Synthesis, antimicrobial activity and in-silico docking of two macrocycles based on pyrazole-tetrazole subunit

Cherfi, Mounir; Harit, Tarik; Idrissi-Yahyaoui, Meryem; Riahi, Abdelkhalek; Asehraou, Abdeslam; Malek, Fouad

doi:10.1016/j.molstruc.2022.132947

Cited by 13 publications

(3 citation statements)

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“…IR analysis was carried out on Shimadzu FTIR 8400s spectrophotometer. Compounds 1 , 4 , 5 [18] and 6 [29] were synthesized using methods reported in our previous works.…”

Section: Methodsmentioning

confidence: 99%

“…In fact, the tetrazolic carbon atom is shifted around 151 and 162 ppm for N1 and N2 isomers, respectively. [18,29] The structure of all new compounds was verifed by spectroscopic and spectrometric methods such NMR, FTIR, mass spectrometry and elemental analysis.…”

Section: Chemistrymentioning

confidence: 99%

“…[11] On the other hand, the design and conception of new families of N-heterocyclic derivatives could be another approach. In fact, they earned a great interest in medicinal chemistry field due to their high antitumor, [12][13][14] antimicrobial, [15][16][17][18][19] antiviral [20,21] and enzyme inhibitors [22][23][24] activities. Furthermore, the hybridization of several N-heterocycles on one skeleton has also been reported to reach several classes of compounds with high biological activities.…”

Section: Introductionmentioning

confidence: 99%

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Hybrid Pyrazole‐Tetrazole Derivatives with High α‐Amylase Inhibition Activity: Synthesis, Biological Evaluation and Docking Study

et al. 2022

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The elaboration of some N‐alkylated pyrazole‐tetrazole derivatives is reported. The structures of the newly ones are verified using NMR and FTIR spectroscopies, mass spectrometry as well as elemental analysis. Their potencies to inhibit the α‐amylase enzyme were evaluated using spectrophotometric method and the obtained results showed that some of them were extremely potent with respect to the used positive control. The structure activity relationship showed that the α‐amylase inhibition activity depends on the alkylation position as well as the nature of the alkyl moiety and the alkylation at the N1 position with a donor group improves the α‐amylase inhibition activity. Docking study was also performed and the obtained results support the experimental results in the case of the alkylation position effect. These findings suggest that the molecules reported in this study may be used as good drug candidate to treat Type 2 diabetes.

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“…IR analysis was carried out on Shimadzu FTIR 8400s spectrophotometer. Compounds 1 , 4 , 5 [18] and 6 [29] were synthesized using methods reported in our previous works.…”

Section: Methodsmentioning

confidence: 99%

Section: Chemistrymentioning

confidence: 99%