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Dissertations / Theses on the topic 'Pirimidine'

Author: Grafiati
Published: 11 March 2023

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1

Fantinel, Leonardo. "Síntese de 2-fenil-3H-pirimidin-4-onas 6-metilsubstituídas e 4- trifluormetil-2-ureído pirimidinas." Universidade Federal de Santa Maria, 2009. http://repositorio.ufsm.br/handle/1/4171.

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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior<br>This study was carried out in three parts: At first, three methods for the bromination of 6-alkylsubstituted 2-phenyl-3H-pyrimidin-4-ones was developed for the synthesis of: (i) a new series of 6-alkylsubstituted 5-bromo-2-phenyl-3H-pyrimidin-4-ones, (ii) a new series of 6-(1-bromoalkyl)-2-phenyl-3H-pyrimidin-4-ones, and (iii) e new series of 5-bromo-6-(1-bromoalkyl)-2-phenyl-3H-pyrimidin-4-ones. On the second part, the brominated pyrimidines obtained, were used to synthesize new 6-methylsubstituted 2-phenyl-3Hpyrimidin-4-ones from
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2

Bolcato, Chiara. "Progettazione sintesi e valutazione biologica di sistemi eterociclici quali antagonisti per i recettori adenosinici. Validazione di modelli recettoriali." Doctoral thesis, Università degli studi di Trieste, 2008. http://hdl.handle.net/10077/2567.

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2006/2007<br>La tesi illustra il lavoro di dottorato mirato allo sviluppo di nuovi antagonisti adenosinici attivi nei confronti dei vari sottotipi recettoriali del ligando naturale Adenosina.<br>XX Ciclo<br>1977
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3

Vaitiulionytė, Diana. "Furo[2,3-d]pirimidinų sintezė ir savybės." Master's thesis, Lithuanian Academic Libraries Network (LABT), 2006. http://vddb.library.lt/obj/LT-eLABa-0001:E.02~2006~D_20060613_174528-81935.

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We report herein on the results of N- and O-alkylation of 5-cyano-2-methylsulfanyl-4(3H)- pyrimidinone with 4-substituted ω-bromoacetophenones. Synthesized N-(phenacyl)-4- pyrimidinones and 4-(phenacyloxy)pyrimidines with suitable substituents in pyrimidine ring are versatile synthons for the preparation of fused pyrimidine heterocycles. Chemical properties of new furo[2,3-d]pyrimidines were investigated. The structure of synthesized compounds was confirmed by data of 1H NMR, IR and UV spectra.
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4

Juškėnas, Robertas. "Triciklių heterosistemų, turinčių pirazolo[3,4-d]pirimidino fragmentą, sintezė. Intramolekulinės pirimidino azoto atomo reakcijos su O,O-acetaliais tyrimas." Doctoral thesis, Lithuanian Academic Libraries Network (LABT), 2014. http://vddb.library.lt/obj/LT-eLABa-0001:E.02~2014~D_20140630_154058-49723.

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Heterociklų chemijos vystymasis turi didelę reikšmę įvairioms mokslo sritims ir pramonės raidai. Pagrindinis šios chemijos srities uždavinys – kurti naujus heterociklinių junginių sintezės metodus, leidžiančius paprasčiau, efektyviau gauti norimos struktūros junginius. Tai apima ne tik heterociklų formavimo būdus, bet ir jų funkcionalizavimą, leidžiantį sukurti įvairiomis cheminėmis ir fizikinėmis savybėmis pasižyminčių junginių įvairovę. Šios mokslo srities pasiekimai pritaikomi biochemijoje, farmacijoje, fotofizikoje ir kitose mokslo ir pramonės šakose. Šiame darbe buvo siekiama sukurti efek
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5

Sūdžius, Jurgis. "Pirimidino junginių - potencialių karboanhidrazių slopuklių - sintezė ir savybės." Doctoral thesis, Lithuanian Academic Libraries Network (LABT), 2011. http://vddb.laba.lt/obj/LT-eLABa-0001:E.02~2011~D_20110519_082321-15451.

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Šio darbo tikslas – pirimidino junginių – potencialių karboanhidrazių (CA) slopiklių –kūrimas. Teoriniai 4-[N-(pirimidin-4-il)]aminobenzensulfonamidų, turinčių pakaitus 2-, 5- ir 6-oje pirimidino žiedo padėtyje, sąveikos su aktyviuoju hCA centru tyrimai parodė, kad šie junginiai gali įsiterpti į aktyvųjį baltymo centrą ir su hCA turėtų sąveikauti kaip tipiški klasikiniai CA slopikliai. Tiksliniai 4-[N-(2,5,6-pakeisti pirimidin-4-il)amino]benzensulfonamidai sintetinti 4,6-dichlorpirimidinuose, 5-oje padėtyje turinčiuose cian-, formil- arba nitrogrupes, chloro atomą keičiant 4-aminobenzensulfona
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6

Scapin, Elisandra. "Pirazolo[1,5-a]pirimidinas: síntese e bromação." Universidade Federal de Santa Maria, 2006. http://repositorio.ufsm.br/handle/1/10375.

