Straightforward synthesis of a novel ring-fused pyrazole-lactam and in vitro cytotoxic activity on cancer cell lines

Bertuzzi, Giulio; Locatelli, Erica; Colecchia, David; Calandro, Pierpaolo; Bonini, Bianca F.; Chandanshive, Jay Zumbar; Mazzanti, Andrea; Zani, Paolo; Chiariello, Mario; Franchini, Mauro Comes

doi:10.1016/j.ejmech.2016.04.006

Cited by 20 publications

(10 citation statements)

References 22 publications

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“…In fact, preparation method equally represents a pivotal role to discover the biologically active pyrazoles and their belongings. There are different synthetic approaches reported . All those showed their unique advantageous.…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis of tri‐substituted pyrazole derivatives as promising antimicrobial agents and investigation of structure activity relationships

Reddy

Garcia

Yuvaraja

et al. 2020

Journal of Heterocyclic Chem

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The major diseases spread in the environment only because of microbes. Even, intensive care units in the hospitals are polluted by microorganisms, particularly, Gram-positive bacteria. Although many antibiotics are existed, there is a need to develop up to date microbial-resistant agents. Hence, the current study aimed to develop prominent antimicrobial drug-related compounds. Thus, a novel series of tri-substituted analogs and their intermediates were synthesized. In addition, total new compounds were screened for their antimicrobial assay and identified as the most efficient biologically active compounds. Moreover, minimal inhibitory antimicrobial activity and appropriate structure activity relationships were investigated. From the results it was observed that, viability of Gram-positive bacteria was most powerfully affected by all active compounds. Finally, this research demonstrated that, these biologically energetic amalgams can be utilized for further preclinical studies with the ambition of standing unique inventive drugs.

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Section: Introductionmentioning

confidence: 99%

Design, synthesis of tri‐substituted pyrazole derivatives as promising antimicrobial agents and investigation of structure activity relationships

Reddy

Garcia

Yuvaraja

et al. 2020

Journal of Heterocyclic Chem

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“…Bertuzzi et al in 2016 reported the synthesis of novel pyrazole derivatives containing lactam moiety and screened them against 5 cancer cell lines (MCF-7, MD-MB-231, HN13, V87MG and HeLa). The IC50 values after 24 h (17.6 -78.3 µM) and 72 h (10.6 -33.5 µM) suggested that compound 7 (Figure 4) might be used as anti-proliferative agent [34]. The prenylation mechanism in cancer causing proteins e.g.…”

Section: Anticancer Activitymentioning

confidence: 99%

Pyrazole Bearing Molecules as Bioactive Scaffolds: A Review

Aziz

Zahoor

Ahmad

2020

J. Chil. Chem. Soc.

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Pyrazole being a heterocyclic motif has secured an eccentric status in the field of medicinal chemistry. Pyrazole and its derivatives have tremendous biological applications like anti-cancer, anti-microbial, antiviral, antifungal, anti-inflammatory, analgesic, insecticidal etc. In this review, some recent developments have been reported for the synthesis of biologically active pyrazole based molecules having biological potential such as anti-SIRT1 and SIRT2, anti-FAAH, anti-NOSs, as liver X receptor partial agonist, CB2 receptor ligand and glucagon receptor antagonists.

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“…In the past years, some azole derivatives were developed as new antimicrobial agents . Pyrazole have diverse biological activities including analgesic , anti‐inflammatory , and anticancer activity . There are a number of antimicrobial compounds containing a pyrazole ring in their structures such as pyrazofurin that are important antimicrobial drugs (Fig.…”

Section: Introductionmentioning

confidence: 99%

Ultrasound‐assisted Synthesis of Novel Pyrazole and Pyrimidine Derivatives as Antimicrobial Agents

Dofe

Sarkate

Shaikh³

et al. 2018

Journal of Heterocyclic Chem

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Herein, we report a convenient and facile methodology for the synthesis of new series of pyrazole and pyrimidine derivatives 2a–f and 3a–f under ultrasound irradiation. Pyrazole and pyrimidine derivatives have been synthesized in better yields and shorter reaction times compared with the conventional method. The chemical structures of all the synthesized compounds were elucidated by their IR, 1H NMR, 13C NMR, MS, and elemental analysis. Further, the target compounds were screened for their antimicrobial activity against four bacteria (Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa) and two fungi (Candida albicans, Aspergillus niger). In particular, compounds 2a, 2d, 2e, 3a, 3e, and 3f exhibited potent antimicrobial activity.

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Straightforward synthesis of a novel ring-fused pyrazole-lactam and in vitro cytotoxic activity on cancer cell lines

Cited by 20 publications

References 22 publications

Design, synthesis of tri‐substituted pyrazole derivatives as promising antimicrobial agents and investigation of structure activity relationships

Design, synthesis of tri‐substituted pyrazole derivatives as promising antimicrobial agents and investigation of structure activity relationships

Pyrazole Bearing Molecules as Bioactive Scaffolds: A Review

Ultrasound‐assisted Synthesis of Novel Pyrazole and Pyrimidine Derivatives as Antimicrobial Agents

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