ChemInform Abstract: Synthesis, Structure and Cytostatic Activity of a Series of 2‐Substituted Perimidines.

Braña, Miguel F.; Garrido, María Concepción Domínguez; Rodríguez, M. L.; Morcillo, M. J.; Alvarez, Y.; Valladares, Y.; Klebe, G.

doi:10.1002/chin.199037215

Cited by 3 publications

(4 citation statements)

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“…Perimidine derivatives, which are key nitrogen-containing heterocycles, have a variety of biological and pharmacological actions, including antibacterial, antimicrobial, anticancer, and anti-inammatory characteristics. [97][98][99] Their high electron-donating properties make them useful intermediates in the synthesis of symmetrical squarylium dyes for NIR absorption. In addition, they serve as antioxidant stabilizers, photochromic chemicals, catalysts, ligand scaffolds, and supramolecular stoppers.…”

Section: Squaric Acid Catalyzed Reactionsmentioning

confidence: 99%

Advances in organocatalyzed synthesis of organic compounds

Zafar,

Iqbal,

Iram

et al. 2024

RSC Adv.

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Section: Squaric Acid Catalyzed Reactionsmentioning

confidence: 99%

Advances in organocatalyzed synthesis of organic compounds

Zafar,

Iqbal,

Iram

et al. 2024

RSC Adv.

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“…Those authors revealed the fused tricycle perimidine was the minimal structure condition for the intercalative biding with DNA and affected by the variation in side chain of chromophore. Braña et al demonstrated that the 2-subtitutes perimidines-induced cytotoxicity action through the presence of basic nitrogen bearing to methyl groups [12]. As new chemicals synthetized, it is worthwhile to be submitted to toxicity studies in order to optimize later the therapeutic doses for heal human diseases.…”

Section: Perimidin-2-yl)-6-mentioning

confidence: 99%

A New Heterocyclic 1H-perimidine synthesized 2-(2,3-dihydro-1H-périmidin-2yl-)-6-methoxyphenol: Evaluation of Acute Toxicity in Wistar Rat

Tiéba

N’Go

Daouda

et al. 2021

JPRI

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Background and Aim: The 1H-perimidne, as novel source carbene ligand, is well known for its anti-fungal, anti-microbial or anti-tumor activities. Here, we aimed to study the acute toxicity in Wistar rat of 2-(2,3-dihydro-1H-perimidin-2-yl)-6-methoxyphenol, a new heterocyclic 1H- perimidine synthetized in our laboratory. Materials and Methods: Five groups of males Wistar rats were intraperitoneally injected with 7 mg/kg, 40 mg/kg, 90 mg/kg, 130 mg/kg and 150 mg/kg dissolved in dimethyl sulfoxide (DMSO), and followed during 14 days. We noted any clinical signs of acute toxicity as body weight loss, salivation, tremor, convulsion among others, as well as food consumption and water intake level. Results: The DL50 of the new 2-(2,3-dihydro-1H-perimidin-2-yl)-6-methoxyphenol was estimated to 65 mg/kg. The No Observed Adverse Effect Level (NOAEL) dose was 7 mg/kg because it did not caused mortality, clinical signs of acute toxicity, and not affected feed and water intake behavior. However, significant abnormalities as inflammation and necrosis were observed at doses-effects dependent in liver, when compared to NOAEL dose and vehicle. Conclusion: The new heterocyclic 2-(2,3-dihydro-1H-perimidin-2-yl)-6-methoxyphenol is considered as high toxicity grade product. From NOAEL dose, subsequent biological, toxicological, pharmacological and neurobehavioral studies are needed before using for clinical trials.

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“…Brafial et al [124] described the synthesis, cytotoxic activity, and structure-activity relationship (SAR) of 2-substituted perimidines. Perimidines were synthesized from the reaction of NDA with different compounds like p-toluenesulphonate and cyanamide and substituted amines.…”

Section: Biologic Applicationsmentioning

confidence: 99%

“…It is used as a coloring agent and dye intermediate in fibers and plastic synthesis, carbene ligand generation, and corrosion inhibitors [10][11][12]. It also works as a potent drug against various diseases and behaves as antitumor, antimicrobial, antifungal, antiulcer, antioxidant, anti-inflammatory agent, and corticotropin-releasing factor (CRF) receptor-selective antagonists [13][14][15][16] etc. (Scheme 2).…”

mentioning

confidence: 99%

Recent Advances in the Synthesis of Perimidines and their Applications

Sahiba¹,

Agarwal²

2020

Top Curr Chem (Z)

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Perimidines are versatile scaffolds and a fascinating class of N-heterocycles that have evolved significantly in recent years due to their immense applications in life sciences, medical sciences, and industrial chemistry. Their ability of molecular interaction with different proteins, complex formation with metals, and distinct behavior in various ranges of light makes them more appealing and challenging for future scientists. Various novel technologies have been developed for the selective synthesis of perimidines and their conjugated derivatives. These methods extend to the preparation of different bioactive and industrially applicable molecules. This review aims to present the most recent advancements in perimidine synthesis under varied conditions like MW radiation, ultrasound, and grinding using different catalysts such as ionic liquids, acid, metal, and nanocatalyst and also under green environments like catalyst and solvent-free synthesis. The applications of perimidine derivatives in drug discovery, polymer chemistry, photo sensors, dye industries, and catalytic activity in organic synthesis are discussed in this survey. This article is expected to be a systematic, authoritative, and critical review on the chemistry of perimidines that compiles most of the state-of-art innovation in this area.

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ChemInform Abstract: Synthesis, Structure and Cytostatic Activity of a Series of 2‐Substituted Perimidines.

Abstract: 215ChemInform Abstract The presence of a basic nitrogen in the side chain of the title compounds, e.g. (IV) and (VI), is important for their in vitro cytotoxic activity. The most active derivative is (IVa).

Cited by 3 publications

References 1 publication

Advances in organocatalyzed synthesis of organic compounds

Advances in organocatalyzed synthesis of organic compounds

A New Heterocyclic 1H-perimidine synthesized 2-(2,3-dihydro-1H-périmidin-2yl-)-6-methoxyphenol: Evaluation of Acute Toxicity in Wistar Rat

Recent Advances in the Synthesis of Perimidines and their Applications

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