Synthesis, characterization and biological evaluation of novel 2,4,6-trisubstituted bis-pyrimidine derivatives

Parveen, Humaira; Hayat, Faisal; Mukhtar, Sayeed; Salahuddin, Attar; Khan, Andleeb; Islam, Fakhrul; Azam, Amir

doi:10.1016/j.ejmech.2011.05.055

Cited by 30 publications

(18 citation statements)

References 26 publications

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“…Nagaraj et al reported the synthesis of a series of bispyrimidines from the reaction of bischalcones with guanidine hydrochloride in aqueous NaOH in ethanol [422]. More examples arise from the reaction of bischalcones with guanidine hydrochloride in 1,4dioxane [423] and with pyrrolidine-1-carboxamidine hydrochloride or piperidine-1-carboxamidine hydrochloride in sodium isopropoxide / isopropanol (Scheme 58) [424].…”

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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“…For example Pyrazolo [3,4-d]pyrimidine derivatives are shown to exhibit anti-amoebic activity [7][8][9][10][11][12][13] and are potential anti-inflammatory agents [14,15], anti-coagulation inhibitors [16], xanthine oxidase inhibitors [17], antiproliferative and proapoptotic agents in various tumor types [18,19]. They are called SRC kinase inhibitors [20] and are beneficial in human cancers treating sustaining oncogenic activation of RET [21].…”

Section: Introductionmentioning

confidence: 99%

Reviewing of Synthesis and Computational Studies of Pyrazolo Pyrimidine Derivatives

Mohamed

Ahmed

2019

J. Chem. Rev.

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In this review we synthesized and conducted a computational studies on Pyrazolo pyrimidine's derivatives that were carried out through density functional theory level utilizing HF/6−311+G**and B3LYP/6−311+G**. Charge transfer occured through molecule was shown by the calculation of HOMO and LUMO energies. The electric dipole moment values (l) of the molecule were counted calculations of DFT. Some geometrical and structural parameters such as total energies (E), relative energies (DE), (bond length in Å, angles in degree), energy gap, relative Gibbs free energy, dipole moment, and molecular electrostatic potentials (MEP) were studied.

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“…On the basis of above observations and as a part of our ongoing research focused on the synthesis of biologically active heterocycles/organometallics, we have synthesized some novel pyrazoline‐based organometallic compounds containing ferrocenyl and quinoline units and evaluated for in vitro antimicrobial studies against fifteen ATCC bacterial and fungal stains to investigate pharmaceutical applications of these compounds.…”

Section: Introductionmentioning

confidence: 99%

Novel Pyrazoline‐based Organometallic Compounds Containing Ferrocenyl and Quinoline units: Synthesis, Characterization and Microbial susceptibilities

Parveen

Alatawi

Alsharif

et al. 2018

Applied Organom Chemis

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Some novel pyrazoline-based organometallic compounds were synthesized as new leads in antimicrobial chemotherapy. The structures of compounds were elucidated by different spectroscopic techniques and elemental analyses. All compounds were investigated for in vitro antimicrobial studies against fifteen ATTC bacterial and fungal strains. The microbial susceptibility of these compounds revealed that all the tested compounds gave good minimum inhibitory concentration (MIC) values against the tested organisms that are either similar or even better than the reference drugs amoxicillin and fluconazole, which gave MIC values 8-64 μg/ml against bacterial and 64 μg/ml against fungal strains, respectively. Among all compounds, compound (4d) 1-(5-(4-chlorophenyl)-3-ferrocenyl-4,5-dihydropyrazol-1-yl)-2-quinolin-8-yloxy) ethanone, emerged out the most promising antimicrobial organometallic derivative with MIC values against all the strains ranging from 8-32 μg/ml. Other compounds gave a range of MIC values between 16-64 μg/ml against S. bovis, 16-32 μg/ml against E. coli, and C. tropicalis except compound (4d) which gave MIC 8 μg/ml against S. bovis and E. coli, whereas 32 μg/ml against C. tropicalis.Collectively, these compounds gave a lower MIC value between 32-64 μg/ml against both of the biofilm forming strains namely, P. aeruginosa and S. mutans. The results of microbial susceptibility concluded that these novel organometallic compounds are new leads in antimicrobial chemotherapy and can be very useful for further optimization work on microbial chemotherapy. KEYWORDSantibacterial studies, antifungal studies, ferrocenyl and quinoline units, new leads in microbial chemotherapy, novel pyrazoline-based organometallics

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Synthesis, characterization and biological evaluation of novel 2,4,6-trisubstituted bis-pyrimidine derivatives

Cited by 30 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

Reviewing of Synthesis and Computational Studies of Pyrazolo Pyrimidine Derivatives

Novel Pyrazoline‐based Organometallic Compounds Containing Ferrocenyl and Quinoline units: Synthesis, Characterization and Microbial susceptibilities

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