Synthesis, Characterization and Antimicrobial Activities of Chalcones and Their Post Transformation to Pyrazole Derivatives

Ramyashree, D.; Raghavendra, K. R.; Kumar, A. Dileep; Vagish, C.B.; Kumar, K. Ajay

doi:10.14233/ajchem.2017.20561

Cited by 4 publications

(3 citation statements)

References 7 publications

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“…As stated, the chalcone derivatives 24 (A 1 K i (r) = 5.3 µM) and 29 (A 1 K i (r) = 6.1 µM) ( Table 2) showed selective A 1 AR affinity below 10 µM, and although, the K i (r) values of these compounds were quite similar the substitutions on ring B were not; 24 was C2′, C4′, C5′-trimethoxy substituted and 29 was C2′-chloro substituted. In the past, the antimicrobial (Karaman et al 2010;Ramyashree et al 2017), anticancer (Juvale et al 2012;Mellado et al 2018) and/or antioxidant (Shenvi et al 2013) activities of compounds 24 and 29 were also explored, and now, selective A 1 AR affinity may be added.…”

Section: Structure-affinity Relationships (Sar)mentioning

confidence: 99%

C3 amino-substituted chalcone derivative with selective adenosine rA1 receptor affinity in the micromolar range

2020

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To identify novel adenosine receptor (AR) ligands based on the chalcone scaffold, herein the synthesis, characterization and in vitro and in silico evaluation of 33 chalcones ( 15 – 36 and 37 – 41 ) and structurally related compounds ( 42 – 47 ) are reported. These compounds were characterized by radioligand binding and GTP shift assays to determine the degree and type of binding affinity, respectively, against rat ( r ) A 1 and A 2A ARs. The chalcone derivatives 24 , 29 , 37 and 38 possessed selective A 1 affinity below 10 µM, and thus, are the most active compounds of the present series; compound 38 was the most potent selective A 1 AR antagonist ( K i ( r ) = 1.6 µM). The structure–affinity relationships (SAR) revealed that the NH 2 -group at position C3 of ring A of the chalcone scaffold played a key role in affinity, and also, the Br-atom at position C3′ on benzylidene ring B. Upon in vitro and in silico evaluation, the novel C3 amino-substituted chalcone derivative 38 —that contains an α,ß-unsaturated carbonyl system and easily allows structural modification—may possibly be a synthon in future drug discovery. Graphic abstract C3 amino-substituted chalcone derivative ( 38 ) with C3′ Br substitution on benzylidene ring B possesses selective adenosine r A 1 receptor affinity in micromolar range. Electronic supplementary material The online version of this article (10.1007/s11696-020-01414-9) contains supplementary material, which is available to authorized users.

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Section: Structure-affinity Relationships (Sar)mentioning

confidence: 99%

C3 amino-substituted chalcone derivative with selective adenosine rA1 receptor affinity in the micromolar range

2020

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“…Phenylhydrazine hydrochloride (PHH) has been widely applied to synthesize multiple fine chemicals [18][19][20][21]. Nowadays, there are 212 PHH suppliers in the global range, and around 70% of the enterprises are located in China [22].…”

Section: Introductionmentioning

confidence: 99%

Harmless Treatment of Phenylhydrazine Hydrochloride Production Effluent: From Lab Scale to Pilot Scale

Zhou

Xi-de

Chen

2019

Water

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More economical and effective technology is being developedin the wastewater treatment process to deal with the products of phenylhydrazine hydrochloride (PHH). Fixed ammonium in the effluent is converted to free ammonia by utilizing the neutralization reaction, and the sulfate is removed in the form of gypsum. Meanwhile, the toxic PHH is recycled according to the extraction and re-extraction technology. The raffinate phase is reused through boiling off ammonia vapor. The recovery rates of PHH reach 93.3% in the laboratory and 92.9% at the pilot scale, respectively. Compared with our previous work, the cost of the new technology is ~1/10 of the original, and the profit increases ~3.5-fold. Consequently, it has great potential to be applied to industrial production.

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“…As a crystalline organic compound with white or pink leaf-shaped crystals, phenylhydrazine hydrochloride (PHH) can be dissolved in water, and it can precipitate from the solution by adding concentrated hydrochloric acid (HCl). Nowadays, PHH has been widely applied in the production of organic intermediates for dye [1], pharmaceutical [2,3], and pesticide [4] industries. Therefore, the market demand for PHH is huge.…”

Section: Introductionmentioning

confidence: 99%

Research on the Treatment and Comprehensive Utilization of Phenylhydrazine Hydrochloride Effluent

Xi-de

Zhou

Zhang

2018

Water

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In the production process of 1 ton of phenylhydrazine hydrochloride (PHH);~10 tons of liquid waste are formed, which includes multiple contaminants but also recyclable resources. In order to realize the recyclingof residual PHH in liquid waste; a liquid ammonia neutralization method is utilized, and extraction-reextraction technology is adopted. As a result, the recovery rate of PHH reachedup to 90.0%. Meanwhile, 3.8 tons of ammonium salts can be obtained after the iquid ammonia neutralization reaction which can be reused as raw materials for compound fertilizer. During the treatment process, there is no discharge of the three wastes, which meets the requirements of harmless treatment. Finally, these results provide important reference values for PHH production enterprises to solve the problems of waste pollution and to achieve recycling of resources.

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Synthesis, Characterization and Antimicrobial Activities of Chalcones and Their Post Transformation to Pyrazole Derivatives

Cited by 4 publications

References 7 publications

C3 amino-substituted chalcone derivative with selective adenosine rA1 receptor affinity in the micromolar range

C3 amino-substituted chalcone derivative with selective adenosine rA1 receptor affinity in the micromolar range

Harmless Treatment of Phenylhydrazine Hydrochloride Production Effluent: From Lab Scale to Pilot Scale

Research on the Treatment and Comprehensive Utilization of Phenylhydrazine Hydrochloride Effluent

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