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Conselho Nacional de Desenvolvimento Científico e Tecnológico<br>The synthesis of a series of 2-methyl-7-trichloromethylpyrazolo[1,5-a]pyrimidines from the cyclocondensation reaction of 3-amino-5-methylpyrazole with 1,1,1-trichloro-4- alkoxyalk-3-en-2-ones [CCl3C(O)CH=C(R1)OR where R1 = H, Me, Et, Pr, Bu, t-Bu e R = Me, Et] in good yields (69-98%) is reported. Also, was performed the synthesis of 2- methyl-7-arylpyrazolo[1,5-a]pyrimidines from de cyclocondensation reaction of 3-amino-5-methylpyrazole with β-dimethylaminovinyl ketones [R2C(O)CH=CHNMe2, where R= Ph, Ph-4-NO2, Ph-4-Me, Ph-4-Br, P
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7

MONTE, Zenaide Severina do. "Pirimidinas: de potenciais fármacos a marcadores fluorescentes." Universidade Federal de Pernambuco, 2016. https://repositorio.ufpe.br/handle/123456789/19607.

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Submitted by Fabio Sobreira Campos da Costa (fabio.sobreira@ufpe.br) on 2017-07-13T14:09:49Z No. of bitstreams: 2 license_rdf: 811 bytes, checksum: e39d27027a6cc9cb039ad269a5db8e34 (MD5) Zenaide S Monte - Tese Doutorado - Defesa 15-jul-2016.pdf: 10509605 bytes, checksum: 9a625f96607c0ccae6d58b896ba38772 (MD5)<br>Made available in DSpace on 2017-07-13T14:09:49Z (GMT). No. of bitstreams: 2 license_rdf: 811 bytes, checksum: e39d27027a6cc9cb039ad269a5db8e34 (MD5) Zenaide S Monte - Tese Doutorado - Defesa 15-jul-2016.pdf: 10509605 bytes, checksum: 9a625f96607c0ccae6d58b896ba38772 (MD5) Prev
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8

Zanelato, Aurelio Izuka. "Investigação teórica do espalhamento de elétrons pela molécula de Pirimidina (C4H4N2)." Universidade Federal do Amazonas, 2014. http://tede.ufam.edu.br/handle/tede/4814.

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Submitted by Divisão de Documentação/BC Biblioteca Central (ddbc@ufam.edu.br) on 2016-01-26T14:01:02Z No. of bitstreams: 1 Dissertação - Aurelio Izuka Zanelato.pdf: 1806931 bytes, checksum: 4c3ce4091083533c8e83aecb05590538 (MD5)<br>Approved for entry into archive by Divisão de Documentação/BC Biblioteca Central (ddbc@ufam.edu.br) on 2016-01-28T12:40:37Z (GMT) No. of bitstreams: 1 Dissertação - Aurelio Izuka Zanelato.pdf: 1806931 bytes, checksum: 4c3ce4091083533c8e83aecb05590538 (MD5)<br>Approved for entry into archive by Divisão de Documentação/BC Biblioteca Central (ddbc@ufam.edu.br) on 20
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9

Barreto, Igor Ramon Lomba. "Planejamento de derivados 1H-pirazolo[1,5-a]pirimidina com potencial atividade antichagásica." Niterói, 2018. https://app.uff.br/riuff/handle/1/5822.

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Submitted by Biblioteca da Faculdade de Farmácia (bff@ndc.uff.br) on 2018-02-26T14:19:29Z No. of bitstreams: 1 Igor Ramon Lomba Barreto.pdf: 3736181 bytes, checksum: ecfcbc6577d554a095f221827960499b (MD5)<br>Made available in DSpace on 2018-02-26T14:19:29Z (GMT). No. of bitstreams: 1 Igor Ramon Lomba Barreto.pdf: 3736181 bytes, checksum: ecfcbc6577d554a095f221827960499b (MD5)<br>Coordenação de Aperfeiçoamento de Pessoal de Nível Superior<br>A doença de Chagas, causada pelo parasita Trypanosoma cruzi, é uma infecção que possui maior impacto na América Latina, onde a doença é endêmica em vários
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10

Vargas, Pâmela Schütz de. "Reações de β-enaminodicetonas com ncn dinucleófilos: obtenção de pirimidinas e sistemas heterocíclicos fundidos". Universidade Federal de Santa Maria, 2016. http://repositorio.ufsm.br/handle/1/4288.

