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Pyrimidine Derivatives (pyrimidine + derivative)
Selected AbstractsPromiscuous Zinc-Dependent Acylase-Mediated One-Pot Synthesis of Monosaccharide-Containing Pyrimidine Derivatives in Organic MediumADVANCED SYNTHESIS & CATALYSIS (PREVIOUSLY: JOURNAL FUER PRAKTISCHE CHEMIE), Issue 11-12 2009Qi Wu Abstract A facile one-pot synthesis route to monosaccharide-containing pyrimidine derivatives was developed by combining the two types of catalytic activities of one enzyme in an organic medium, i.e., the Michael addition/acylation activities of zinc-dependent D -aminoacylase (DA) from Escherichia coli. First, the stepwise approach was investigated. DA showed higher activity towards the Michael addition than acylation in this reaction system. The enzymatic Michael additions of pyrimidines to vinyl acrylate proceeded very rapidly and the initial reaction rates for the Michael addition of pyrimidines to vinyl acrylate were 7.2,16.5,mM,min,1. The catalytic specificity of aminoacylases toward Michael addition was demonstrated by the combination of different control experiments. Then, the two steps could be performed in one pot and a single aminoacylase catalyzed one-pot biotransformation was constructed. Using this strategy, a series of saccharide-pyrimidine complexes with potentially biological and pharmacological applications was prepared efficiently. This high Michael addition activity of zinc-dependent aminoacylases and the novel single aminoacylase-catalyzed one-pot synthesis combining two catalytic activities in vitro is of practical significance in expanding the application of enzymes and in the evolution of new biocatalysts. [source] Synthesis and Biological Evaluation of Some Novel Polysubstituted Pyrimidine Derivatives as Potential Antimicrobial and Anticancer AgentsARCHIV DER PHARMAZIE, Issue 5 2009Sherif A. F. Rostom Abstract Synthesis and evaluation of the antimicrobial and cytotoxic activity of two series of polysubstituted pyrimidines comprising the thioether functionality and other pharmacophores, reported to contribute to various chemotherapeutic activities are described. All newly synthesized compounds were subjected to in-vitro antibacterial and antifungal screening. Out of the compounds tested, 18 derivatives displayed an obvious inhibitory effect on the growth of the tested Gram-positive and Gram-negative bacterial strains, with special effectiveness against the Gram-positive strains. Compounds 1, 2, 6, 7, 9, 10, 11, 21, and 24 revealed remarkable broad antibacterial spectrum profiles. Among those, compounds 1, 2, 6, 7, 9, and 24 exhibited an appreciable antifungal activity against C. albicans. Compound 2 proved to be the most active antimicrobial member identified here as it showed twice the activity of ampicillin against B. subtilis and the same activity of ampicillin against M. Luteus and P. aeruginosa together with a moderate antifungal activity. Further, eleven analogs were evaluated for their in-vitro cytotoxic potential utilizing the standard MTT assay against a panel of three human cell lines: breast adenocarcinoma MCF7, hepatocellular carcinoma HePG2, and colon carcinoma HT29. The obtained data revealed that six of the tested compounds 1, 3, 7, 12, 13, and 15 showed a variable degree of cytotoxic activity against the tested cell lines at both the LC50 and LC90 levels. Compound 7 proved to be the most active cytotoxic member in this study with special effectiveness against the colon carcinoma HT29 and breast cancer MCF7 human cell lines for LC50 and LC90. Thus, compounds 1 and 7 could be considered as possible dual antimicrobial-anticancer agents. [source] ChemInform Abstract: Reduction of Pyrimidine Derivatives by LiAlH4.CHEMINFORM, Issue 7 2008Yu-Xiu Liu Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Synthesis and Biological Evaluation of New Pyrimidine Derivatives.CHEMINFORM, Issue 33 2006O. A. Fathalla Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Synthesis and Reactions of Some New Substituted Pyridine and