Synthesis and Muscarinic Activity of 1,2,3,4-Tetrahydropyrimidine Derivatives

Jung, Myung Hun; Park, Jewn-Giew; Yang, Kong Jae; Lee, Mi-Jeoung

doi:10.1002/1521-4184(200103)334:3<79::aid-ardp79>3.0.co;2-7

Cited by 23 publications

(7 citation statements)

References 10 publications

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“…These compounds were used for the treatment of Alzheimer's disease [182][183][184][185]. Several papers have been devoted to the investigation of piperazine oximes as neurokinin antagonists; these compounds are used in the treatment of diseases of the central nervous system [186][187][188][189].…”

Section: Action On the Central Nervous Systemmentioning

confidence: 99%

Oximes of six-membered heterocyclic compounds with two and three heteroatoms. II.* Reactions and biological activity (review)

Абеле

Golomba

et al. 2010

Chem Heterocycl Comp

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Data on the reactions of pyridazine, pyrimidine, pyrazine, triazine, oxazine, thiazine, oxadiazine, and thiadiazine aldoximes, ketoximes, and amidoximes and their derivatives are reviewed. The synthesis of new heterocycles based on the oximes of six-membered heterocyclic compounds with two and three heteroatoms is considered separately. The principal results of research into the biological activity of these oximes and their ethers are also presented.The oximes of six-membered heterocyclic compounds with two and three heteroatoms are widely used as intermediates in fine organic synthesis. Their production methods and structural features were examined in the review [1]. In this article we discuss the reactions of pyridazine, pyrimidine, pyrazine, triazine, oxazine, thiazine, oxadiazine, and thiadiazine aldoximes, ketoximes, and amidoximes and their derivatives. Methods for the synthesis of new heterocyclic systems from the derivatives of these oximes are considered in a separate section. In the last section some results from investigation of the biological activity of the ethers of these oximes are considered.

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Section: Action On the Central Nervous Systemmentioning

confidence: 99%

Oximes of six-membered heterocyclic compounds with two and three heteroatoms. II.* Reactions and biological activity (review)

Абеле

Golomba

et al. 2010

Chem Heterocycl Comp

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“…In recent years, substituted 2-oxo/thioxo-1,2,3,4-tetrahydropyrimidines received significant attention owing to their diverse range of biological properties such as calcium channel modulator [1], 1-adrenoreceptor selective antagonist [2], HIV gpl20-CD 4 inhibition [3], antiviral [4], oral antihypertensive [5], useful for the treatment of benign prostatic hyperplasia [6], antiinflammatory [7], Muscarinic [8], antifungal and antibacterial [9]. The presence of several interacting functional groups in these compounds also determines their great synthetic potential [10].…”

Section: Introductionmentioning

confidence: 99%

<b>Synthesis, screening and QSAR studies of 3-benzoyl-2-oxo/thioxo-1,2,3,4-tetrahydro-pyrimidine analogues as antibacterial agents</b>

Sawant

Bhatia

2008

Bull. Chem. Soc. Eth.

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The purpose of this study was to synthesize several 3-benzoyl-5-acyl-6-methyl-4-substituted-2oxo/thioxo-1,2,3,4-tetrahydropyrimidines, evaluate them for their antibacterial activity and to establish correlation between the activity and physicochemical properties. 5-Acyl-6-methyl-4-substituted-2-oxo/thioxo-1,2,3,4tetrahydropyrimidines (A) were synthesized by cyclocondensation reaction between appropriate aldehyde, acetoacetate and urea/thiourea in presence of aluminium chloride and hydrochloric acid which upon treatment with benzoyl chloride in presence of pyridine in benzene furnish the title compounds (1-28). The structures of all title compounds have been confirmed on the basis of their analytical, IR and NMR spectral data. The title compounds have been tested for antibacterial activity against Staphylococcus aureus. The compounds were divided into training and test sets. A quantitative structure activity relationship study was made using various descriptors. Several statistical expressions were developed using stepwise multiple linear regression analysis. The best quantitative structure activity relationship model was further cross validated. The study revealed that total positive partial charge (PC+) and total polar negative Van der Waals surface area (Q_VSA_PNEG) contributes negatively where as contribution of Van der Waals surface area to molar refractivity (SMR_VSA7) contributes positively to the antibacterial activity. The compounds with improved antibacterial potential can be successfully designed with selected quantitative structure activity relationship model.

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“…1,2,3,4-Tetrahydropyrimidine ring is an important moiety in both natural and synthetic organic compounds, and many compounds containing it show interesting biological activities [6][7][8][9][10][11][12]. Accordingly many methods have been developed for the synthesis of various 1,2,3,4-tetrahydropyrimidines [13].…”

Section: Introductionmentioning

confidence: 99%

A convenient three-component reaction for the construction of multifunctional 6-fluoroalkyl-1,2,3,4-tetrahydropyrimidines

Lin

Liu

Zhao

2005

Journal of Fluorine Chemistry

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Synthesis and Muscarinic Activity of 1,2,3,4-Tetrahydropyrimidine Derivatives

Cited by 23 publications

References 10 publications

Oximes of six-membered heterocyclic compounds with two and three heteroatoms. II.* Reactions and biological activity (review)

Oximes of six-membered heterocyclic compounds with two and three heteroatoms. II.* Reactions and biological activity (review)

<b>Synthesis, screening and QSAR studies of 3-benzoyl-2-oxo/thioxo-1,2,3,4-tetrahydro-pyrimidine analogues as antibacterial agents</b>

A convenient three-component reaction for the construction of multifunctional 6-fluoroalkyl-1,2,3,4-tetrahydropyrimidines

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