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Conselho Nacional de Desenvolvimento Científico e Tecnológico<br>In this study the reactivity of β-enamino diketones [RC(O)C(=CHNMe2)C(O)CO2Et, R = C6H5, 4-Me-C6H4, 4-MeO-C6H4, 4-F-C6H4, 4-Br-C6H4, 4-NO2-C6H4, tien-2-il] with NCN bisnucleophiles as amidine and guanidine was investigated. The tiopirimidines ethyl 2-benzylthio-pyrimidine-4-carboxylates, (65-91 %) and Ethyl 2-metiltiopirimidine-4-carboxylates (69-91 %) were obtained in a highly regioselective manner by cyclocondensation reaction of β-enamino diketones with benzylisothiourea hydrochloride and methylisothiourea sulfate, respectivel
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11

Bortolotto, Guilherme Pivotto. "Síntese de 1,2,4-triazol-5-ilamino pirimidinas trifluormetil substituídas." Universidade Federal de Santa Maria, 2009. http://repositorio.ufsm.br/handle/1/10456.

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This work describes the synthesis and characterization of fourteen 4-trifluoromethyl-2-[3-(pyridyl)-1H-1,2,4-triazol-5-ylamino]pyrimidines (6, 7), from the cyclocondensation reaction of N-[3-(pyridyl)-1H-1,2,4-triazol-5-yl]guanidines (4, 5), a 1,3-dinucleophile precursor of the type (N-C-N), with 1,1,1-trifluoro-4-alkoxy-3-alken-2-ones (1), a versatile 1,3-dieletrophile. The 1,1,1-trifluoro-4-alkoxy-3-alken-2-ones (1), of the general formula F3C-C(O)- CH=C(R)-OR1 where R1 = Me, Et and R = H, Me, Ph, 4-FPh, 4-MePh, 4-OMePh, Furyl, were obtained from trifluoroacetylation reactions of enolethers
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12

Frizzo, Clarissa Piccinin. "Estrutura Molecular e Supramolecular de Pirazolo[1,5- a]pirimidinas." Universidade Federal de Santa Maria, 2010. http://repositorio.ufsm.br/handle/1/4195.

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Conselho Nacional de Desenvolvimento Científico e Tecnológico<br>This work describes the molecular and supramolecular structure of fourteen pyrazolo[1,5-a]pyrimidines from bond lengths, torsion angles, angles between planes and interatomic distances. The data discussed were originated from xray and theoretical calculations. Torsion angle N1-N8-C3a-N4, algles between planes of pyrazole and pyrimidine rings and the pyrazolo[1,5-a]pyrimidine RMS value showed that the fused rings are plane. The heterocyclic ring bond lengths demonstrated that the p-electrons are delocalized by resonance and the pe
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13

Peter, da Silva Falcão Emerson. "Novas pirimidinas : : síntese e avaliação de suas propiedades farmacológicas." Universidade Federal de Pernambuco, 2003. https://repositorio.ufpe.br/handle/123456789/1864.

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Made available in DSpace on 2014-06-12T15:52:51Z (GMT). No. of bitstreams: 2 arquivo5061_1.pdf: 6080372 bytes, checksum: a441efc9cf6c4eca97dca5d12fe066c8 (MD5) license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) Previous issue date: 2003<br>Este trabalho descreve a síntese de três séries de compostos contendo o núcleo pirimidínico e sua avaliação farmacológica. Primeiro, foram sintetizados os compostos 4-amino-2,6-(diarildissubistituídos)- 5-carbonitrila-pirimidínicos (5a-h), a partir de intermediários arilamidínicos e bisnitrílicos. Segundo, foram reduzidos os nitro
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14

Santos, Barbara Helen Cortat. "Papel biológico dos dímeros de pirimidina em células humanas irradiadas com radiação UVA." Universidade de São Paulo, 2010. http://www.teses.usp.br/teses/disponiveis/41/41131/tde-07122010-101150/.

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A radiação ultravioleta (UV) pode ser absorvida por diferentes moléculas celulares, incluindo o DNA no qual provoca distorções estruturais. As lesões mais comuns induzidas pela radiação UV são o ciclobutano de pirimidina (CPD) e o fotoproduto (6-4)-pirimidina-pirimidona [(6-4)PPs]. Estas lesões podem ser reparadas pela fotorreativação, caracterizada por ter uma única proteína (fotoliase) que remove lesões empregando luz visível (320-500 nm) como fonte de energia. Foram identificados dois tipos de fotoliases que diferem por sua especificidade ao substrato: CPD-fotoliase e (6-4)-fotoliase. Um ou
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15

Barbosa, Sara Isabel Cadinha. "Compostos que interferem no metabolismo dos purina- e pirimidina-nucleótidos: utilização como agentes terapêuticos." Master's thesis, [s.n.], 2015. http://hdl.handle.net/10284/5160.

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Projeto de Pós-Graduação/Dissertação apresentado à Universidade Fernando Pessoa como parte dos requisitos para obtenção do grau de Mestre em Ciências Farmacêuticas<br>O conteúdo deste trabalho será desenvolvido em dois temas principais, um referente à utilização de compostos que interferem no metabolismo dos purina- e pirimidinanucleótidos como agentes antineoplásicos e outro referente à sua utilização como agentes antivirais. A síntese dos nucleótidos envolve a construção de ácidos nucleicos e a inserção dos derivados de nucleótidos noutras vias bioquímicas, sendo responsável por inúmera
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16

Galve, Murillo Iñaki. "Síntesis de pirido[2,3-d]pirimidin-7(8H)-onas 2-arilamino sustituidas y derivados." Doctoral thesis, Universitat Ramon Llull, 2013. http://hdl.handle.net/10803/101403.