Pyrimidine Derivatives as Analgesic Anticonvulsant and Antiparkinsonian Agents.CHEMINFORM, Issue 2 2006Abd El-Galil E. Amr Abstract For Abstract see ChemInform Abstract in Full Text. [source] Syntheses of 2,4,6-Trisubstituted Pyrimidine Derivatives as a New Class of Antifilarial Topoisomerase II Inhibitors.CHEMINFORM, Issue 15 2005Sanjay Babu Katiyar Abstract For Abstract see ChemInform Abstract in Full Text. [source] Enaminonitrile in Heterocyclic Synthesis: Synthesis and Reactions of Some Pyrimidine Derivatives.CHEMINFORM, Issue 5 2005H. H. Abdel-Razik Abstract For Abstract see ChemInform Abstract in Full Text. [source] Microwave Assisted Solid Phase Synthesis of Pyrimidine Derivatives.CHEMINFORM, Issue 10 2003Mazaahir Kidwai Abstract For Abstract see ChemInform Abstract in Full Text. [source] Synthesis of Polyfunctionally Substituted Fused Pyrimidine Derivatives as Antimicrobial AgentsCHINESE JOURNAL OF CHEMISTRY, Issue 8 2008Abd EI-Monem Mohamed Farag EISSA Abstract A variety of pyrimidine derivatives 2,4 and annulated pyrimidine derivatives 5,17 have been synthesized via a sequence of heterocyclization reaction of readily available 6-naphthyl-4-oxo-2-thioxo-1,2,3,4-tetrahydroprimidine-5-carbonitrile (1) with different acidic and basic reagents. The new compounds were synthesized with the aim of study of their antimicrobial activity. The structures of all synthesized compounds were elucidated by elemental analysis and spectroscopic studies. [source] An Efficient Synthesis of Novel Hexahydropyrido[2,3- d]pyrimidine Derivatives from (Arylmethylidene)pyruvic Acids (=(3E)-4-Aryl-2-oxobut-3-enoic Acids) in Aqueous MediaHELVETICA CHIMICA ACTA, Issue 5 2009Saeed Balalaie Abstract A series of new hexahydropyrido[2,3- d]pyrimidine derivatives 3 were synthesized by the cyclocondensation reaction of (arylmethylidene)pyruvic acids (=(3E)-4-aryl-2-oxobut-3-enoic acids) 1 and 6-aminouracils (=6-aminopyrimidine-2,4(1H,3H)-diones) 2 in H2O under reflux conditions (Scheme,1, Table). This novel protocol has the advantages of facility, of easy workup, of high yields, and of an environmentally benign procedure. The structures of compounds 3a,3f were corroborated spectroscopically (IR, 1H- and 13C-NMR, and EI-MS). A plausible mechanism for the reaction is proposed (Scheme,2). [source] Pyrazolo[3,4- d]pyrimidine Derivatives as COX-2 Selective Inhibitors: Synthesis and Molecular Modelling StudiesARCHIV DER PHARMAZIE, Issue 6 2009Demetrio Raffa Abstract The pyrazolo[3,4- d]pyrimidine system shows a multitude of interesting pharmacological properties. Owing to the potential anti-inflammatory activity of 5-benzamido-pyrazolo[3,4- d]pyrimidin-4-one derivatives and considering the easy synthesis of this class of compounds, a set of new 5-benzamido-1H -pyrazolo[3,4- d]pyrimidin-4-ones has been prepared in 42-80% yields by reacting 5-aminopyrazole-4(N -benzoyl)carbohydrazide derivatives and the opportune triethylorthoesters. Compounds 8a, b, 10a,d, and 11a, b revealed a superior inhibitory profile against COX-2, when compared to that of reference standards NS398 and indomethacin. Molecular modelling studies confirmed the obtained biological results. [source] ChemInform Abstract: Molecular Iodine Promoted Synthesis of New Pyrazolo[3,4-d]pyrimidine Derivatives as Potential Antibacterial Agents.CHEMINFORM, Issue 23 2010Mehdi Bakavoli Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: An Efficient Microwave-Assisted Synthesis of Pyrido[2,3-d]pyrimidine Derivatives.CHEMINFORM, Issue 45 2009Shujiang Tu Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Synthesis and Antiproliferative Activities of Pyrrolo[2,3-d]pyrimidine Derivatives for Melanoma Cell.CHEMINFORM, Issue 11 2009Myung-Ho Jung Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Enaminonitriles in Heterocyclic Synthesis: Novel Synthesis of 3-Aminopyrroles and Pyrrolo[3,2-d]pyrimidine Derivatives.CHEMINFORM, Issue 36 2008Abdellatif M. Salaheldin Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: A Novel, One-Pot, Three-Component Synthesis of 