In vitro microbiological evaluation of novel bis pyrazolones

a b s t r a c tThe pyrazolone structural motif is a critical element of drugs aimed at different biological end-points. Medicinal chemistry researches have synthesized drug-like pyrazolone candidates with several medicinal features including antimicrobial, antitumor, CNS (central nervous system) effect, anti-inflammatory activities and so on. Meanwhile, SAR (Structure-Activity Relationship) investigations have drawn attentions among medicinal chemists, along with a plenty of analogues have been derived for multiple targets. In this review, we comprehensively summarize the biological activity and SAR for pyrazolone analogues, wishing to give an overall retrospect and prospect on the pyrazolone derivatives.

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“…Narayana Rao et al [25] designed and synthesized several pyrazolone analogues 25, 26, 27 and 28 ( Fig. 3) with favorable activity ( Table 1).…”

Section: Pyrazolones As Antimicrobial Agents and Their Sarmentioning

confidence: 99%

Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect

Zhao

Dai

et al. 2020

European Journal of Medicinal Chemistry

139

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“…Pyrazolone derivatives express different pharmacological activities like antimicrobial (Akondi et al, 2016;Parmar et al, 2015), antitumor (Gouda et al, 2016, anti-inflammatory and analgesic (Mariappan et al, 2011), antifungal (Narayana Rao et al, 2014), anti-mycobacterial (Ahsan et al, 2012), anti-cholinergic and monoamnine oxidase inhibitors (Tok et al, 2019), antioxidants (Sivakumar et al, 2014), and antidiabetic (Yousuf et al, 2018). They are also used as ligands (Akcha et al, 2018) in complexes with catalytic activity.…”

Section: Pyrazolones As An Anticancer Agentmentioning

confidence: 99%

Pyrazolones as a potential anticancer scaffold: Recent trends and future perspectives

Suman¹,

Singh²,

Sandeep³

2021

J Appl Pharm Sci

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Cancers are already placing an enormous load on the worldwide healthcare practice; so, anti-neoplastic compounds nowadays are most essential in cancer remedy. Nevertheless, the expanding resistance in drug profiles' appearance in recently available anticancer drugs has so far risen to a distressing level over past decades. Pyrazolone holds wideranging chemotherapeutic characteristics, including anticancer activity, and they inhabit a significant place in the novel drug development process. As per the literature, various hybridized pyrazolone moieties with different pharmacophores and pyrazolone metal complexes have anticancer activities with good potency. In recent years, pyrazolone hybrids and metal complexes were generated to study their anticancer properties. Out of these, some derivatives displayed promising strengths against the case of resistant and susceptible cell lines of cancer. This current review encloses the latest advances of pyrazolone hybrids including thiophene, aminomethylidenes , naphthoquinones, combretastatins, 2-substituted-4-(2-fluorophenoxy) pyridine, hydroxybenzo[a]phenazine, coumarin, dihydrobenzoxepine, cyclic peptide, cambinol derivatives of pyrazolone, and different metal complexes as a potential anticancer agent.

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“…Among these applications, pyrazolones have been extensively studied for their medicinal properties. For example, pyrazolone has been used as an antimicrobial [2], antitumor [3], anti-in ammatory and analgesic [4], anti-fungal [5], anti-mycobacterial [6], anti-cholinergic monoamine oxidase inhibitors [7],…”

Section: Introductionmentioning

confidence: 99%

Facile one-pot synthesis of hydroxylated 1,3-dithiane-pyrazolone hybrids

Rabiei,

Nasiri

2024

Res Chem Intermed

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This study presents an effective one-pot strategy for the synthesis of hydroxylated 1,3-dithianepyrazolone hybrids. The process involves a reaction between pyrazolone derivatives and carbon disul de in the presence of epichlorohydrin (ECH). The structural elucidation of the products was accomplished using various spectroscopic techniques. To further corroborate the proposed reaction mechanism, enantiomerically pure ECH was utilized.

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In vitro microbiological evaluation of novel bis pyrazolones

Cited by 7 publications

References 10 publications

Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect

Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect

Pyrazolones as a potential anticancer scaffold: Recent trends and future perspectives

Facile one-pot synthesis of hydroxylated 1,3-dithiane-pyrazolone hybrids

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