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Les Cinases de Proteïna (PKs) estan implicades en processos fonamentals de la regulació del cicle cel•lular. L’acumulació d’anomalies als mecanismes de control i el comportament disfuncional que se’n deriva han estat detectats a cèl•lules de diferents teixits afectades per càncer, desordres immunològics, endocrins, nerviosos, neurodegenaratius, cardiovasculars, malalties infeccioses, diabetis, Alzheimer, asma, restenosi, arteriosclerosi, leucèmia, artritis, etc. Però d’entre totes les PKs, les Cinases de Tirosina (TKs) han estat destacades com a l’element central de tots aquests processos i, p
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17

Tier, Aniele Zolin. "Efeito da Topologia Molecular no Empacotamento Cristalino de Pirazolo[1,5-a]pirimidinas." Universidade Federal de Santa Maria, 2013. http://repositorio.ufsm.br/handle/1/10550.

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Conselho Nacional de Desenvolvimento Científico e Tecnológico<br>This study shows the influence of the molecular topology of the crystal of a series of 14 pyrazolo[1,5-a]pyrimidines. The topological data were obtained from X-ray diffraction data and energy stabilization were determined by thermal analysis and chemical computations. Topological analysis carried out was Molecular Coordination Number (NCM) using the Voronoi-Dirichlet polyhedra and Hirshfeld surface. The NCM found for the majority of compounds was 14. Furthermore, it was determined contact area and the solid angle between molecule
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VITAL, Fernando Antonio Chaves. "Novas 5-oxo Tiazolidino Pirimidinas: síntese e avaliação de suas atividades biológicas." Universidade Federal de Pernambuco, 2009. https://repositorio.ufpe.br/handle/123456789/1557.

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Made available in DSpace on 2014-06-12T15:51:09Z (GMT). No. of bitstreams: 2 arquivo1560_1.pdf: 1445052 bytes, checksum: 334f3bd99a8b1e3c11b2c9898b77c3a5 (MD5) license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) Previous issue date: 2009<br>Coordenação de Aperfeiçoamento de Pessoal de Nível Superior<br>As pirimidinonas são compostos heterocíclicos de seis membros com dois átomos de nitrogênio nas posições 1 e 3, e com ao menos uma carbonila ligada ao heterociclo. Esses compostos são amplamente conhecidos pelo seu vasto espectro de atividades farmacológicas, como a
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CARVALHO, Maíra de Almeida. "Aplicações de metodologias teóricas em estudos de QSAR-3D de Pirimidinas substituídas." Universidade Federal de Pernambuco, 2004. https://repositorio.ufpe.br/handle/123456789/8915.

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Made available in DSpace on 2014-06-12T23:03:15Z (GMT). No. of bitstreams: 2 arquivo9298_1.pdf: 10896298 bytes, checksum: 57929e1373c32b8a62e0afb56b85d2af (MD5) license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) Previous issue date: 2004<br>Este trabalho tem em vista um estudo sistemático para a determinação de um modelo QSAR-3D para uma série homóloga de pirimidinas substituídas, cujas atividades anti-inflamatórias são conhecidas. Estudos preliminares de QSAR clássica, incluindo parâmetros calculados pelo método AM1, mostraram a importância de parâmetros eletrônico
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Brondani, Patrícia Bulegon. "Estudo de reações de N-alquilação de pirimidin-2-onas: síntese de novos análogos nucleosídicos modificados." Universidade Federal de Santa Maria, 2008. http://repositorio.ufsm.br/handle/1/10402.

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This work presents a study of the N-alkylation reactions of 4- (trichloromethyl)pyrimidin-2(1H)-one(2), 5-bromo-4-methoxy-4-(trichloromethyl)-3,4-dihydropyrimidin-2-(1H)-one (7), 4-methoxy-4-(trichloromethyl)-3,4-dihydropyrimidin-2(1H)-one (6), cytosine (1), 3-benzoylpyrimidine-2,4(1H,3H)-dione (or 3-benzoyl-uracil) (10), 3-benzoyl-5-methylpyrimidine-2,4(1H,3H)-dione (or 3-benzoyl-thymine) (11). The pyrimidines were tested with the alkylating agents chloro-acetamide (3a) and diethyl 2-bromomalonate (3b) in the presence of polar solvents (acetone, DMF, THF) and base (K2CO3 e NaH). The pyrimidin
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OLIVEIRA, Janice Vasconcelos. "Desenvolvimento de lipossomas contendo composto 2-fenil-4-amino-6-p-fluorfenil-5-carbonitrila-pirimidina e avaliação de seu potencial antitumoral." Universidade Federal de Pernambuco, 2013. https://repositorio.ufpe.br/handle/123456789/10564.