5H-[1,3]Thiazolo[3,2-a]pyrimidine Derivatives.CHEMINFORM, Issue 10 2008Mehdi Adib Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Three-Component, One-Pot Synthesis of Pyrimido[4,5-b]quinoline and Pyrido[2,3-d]pyrimidine Derivatives.CHEMINFORM, Issue 47 2007N. A. Hassan Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Synthesis of New Pyrido[2,3-d]pyrimidine Derivatives by Three-Component Condensation of 5-Acetyl-4-aminopyrimidines, Cyclohexane-1,3-diones, and Orthocarboxylic Acid Esters.CHEMINFORM, Issue 36 2007A. V. Komkov Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Synthesis of Novel Thieno[2,3-b][1,6]naphthyridine and Thieno[2,,3,:2,3]pyrido[4,5-d]pyrimidine Derivatives.CHEMINFORM, Issue 30 2007Fatima Al-Omran Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] An Efficient Regiospecific Synthesis of Highly Functionalized Novel Dihydropyrimido[4,5-d]pyrimidine Derivatives by a Three-Component One-Pot Condensation under Solvent-Free Conditions.CHEMINFORM, Issue 28 2007Dipak Prajapati Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] An Efficient Route to Thieno[2,3-d]pyrimidine Derivatives by Tandem [2,3] and [3,3] Sigmatropic Rearrangement.CHEMINFORM, Issue 15 2007Krishna C. Majumdar Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] KF-Alumina Catalyzed One-Pot Synthesis of Pyrido[2,3-d]pyrimidine Derivatives.CHEMINFORM, Issue 19 2005Xiang-shan Wang Abstract For Abstract see ChemInform Abstract in Full Text. [source] Preparation of Nitrogen Heterocycles of Spiro[furo[2,3-d]-pyrimidine]pyrimidine Derivatives.CHEMINFORM, Issue 10 2005Branko S. Jursic Abstract For Abstract see ChemInform Abstract in Full Text. [source] Synthesis of 2,3-Dihydro-1,3,4-thiadiazole, Thiazole, and Thiazolo[4,3-a]pyrimidine Derivatives from Ethyl Benzoylacetate.CHEMINFORM, Issue 32 2004Nora M. Rateb Abstract For Abstract see ChemInform Abstract in Full Text. [source] ChemInform Abstract: Synthesis and Antimicrobial Activities of Novel Naphtho[2,1-b]pyran, Pyrano[2,3-d]pyrimidine and Pyrano[3,2-e][1,2,4]triazolo[2,3-c]pyrimidine Derivatives.CHEMINFORM, Issue 17 2002Ahmed H. Bedair Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Synthesis and Bioactivity of Novel Triazolo[1,5-a]pyrimidine Derivatives.CHEMINFORM, Issue 3 2002Guangfu Yang Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Application of Selective Palladium-Mediated Functionalization of the Pyrido[3,,2,:4,5]pyrrolo[1,2- c]pyrimidine Heterocyclic System for the Total Synthesis of Variolin B and Deoxyvariolin B,EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 29 2010Alejandro Baeza Abstract The reaction of protected 3-bromo-2-(bromomethyl)-4-methoxypyrrolo[2,3- b]pyridine and tosylmethyl isocyanide (TosMIC) afforded a pyrido[3,,2,:4,5]pyrrolo[1,2- c]pyrimidine derivative in good yield. This compound was transformed through installation of the pyrimidine moiety in the C5 position, hydrolysis, and decarboxylation in an advanced intermediate for the total or formal synthesis of the naturalalkaloid variolin B. Reaction of 3-bromo-2-(bromomethyl)-4-chloropyrrolo[2,3- b]pyridine with N -tosylmethyl dichloroformimide as a synthetic TosMIC equivalent afforded trihalo-substituted pyrido[3,,2,:4,5]pyrrolo[1,2- c]pyrimidine. This compound was used in a new total synthesis of the alkaloid variolin B by selective and sequential C,N, C,C, and C,O palladium-mediated functionalization at the C9, C5, and C4 positions of the pyrido[3,,2,:4,5]pyrrolo[1,2- c]pyrimidine system. A formal synthesis of deoxyvariolin B is also described by using the same synthetic strategy. [source] New N6 -substituted 8-alkyl-2-phenylmethylsulfanyl-adenines.JOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 4 2004Title compounds bearing substituents on C(2), C(6) and C(8) were prepared from a newly synthesized pyrimidine derivative 11. The new pyrimidine 11 was generated from compound 2 through two different synthetic schemes. In one pathway, compound 2 was nitrosated, reduced and alkylated to produce com pounds 9, 10 and 11 respectively (Scheme). In an alternate route