Chapter 3 Antidepressant Agents

Luttinger, Daniel; Hlasta, Dennis J.

doi:10.1016/s0065-7743(08)61151-3

Cited by 21 publications

(24 citation statements)

References 81 publications

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“…Nowadays, pyrazole systems, as biomolecules, have attracted more attention due to their interesting pharmacological properties. This heterocycle can be traced in a number of well-established drugs belonging to different categories with diverse therapeutic activities ( Figure 1 ) [ 3 , 4 , 5 , 6 , 7 , 8 , 9 , 10 ].…”

Section: Introductionmentioning

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: Introductionmentioning

confidence: 99%

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

et al. 2018

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“…Various pharmacological and biological activities have been reported for pyrazoles, including sodium channel blocker, [1] antiglaucoma, [2] antitubercular, [3] antiviral, [4] anti‐inflammatory, [5] antioxidant, [6] anticancer, [7–14] antialzheimer, [15–19] antidiabetic, [20–23] antimalarial, [24–26] antiparkinson, [27–29] antileishmanial and antitrypanosomal [30] . For example, compound 1 as an antialzheimer, [15] compound 2 as an antidiabetic, [20] fezolamine ( 3 ) as an antidepressant drug, [31] lozanolac ( 4 ) as an anti‐inflammatory, [32] rimonabant ( 5 ) as a antiobesity drug [33] and difenamizole ( 6 ) as an analgesic drug [34] are known ( Figure 1).…”

Section: Introductionmentioning

confidence: 99%

Preparation of New Spiropyrazole, Pyrazole and Hydantoin Derivatives and Investigation of Their Antioxidant and Antibacterial Activities.

Ghasempour

Asghari

Tajbakhsh

et al. 2021

Chemistry & Biodiversity

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In this study, the synthesis of new spiropyrazoles, pyrazole and hydantoin heterocycles is reported by three component reactions of parabanic acids, hydrazine derivatives, and phenacyl bromides in the presence of triphenylphosphine as a nucleophile and triethylamine as a base in good to high yields (69–91 %). Evaluation of the synthesized compounds revealed a good to excellent antioxidant activities (37.6–96.2 %) using DPPH inhibitory potency. Among these compounds, hydantoin derivatives displayed higher antioxidant activities (93.7–96.2 %) comparing with spiropyrazoles and pyrazoles. The obtained results showed that Cl and Br substituents on the phenyl ring increased antioxidant activities of the related heterocycles. The antibacterial activities of the synthesized compounds were examined against two Gram‐negative (Escherichia coli and Pseudomonas aeruginosa) and two Gram‐positive (Staphylococcus aureus and Bacillus subtilis) bacteria. Among the synthesized heterocycles, 2‐[1,3‐dimethyl‐2,5‐dioxo‐4‐(2‐oxo‐2‐phenylethyl)imidazolidin‐4‐yl]hydrazine‐1‐carbothioamide exhibited the excellent antibacterial activity against both Gram‐positive and Gram‐negative bacteria.

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“…There are many naphthalene derived bioactive phytoconstituents present in nature such as rifampicin (anti-tubercular agent)[ 13 ]. Similarly, the pyrazole ring is present as the core structure of several leading drugs such as celecoxib, a potent anti-inflammatory[ 14 ], the anti-depressant agent fezolamine[ 15 ], the anti-obesity rimonabant[ 16 ], and difenamizole[ 17 ] (an analgesic). Pyrazole derivatives exhibit several biological activities including anti-bacterial properties [ 18 , 19 ].…”

Section: Introductionmentioning

confidence: 99%

Design and synthesis of 4-[4-formyl-3-(2-naphthyl)pyrazol-1-yl]benzoic acid derivatives as potent growth inhibitors of drug-resistant Staphylococcus aureus

Alnufaie

Alsup

et al. 2020

J Antibiot

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We report the synthesis and antimicrobial studies of a new series of naphthyl-substituted pyrazole-derived hydrazones. Many of these novel compounds are potent growth inhibitors of several strains of drug-resistant bacteria. These potent compounds have inclined growth inhibitory properties for planktonic Staphylococcus aureus and Acinetobacter baumannii, and its drug-resistant variants with minimum inhibitory concentration (MIC) as low as 0.78 and 1.56 μg/mL respectively. These compounds also show potent activity against S. aureus and A. baumannii biofilm formation and eradication properties. Time Kill Assay shows that these compounds are bactericidal for S. aureus and bacteriostatic for A. baumannii . The probable mode of action is the disruption of the bacterial cell membrane. Furthermore, potent compounds are nontoxic to human cell lines at several fold higher concentrations than the MICs.

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Chapter 3 Antidepressant Agents

Cited by 21 publications

References 81 publications

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

Preparation of New Spiropyrazole, Pyrazole and Hydantoin Derivatives and Investigation of Their Antioxidant and Antibacterial Activities.

Design and synthesis of 4-[4-formyl-3-(2-naphthyl)pyrazol-1-yl]benzoic acid derivatives as potent growth inhibitors of drug-resistant Staphylococcus aureus

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