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Submitted by Nayara Passos (nayara.passos@ufpe.br) on 2015-03-05T12:13:54Z No. of bitstreams: 2 DISSERTAÇÃO JANICE Oliveira.pdf: 1136330 bytes, checksum: a8f4e5393ba47301910ecc5f7919fcdd (MD5) license_rdf: 1232 bytes, checksum: 66e71c371cc565284e70f40736c94386 (MD5)<br>Made available in DSpace on 2015-03-05T12:13:54Z (GMT). No. of bitstreams: 2 DISSERTAÇÃO JANICE Oliveira.pdf: 1136330 bytes, checksum: a8f4e5393ba47301910ecc5f7919fcdd (MD5) license_rdf: 1232 bytes, checksum: 66e71c371cc565284e70f40736c94386 (MD5) Previous issue date: 2013<br>CAPES<br>O aumento na incidência de neoplasia
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Patoilo, Diana Torrão. "Síntese e transformações de Diels-Alder de 2-estirilcromonas: síntese de flavonas contendo unidades do ripo pirimidina." Doctoral thesis, Universidade de Aveiro, 2005. http://hdl.handle.net/10773/4980.

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Doutoramento em Química<br>Na primeira parte desta dissertação reporta-se a síntese de 2-estirilcromonas, 5-hidroxi-2-estirilcromonas e benziloxi-2-estirilcromonas; e de precursores de dienos do tipo o-quinodimetanos, 2,2-dióxido de 1,3-di-hidrobenzo[c]tiofeno, 2,2-dióxido de 4,7-dimetoxi-1,3-di-hidrobenzo[c]tiofeno e 6,6-dióxido de 2- metil-4-metoxi-5,7-di-hidrotieno[3,4-d]pirimidina. Na segunda parte desta dissertação reportam-se os estudos de reacções de Diels-Alder de 2-estirilcromonas com dienos gerados “in-situ”, por extrusão térmica de dióxido de enxofre, a partir de sulfonas, am
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Jaime, Bezerra Mendonça Junior Francisco. "Síntese e avaliação da atividade antimicrobiana de novas 3,4-dihidro-2,6-diaril-4-oxo-pirimidina-5-carbonitrilas." Universidade Federal de Pernambuco, 2003. https://repositorio.ufpe.br/handle/123456789/3396.

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Made available in DSpace on 2014-06-12T16:30:46Z (GMT). No. of bitstreams: 2 arquivo5766_1.pdf: 286300 bytes, checksum: 342a5be7fb21363269f7df5a812925e0 (MD5) license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) Previous issue date: 2003<br>Compostos heterocíclicos do tipo pirimidinona são reconhecidos na terapêutica pela enorme riqueza de seu potencial farmacológico. Diversas atividades como: antiviral, antitumoral, antiinflamatórias, anticonvulsivantes, indutoras de interferon, antihistamínicas, antibióticas e herbicidas, entre outras, são extensamente relatadas na
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Dal, Pizzol Carine. "Desenvolvimento de nanopartícula lipídica sólida contendo um análogo de pirimidina e avaliação in vitro da atividade antitumoral." reponame:Repositório Institucional da UFSC, 2014. https://repositorio.ufsc.br/xmlui/handle/123456789/128894.

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Tese (doutorado) - Universidade Federal de Santa Catarina, Centro de Ciências da Saúde, Programa de Pós-Graduação em Farmácia, Florianópolis, 2014<br>Made available in DSpace on 2015-02-05T20:27:46Z (GMT). No. of bitstreams: 1 331123.pdf: 8939835 bytes, checksum: c99e68a52a7441188881d0e1802660a8 (MD5) Previous issue date: 2014<br>Esta tese está sendo apresentada em quatro etapas. A primeira foi avaliar doze moléculas de análogos de pirimidina, quanto ao aspecto de citotoxicidade e tipo de morte celular em três linhagens celulares tumorais (L1210, B16F10 e CEM). Quatro moléculas apresentaram
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UBERTINI, FULVIA. "Pirimidina 5'-nucleotidasi umana, p5N-1: evidenze della formazione di un intermedio fosforilato e mutagenesi sito-diretta." Doctoral thesis, Università Politecnica delle Marche, 2008. http://hdl.handle.net/11566/242603.

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Renata, Leite Monteiro Maria. "6-Aril-Pirimidinas contendo uma função imida : síntese e avaliação das propriedades antimicrobianas." Universidade Federal de Pernambuco, 2005. https://repositorio.ufpe.br/handle/123456789/1614.

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Made available in DSpace on 2014-06-12T15:51:28Z (GMT). No. of bitstreams: 2 arquivo4494_1.pdf: 2968685 bytes, checksum: 78b451af69b3432d863083edc34c0dee (MD5) license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) Previous issue date: 2005<br>Os derivados pirimidínicos vêm ganhando destaque devido à sua grande importância biológica. Atividades antitumoral, antiinflamatória, antimicrobiana, anticonvulsivante, anti-hipertensiva, entre outras são atribuídas ao heterociclo da pirimidina. Por outro lado, compostos contendo a função imida vem ganhando grande importância dad
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Campos, Luana Janaína de. "Estudos QSAR de derivados de pirimidonas, pirimidinas e piridopirazinas carboxamidas inibidoras da HIV 1 integrase." Universidade Estadual do Oeste do Parana, 2015. http://tede.unioeste.br:8080/tede/handle/tede/8.