using compound 2 as the starting material, a coupling reaction using the diazonium salt derived from p -methylaniline afforded the azo derivative 7, which was subsequently alkylated and reductively cleaved to form compounds 8 and 11 respectively (See Scheme). Compound 11 was annulated to the corresponding hypoxanthine derivatives 12,14; compounds 12 and 13 were chlorinated with phosphorus oxychloride, then reacted with amines to yield compound 17 and 20 respectively. Compounds 21, 22 and 23 were obtained by oxidation of the corresponding sulfide as depicted in Scheme. Alkylation of the thiol function of 1 gave a mixture of 3 and 4. Compound 3 was chlo rinated to 5. Nitration of 5 resulted in electrophilic aromatic substitution of the aryl ring and concomitant oxidation of the sulfide to the sulfoxide, producing 6. [source] Tyrosine kinase inhibitors: From rational design to clinical trialsMEDICINAL RESEARCH REVIEWS, Issue 6 2001Peter Traxler Abstract Protein kinases play a crucial role in signal transduction as well as in cellular proliferation, differentiation, and various regulatory mechanisms. The inhibition of growth related kinases, especially tyrosine kinases, might provide new therapies for diseases such as cancer. The progress made in the crystallization of protein kinases has confirmed that the ATP-binding domain of tyrosine kinases is an attractive target for drug design. Three successful examples of drug design at Novartis using a tyrosine kinase as a molecular target are described. PKI166, a pyrrolo[2,3,- d]pyrimidine derivative, is a dual inhibitor of both the EGFR and the ErbB2 kinases. The compound entered clinical trials in 1999, based on its favorable preclinical profile: potent inhibition of EGF-mediated signalling in cells, in vivo antitumor activity in several EGFR overexpressing xenograft tumor models in nude mice, long-lasting inhibition of EGF-stimulated EGFR autophosphorylation in tumor tissue, good oral bioavailability in animals, and no prohibitive in vitro and in vivo toxicity findings. The anilino-phthalazine derivative PTK787/ZK222584 (Phase I, co-developed by Schering AG, Berlin) is a potent and selective inhibitor of both the KDR and Flt-1 kinases with interesting anti-angiogenic and pharmacokinetic properties (orally bioavailable). STI571 (GlivecÔ, GleevecÔ), a phenylamino-pyrimidine derivative, is a potent inhibitor of the Abl tyrosine kinase, which is present in 95% of patients with chronic myelogenous leukemia (CML). The compound specifically inhibits proliferation of v-Abl and Bcr-Abl expressing cells (including cells from CML patients) and shows anti-tumor activity as a single agent in animal models at well-tolerated doses. Pharmacologically relevant concentrations are achieved in the plasma of animals (oral administration). Promising data from phase I and II clinical trials in CML patients (98% haematological response rate in Phase I) support the fact that the STI571 represents a new treatment modality for CML. In addition, potent inhibition of the PDGFR and c-Kit tyrosine kinases also indicates its possible clinical use in solid tumors. © 2001 John Wiley & Sons, Inc. Med Res Rev, 21, No. 6, 499,512, 2001 [source] An Efficient Synthesis of Novel Hexahydropyrido[2,3- d]pyrimidine Derivatives from (Arylmethylidene)pyruvic Acids (=(3E)-4-Aryl-2-oxobut-3-enoic Acids) in Aqueous MediaHELVETICA CHIMICA ACTA, Issue 5 2009Saeed Balalaie Abstract A series of new hexahydropyrido[2,3- d]pyrimidine derivatives 3 were synthesized by the cyclocondensation reaction of (arylmethylidene)pyruvic acids (=(3E)-4-aryl-2-oxobut-3-enoic acids) 1 and 6-aminouracils (=6-aminopyrimidine-2,4(1H,3H)-diones) 2 in H2O under reflux conditions (Scheme,1, Table). This novel protocol has the advantages of facility, of easy workup, of high yields, and of an environmentally benign procedure. The structures of compounds 3a,3f were corroborated spectroscopically (IR, 1H- and 13C-NMR, and EI-MS). A plausible mechanism for the reaction is proposed (Scheme,2). [source] | |||||||||||||||||||||||||