as antidiabetic, antibacterial, anti‐HIV, anticancer, antifungal, antitubercular, antileishmanial, kinase inhibitor, and so on. [ 36–41 ]…”

Section: Introductionmentioning

confidence: 99%

Synthesis of 1,2,3‐triazole‐1,3,4‐thiadiazole hybrids as novel α‐glucosidase inhibitors by in situ azidation/click assembly

Kumar

Dhameja

Kurella

et al. 2023

Archiv der Pharmazie

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α-Glucosidase inhibition is widely used in the oral management of diabetes mellitus (DM), a disease characterized by high blood sugar levels (hyperglycemia) and abnormal carbohydrate metabolism. In this respect, a series of 1,2,3-triazole-1,3,4thiadiazole hybrids 7a-j were synthesized, inspired by a copper-catalyzed one-pot azidation/click assembly approach. All the synthesized hybrids were screened for inhibition of the α-glucosidase enzyme, displaying IC 50 values ranging from 63.35 ± 0.72 to 613.57 ± 1.98 μM, as compared to acarbose (reference) with IC 50 of 844.81 ± 0.53 μM. The hybrids 7h and 7e with 3-nitro and 4-methoxy substituents at the phenyl ring of the thiadiazole moiety were the best active hybrids of this series with IC 50 values of 63.35 ± 0.72 μM, and 67.61 ± 0.64 μM, respectively. Enzyme kinetics analysis of these compounds revealed a mixed mode of inhibition. Moreover, molecular docking studies were also performed to gain insights into the structure-activity-relationships of the potent compounds and their corresponding analogs.

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“…Furthermore, carbohydrate scaffolds due to their noteworthy features including as an integral part of the living cells, involvement in cellular interactions, chirality in nature, wide structural diversity, biocompatibility, bioavailability, superior ADME and pharmacokinetic parameter, improved water solubility, hydrophilicity, and moreover notable minimal toxicity encouraged them to be widely explored in drug discovery and development [7–9] . Also, the ‘CuAAC’ click chemistry‐mediated molecular hybridization approach is well utilized in recent years to develop novel, safe, more potent, and fast‐acting drug candidates to fight against a number of front‐line diseases [10–12] . Therefore, our experience on CuAAC ‘click’ chemistry in glycoscience [13] inspired us to develop 1,2,3‐triazolyl quinine conjugates as promising chemotherapeutic potential.…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and Docking Study of Quinine‐9‐Triazolyl Conjugates

Tiwari

Bose

Singh

et al. 2023

Chemistry & Biodiversity

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To develop a better chemotherapeutically potential candidate for lung cancer treatment and cure with repurposed motifs, quinine has been linked with biocompatible CuAAC‐inspired regioselective 1,2,3‐triazole linker and a series of ten novel 1,2,3‐triazolyl‐9‐quinine conjugates have been developed by utilizing click conjugation of glycosyl ether alkynes with 9‐epi‐9‐azido‐9‐deoxy‐quinine under standard click conditions. In parallel, the docking study indicated that the resulting conjugates have an overall appreciable interaction with ALK‐5 macromolecules. Moreover, the mannose‐triazolyl conjugate exhibited the highest binding interactions of −7.6 kcal/mol with H‐bond interaction with the targeted macromolecular system and indicate the hope for future trials for anti‐lung cancer candidates.

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Emerging impact of triazoles as anti-tubercular agent

Cited by 45 publications

References 257 publications

Click chemistry: A fascinating, Nobel-winning method for the improvement of biological activity

Click chemistry: A fascinating, Nobel-winning method for the improvement of biological activity

Synthesis of 1,2,3‐triazole‐1,3,4‐thiadiazole hybrids as novel α‐glucosidase inhibitors by in situ azidation/click assembly

Design, Synthesis, and Docking Study of Quinine‐9‐Triazolyl Conjugates

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