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Made available in DSpace on 2017-05-12T14:36:24Z (GMT). No. of bitstreams: 1 DISSERTAcaO_ Final.pdf: 7044304 bytes, checksum: 2c043ef6d78e2a532d7a87d8a9b74434 (MD5) Previous issue date: 2015-12-04<br>The computer-aided drug design field have attracted attention with regard to the discovery of new antiretroviral for use in AIDS pharmacotherapy. Thus, the aim of this study was to develop mathematical models that can predict the anti HIV1-IN activity of analogues not synthesized from pyrimidones, pyrimidines and pyridopyrazine carboxamides, reducing the time to obtain new prototypes of drugs. T
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28

Miret, Casals Laia. "Small molecules for modulating biological targets." Doctoral thesis, Universitat de Barcelona, 2014. http://hdl.handle.net/10803/279548.

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CHAPTER 1: Respiratory Infectious Diseases (RID) are diseases affecting the air passages, the bronchi and the lungs. They range from acute infections, such as pneumonia and bronchitis, to chronic conditions such as asthma, cystic fibrosis and chronic obstructive pulmonary disease. Respiratory lung infections are leading causes of morbidity and mortality worldwide with a considerable human, social and financial burden. RID can be caused by an increasing number of multi resistant bacteria to the existing antibiotics. Bacteria, which normally inhabit the mucus, grow out of control and con
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29

Rosa, Wilian Carvalho da. "Síntese de espiro[cromeno[4,3-d]pirimidinas-5,1 -cicloalcano] e 5,6-diidrobenzo[h]quinazolinas trifluormetil substituídas." Universidade Federal de Santa Maria, 2016. http://repositorio.ufsm.br/handle/1/10616.

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Conselho Nacional de Desenvolvimento Científico e Tecnológico<br>The present dissertation initially describes new methods for the synthesis of 4-(trifluoromethyl)-5,6-dihydrobenzo[h]quinazolines and 4-(trifluoromethyl)spiro[chromeno[4,3-d]pyrimidines-5,1'-cycloalkane], as new trifluoromethyl substituted heterocyclic systems. Cyclocondensation reactions type [3 + 3] involving 2,2,2-trifluoro-1-(1-methoxy-3,4-dihydronaphthalen-2-yl)ethanone and five amidines [NH2-(C=NH)R] conducted to the synthesis of a new series of five examples of 2-substituted 4-(trifluoromethyl)-5,6-dihydrobenzo[h]quinazoli
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30

Rosa, Fernanda Andreia. "Acilenaminonas: Síntese e Aplicação na Obtenção de Pirazóis, Pirazolo[3,4-d]piridazinonas e Pirazolo[1,5-a]pirimidinas." Universidade Federal de Santa Maria, 2009. http://repositorio.ufsm.br/handle/1/4174.

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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior<br>The regioespecific synthesis of a series of 14 N-acylated enaminones (52-88%) from the acylation reaction of secondary β-enamino ketones [RC(O)CH=CHNR1R2; R = Ph, 4- FC6H4, 4-NO2C6H4, thien-2-yl, CCl3, CF3; R1 = H; R2 = Bn, Ph, 4-NO2C6H4] with trifluoroacetic anhydride or ethyl oxalyl chloride in pyridine is reported. On the other hand, when tertiary enaminone precursors [R = Ph, 4-MeC6H4, 4-MeOC6H4, 4-BrC6H4, 4-ClC6H4, 4-FC6H4, 4-O2NC6H4, thien-2-yl, benzofur-2-yl, CCl3, CF3; R1,R2 = Me] were used, the acylation reaction led to a
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31

Fortes, Andressa Silveira. "Síntese de 2-Benzil(metil)tio-6-aril(metil)pirimidinas-4-carboxilato de Etila e seus Ácidos Derivados." Universidade Federal de Santa Maria, 2012. http://repositorio.ufsm.br/handle/1/10522.

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Conselho Nacional de Desenvolvimento Científico e Tecnológico<br>This work presents a simple and versatile synthetic strategy for the preparation of a novel series of Ethyl 2-Benzyl(methyl)tiopyrimidines-4-carboxylate 6-substituted and their acids derivatives. The Ethyl 2-Benzyl(methyl)tiopyrimidines-4-carboxylate 6-substituted were obtained from the reaction of 2-Benzyl(methyl)isothiourea with Ethyl 4-Aryl(methyl)-4-methoxy-2-oxo-3-butenoates (where Ar= Ph, 4-FC6H4, 4-BrC6H4, 4-MeC6H4, 4-MeOC6H4 and 4-NO2C6H4), in the presence of sodium carbonate in ethanol and water to produce the correspond
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32

Marzari, Mara Regina Bonini. "Síntese de pirazolo[1,5-a]pirimidinas e fluorfenilpirazóis trifluormetilados em ultrassom e síntese e aplicação de [2]rotaxanos." Universidade Federal de Santa Maria, 2014. http://repositorio.ufsm.br/handle/1/4287.

