Synthesis and <i>in vivo</i> diuretic activity of some novel pyrimidine derivatives

Majeed, Jaseela; Shaharyar, Mohammad

doi:10.3109/14756366.2011.557022

Cited by 29 publications

(16 citation statements)

References 26 publications

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“…High yields of 1,6-dihydropyrimidines result from the reaction of chalcone-type compounds with urea [426], thiourea and guanidine hydrochloride [427], under basic conditions (Scheme 60). A facile microwave assisted synthesis of 4,5-dihydropyrimidin-2amines occurs through the reaction of benzofuran-chalcones and guanidine hydrochloride in the presence of NaOH [428].…”

Section: Transformation Of Chalcones To Pyrimidinesmentioning

confidence: 99%

Chalcones as Versatile Synthons for the Synthesis of 5- and 6-membered Nitrogen Heterocycles

Albuquerque¹,

Santos²,

Cavaleiro³

et al. 2014

COC

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Chalcones belong to the flavonoid family which constitutes one of the major classes of naturally occurring oxygen heterocyclic compounds. The ,-unsaturated carbonyl system of chalcones possesses two electrophilic reactive centers allowing them to participate in addition reactions via attack to the carbonyl group (1,2-addition) or involving the-carbon (1,4-conjugate addition), leading to the synthesis of promising bioactive heterocyclic compounds. The purpose of this review is to present a systematic survey of the most recent literature that uses chalcones in the synthesis of biologically active 5-and 6-membered nitrogen heterocycles such as pyrroles, indoles, isoxazoles, imidazoles, pyrazoles, indazoles, triazoles, tetrazoles, pyridines and pyrimidines. Efficiency, easy-to-handle and cheap reagents, alternative heating conditions and greener protocols will be highlighted. In this review we will cover the literature since the beginning of the 21 st century in more than 400 publications.

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Section: Transformation Of Chalcones To Pyrimidinesmentioning

confidence: 99%

Chalcones as Versatile Synthons for the Synthesis of 5- and 6-membered Nitrogen Heterocycles

Albuquerque¹,

Santos²,

Cavaleiro³

et al. 2014

COC

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“…In medicinal chemistry, both pyrimidine derivatives and pyrazole derivatives have been very well known for their biological potency. They demonstrate various types of pharmacological activities such as anticancer, antiviral, anti‐HIV, antihypertensive, antitubercular, diuretic, antibacterial, antifungal, and antiepileptic properties, and many classes of chemotherapeutic agents containing pyrimidine and pyrazolenucleus are in clinical trials.…”

Section: Introductionmentioning

confidence: 99%

Pyrimidine‐based pyrazoles as cyclin‐dependent kinase 2 inhibitors: Design, synthesis, and biological evaluation

Vekariya

Brahmkshatriya

et al. 2018

Chem Biol Drug Des

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A series of new pyrimidine-pyrazole hybrid molecules were designed as inhibitors of cyclin-dependent kinase 2. Designed compounds were docked using Glide and the compounds showing good score values and encouraging interactions with the residues were selected for synthesis. They were then evaluated using CDK2-CyclinA2 enzyme inhibition by a luminescent ADP detection assay. We show that of the 26 compounds synthesized and evaluated, at least 5 compounds were found to be highly potent (IC < 20 nm); which can be further optimized to have selectivity over other kinase isoforms.

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“…Furthermore, pyrimidine derivatives have an extensive scope of healing actions such as: anti-microbial, [16][17][18][19] anti-viral, anti-HIV, [20,21] anti-tubercular, [22,23] antimalarial, [24,25] analgesic, anti-inflammatory, [26,27] diuretic, [28] cardiovascular, [29,30] hypnotic for the nervous system, [31,32] and antioxidant, [33,34] anticancer. [35] On the other hand, many pyrimidine-5-carbo nitriles, [2,[36][37][38][39] and pyrimidinethione derivatives [40][41][42][43][44] have been reported to possess a significant anticancer and antimicrobial actions.…”

mentioning

confidence: 99%

Synthesis and antitumor activity of some nitrogen heterocycles bearing pyrimidine moiety

Ahmed

El‐Hashash

Marzouk

et al. 2020

Journal of Heterocyclic Chem

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Synthesis of novel pyrimidine derivatives 4‐16 was accomplished by heterocyclization of polarized system, for example, Chalcone. Claisen‐Schmidt condensation of 2‐acetyl naphthalene with 4‐(N, N‐dimethylaminobenzaldehyde) afforded chalcone 3, which was utilized for synthesis various pyrimidine derivatives by treatment with urea, thiourea, and guandine hydrochloride in ethanolic sodium hydroxide solution. The reactivity of the synthesized pyrimidine derivatives towards different nucleophilic and electrophilic reagent were examined. The constructions of the newly synthesized pyrimidine derivatives were elucidated from their spectral and elemental analysis. All the synthesized compounds were tested in vitro for their anticancer activities against HePG‐2 and MCF‐7 cell lines. Some of them posses a wide range of pharmacological activity. Finally, a molecular docking study was conducted to reveal the probable interaction with the dihydrofolate reductase (DHFR) active site.

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Synthesis and in vivo diuretic activity of some novel pyrimidine derivatives

Cited by 29 publications

References 26 publications

Chalcones as Versatile Synthons for the Synthesis of 5- and 6-membered Nitrogen Heterocycles

Chalcones as Versatile Synthons for the Synthesis of 5- and 6-membered Nitrogen Heterocycles

Pyrimidine‐based pyrazoles as cyclin‐dependent kinase 2 inhibitors: Design, synthesis, and biological evaluation

Synthesis and antitumor activity of some nitrogen heterocycles bearing pyrimidine moiety

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