Synthesis, antimycobacterial activity and docking study of 2-aroyl-[1]benzopyrano[4,3- c ]pyrazol-4(1 H )-one derivatives and related hydrazide-hydrazones

Angelova, Violina T.; Valcheva, Violeta; Pencheva, Tania; Voynikov, Yulian; Vassilev, Nikolay G.; Mihaylova, Rositsa; Momekov, Georgi; Shivachev, Boris

doi:10.1016/j.bmcl.2017.05.011

Cited by 33 publications

(15 citation statements)

References 41 publications

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“…A new 2-aroyl-[1]benzopyrano[4,3- c ]pyrazol-4(1 H )-one derivatives containing hydrazide-hydrazone analogues were prepared and tested in vitro for their anti-mycobacterial activity against reference strain M. tuberculosis H37Rv. Compound 378 demonstrated significant MIC value 0.32 µM, which was comparable to those of isoniazid [ 277 ]. A new bedaquiline derivatives containing a pyrazole moiety were identified by He et al and tested for their inhibitory activities against ATP synthesis inhibition in mycobacteria.…”

Section: Pharmacological Activitiesmentioning

confidence: 99%

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

et al. 2018

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Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antipsychotic CDPPB, the anti-obesity drug rimonabant, difenamizole, an analgesic, betazole, a H2-receptor agonist and the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. Owing to this diversity in the biological field, this nucleus has attracted the attention of many researchers to study its skeleton chemically and biologically. This review highlights the different synthesis methods and the pharmacological properties of pyrazole derivatives. Studies on the synthesis and biological activity of pyrazole derivatives developed by many scientists around the globe are reported.

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Section: Pharmacological Activitiesmentioning

confidence: 99%

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

et al. 2018

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“…Hydrazide–hydrazones are of great interest due to their antibacterial, antifungal, antitubercular, antiviral, analgesic, anticonvulsant, and larvicidal activities . Hydrazide–hydrazones are also potent inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and poly(ADP‐ribose) glycohydrolase .…”

Section: Introductionmentioning

confidence: 99%

New hydrazide–hydrazones of isonicotinic acid: synthesis, lipophilicity and in vitro antimicrobial screening

et al. 2018

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This study describes the synthesis, lipophilicity and in vitro antimicrobial assays of 15 new hydrazide-hydrazones of isonicotinic acid. New derivatives were obtained on the basis of the condensation reaction of isonicotinic acid hydrazide with different aromatic aldehydes. The chemical structure of synthesized compounds was confirmed by spectral methods. Experimental lipophilicity of new isonicotinic acid derivatives was determined using reversed-phase thin-layer chromatography. All synthesized compounds were subjected to in vitro antimicrobial assays against reference strains of Gram-positive bacteria, Gram-negative bacteria and fungi belonging to Candida spp. Some of the synthesized hydrazide-hydrazones proved to be significant antibacterial compounds and more potent than commonly used chemotherapeutic agents.

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“…In order to discover the potential mechanism of antimycobacterial activity of synthesized compounds, the authors performed molecular docking studies and investigated binding to the 2-trans-enoyl-ACP reductase (InhA) enzyme involved in M. tuberculosis cell wall biogenesis. On the basis of obtained results, the authors suggested that the activity of synthesized molecules may be connected with interactions with the inhibitor binding cavity of M. tuberculosis enoyl-ACP reductase and/or related to the ability of the tested compounds to penetrate mycobacterial cells [34]. Hydrazide-hydrazones synthesized and tested for potential antimycobacterial activity by Atta et al displayed high potency against M. tuberculosis H37Rv.…”

Section: Antimycobacterial Activitymentioning

confidence: 99%

Updated Information on Antimicrobial Activity of Hydrazide–Hydrazones

Popiołek

2021

IJMS

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Hydrazide–hydrazones possess a wide spectrum of bioactivity, including antibacterial, antitubercular, antifungal, anticancer, anti-inflammatory, anticonvulsant, antidepressant, antiviral, and antiprotozoal properties. This review is focused on the latest scientific reports regarding antibacterial, antimycobacterial, and antifungal activities of hydrazide–hydrazones published between 2017 and 2021. The molecules and their chemical structures presented in this article are the most active derivatives, with discussed activities having a hydrazide–hydrazone moiety as the main scaffold or as a side chain. Presented information constitute a concise summary, which may be used as a practical guide for further design of new molecules with antimicrobial activity.

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Synthesis, antimycobacterial activity and docking study of 2-aroyl-[1]benzopyrano[4,3- c ]pyrazol-4(1 H )-one derivatives and related hydrazide-hydrazones

Cited by 33 publications

References 41 publications

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

New hydrazide–hydrazones of isonicotinic acid: synthesis, lipophilicity and in vitro antimicrobial screening

Updated Information on Antimicrobial Activity of Hydrazide–Hydrazones

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