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Conselho Nacional de Desenvolvimento Científico e Tecnológico<br>This work presents the synthesis of three series of trifluoromethylated heterocycles by using ultrasound irradiation, nomely pyrazolo[1,5-a]pyrimidines, 2,4- difluorophenylpyrazoles and pentafluorophenylpyrazoles. The reactions were performed between trifluoromethylated enones ([CF3C(O)CH=C(R)(OMe], where R = Me, Bu, i-Bu, Ph, 4-MeC6H4, 4-FC6H4, 4-ClC6H4, 4-BrC6H4, 4-IC6H4, thien-2-yl, naphthyl and biphenyl) with three different nucleophiles, nomely (3)(5)-amine-(5)(3)- methylpyrazole, 2,4-difluorophenylhydrazine hydrochloride an
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33

Malavolta, Juliana Limana. "Síntese de Pirimidinas derivadas de 7,7,7-trialo-4-metoxi-6-oxo-4- heptenoatos de metila e bi-heterociclos trifluormetilados." Universidade Federal de Santa Maria, 2012. http://repositorio.ufsm.br/handle/1/10501.

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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior<br>An efficient method to obtain pyrimidinones and pyrimidines trialomethylated from the cyclocondensation reaction of compounds of methyl 7,7,7-trihalo-4-methoxy-6-oxoheptenoate with urea and differents amidines providing the series of compounds pyrimidines and pyrimidinones trifluoromethylated and trichloromerthylated is reported.Some compounds of the series were selected and brought to reaction with hydrazine monohydrate obtaining the series of new 6-(trifluoromethyl)pyrimidin-4-propanehydrazide, of which two were later brought to
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34

Pizzuti, Lucas. "Síntese de 4-(fur-2-il)- e 4-(tien-2-il)-pirimidinas a partir de β-Alcoxivinil trifluormetil cetonas". Universidade Federal de Santa Maria, 2005. http://repositorio.ufsm.br/handle/1/10401.

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Conselho Nacional de Desenvolvimento Científico e Tecnológico<br>The cyclocondensation of the 1,1,1-trifluoro-4-methoxy-4-(2-heteroaryl)-3-buten-2-ones (heteroaryl = furyl and thienyl) with urea and amidines (acetamidine, benzamidine, guanidine, 1H-pyrazole-1-carboxamidine and 2-methyl-2-thiopseudourea) for synthesis of two 4-(2-heteroaryl)-6-trifluoromethylpyrimidinones and a series of ten 4-(2-heteroaryl)-6-trifluoromethylpyrimidines is reported. The reaction of the 1,1,1-trifluoro-4-methoxy-4-(2-heteroaryl)-3-buten-2-ones with urea was carried out in the presence of boron trifluoride ethera
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35

Silva, Andreia Medianeira Pedrolo Weber da. "Síntese regiosseletiva de 4-trifluormetil-2-(metiltio)-3,4-diidropirimidin-4-óis 3,6-dissubstituídos com efeito inibitório enzimático." Universidade Federal de Santa Maria, 2012. http://repositorio.ufsm.br/handle/1/10536.

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Conselho Nacional de Desenvolvimento Científico e Tecnológico<br>This work reports a simple and versatile new strategy for the regiosselective synthesis of N3-substituted 6-alkyl(aryl or heteroaryl)-4-trifluoromethyl-2-(methylthio)-3,4-dihydropyrimidin-4-ols, which enabled to establish the regiochemistry of the cyclocondensation reaction between trifluoromethylated enones and N-substituted 2-methylisothioureas. The N3-substituted 6-alkyl(aryl or heteroaryl)-4-trifluoromethyl-2-(methylthio)-3,4-dihydropyrimidin-4-ols were obtained from the cyclocondensation reaction of 4-alkoxy-1,1,1-trifluorom
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36

Sūdžius, Jurgis. "Synthesis And Properties Of Pyrimidine Derivatives – Potent Carbonic Anhydrase Inhibitors." Doctoral thesis, Lithuanian Academic Libraries Network (LABT), 2011. http://vddb.laba.lt/obj/LT-eLABa-0001:E.02~2011~D_20110519_082332-05105.

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The aim of the work was design of pyrimidine derivatives – potent carbonic anhydrase (CA) inhibitors. Theoretical investigation of interaction of 4-[N-(pyrimidin-4-yl)]aminobenzenesulfonamides containing substituents at 2-, 5- and 6- positions of pyrimidine ring with an active site of hCAs suggested that these compounds can fit into an active site of the enzymes and should interact with them as typical hCA inhibitors. Synthesis of target compounds was carried out by substitution of chloro group at 4,6-dichloropyrimidines containing cyano-, formyl- or nitro groups at position 5 of the pyrimidin
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37

Azevedo, Ana Carolina de Almeida [UNIFESP]. "Avaliação do perfil de susceptibilidade a fluconazol e voriconazol frente a isolados de Candida spp. pelo método de disco-difusão." Universidade Federal de São Paulo (UNIFESP), 2005. http://repositorio.unifesp.br/handle/11600/9094.

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Made available in DSpace on 2015-07-22T20:49:35Z (GMT). No. of bitstreams: 0 Previous issue date: 2005-01-01<br>Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)<br>Introdução: Em 2004, o NCCLS padronizou a técnica de disco-difusão para ensaios com fluconazol. Este teste permite a análise de grande número de amostras com custo reduzido, resultado rápido e de fácil interpretação, não exigindo equipamento especial, sendo assim de grande utilidade em estudos de vigilância de resistência a fluconazol e voriconazol. Objetivos: 1) Avaliar a distribuição de espécies de Candida id
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38

Obregon, Adriana Dornelles Carpes. "3-alcoxi-4-hidroxi pirrolidin-2-onas, 2-metilsulfanil pirimidina, enoilcarbamatos e 3-dialcoxi fosforiloxi trialometilados: síntese e potencial inibitório sobre a atividade da enzima acetilcolinesterase." Universidade Federal de Santa Maria, 2006. http://repositorio.ufsm.br/handle/1/4239.

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This work presents a study of the several organic compounds such as trihalomethylated enaminones, γ-amino alcohols, oxazinones, oxazines, dihydrofuranones, pyrrolidin-2-ones, 2-methylsulfanyl pyrimidine, enoylcarbamates and 3-dialkoxy phosphoryloxy on the acetylcholinesterase enzyme activity. Also, this work shows the effect per se of organic solvents on the AChE of different cerebral structures of rats. The N- and N-O-alkylated 3-alkoxy-5-hydroxy-trifluormethyl-pyrrolidin-2-ones and trifluoromethylated enoylcarbamates showed in vitro inhibitory effect of the AChE activity in the striatum cere
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39

Aquino, Estefania da Costa. "Aplicação de 5-bromo-1,1,1-trifluor-4-metoxipent-3-en-2-ona na síntese de pirróis, pirazóis, pirimidinas e 1,2,3-triazóis." Universidade Federal de Santa Maria, 2015. http://repositorio.ufsm.br/handle/1/4275.

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Conselho Nacional de Desenvolvimento Científico e Tecnológico<br>This thesis reports the synthesis of various series of trifluoromethyl substituted nitrogenated heterocycles, such as pyrroles, pyrazoles, pyrimidines and 1,2,3-triazoles, exploiting the synthetic versatility of 5-bromo-1,1,1-trifluoro-4-methoxypent-3-en-2-one in reactions with nitrogenated nucleophiles. In this way, synthesis of a novel series of 4-amino-3-trifluoromethyl-1H-N-substituted pyrroles was performed through two reaction steps. In the first stage is an addition reaction of primary or secondary amine in the 4-position
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40

Berzosa, Rodríguez Xavier. "Diseño y síntesis de una quimioteca de sistemas 5,6-dihidropirido[2,3-d]pirimidin-7(8H)-ona no sustituidos en C4 como inhibidores potenciales de tirosina quinasas." Doctoral thesis, Universitat Ramon Llull, 2010. http://hdl.handle.net/10803/9299.

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Les Tirosina Cinases (TKs) són un grup de Proteïna Cinases claus en la senyalització cel·lular. Aquestes Cinases estan implicades, entre d'altres, en processos de creixement tumoral, fet que fa que la recerca d'inhibidors de TKs sigui una àrea d'investigació molt important en química mèdica.<br/>En aquest context es desenvolupa el present treball en el qual es pretenen sintetitzar inhibidors potencials de Tirosina Cinases amb estructura 4-hidrogenpirido[2,3-d]pirimidínica. Molècules amb aquesta estructura han presentat elevada activitat com inhibidors de TKs pel que en primer lloc s'aborda la
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41

Canelli, Tommaso. "Development of tandem C-H borylation/functionalization procedures for late stage functionalization of compounds." Master's thesis, Alma Mater Studiorum - Università di Bologna, 2015. http://amslaurea.unibo.it/9273/.

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The development of procedures for the iridium catalyzed C-H borylation of 1-aryl pyrazolopyrimidines and 1-aryl indazoles is reported. Investigation on the activity of the catalyst revealed the combination of an iridium (I) precursor and tetramethylphenantroline as the best catalytic system. Moreover, the procedures are regioselective resulting in the selective borylation of different C-H bonds within the substrates. The application of C-H borylation to late stage functionalization is demonstrated: a biologically active compound in AstraZeneca's project underwent tandem borylation/oxidation re
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42

Calheiro, Tainara Paulus. "(Benzo[d]azolil)guanidinas: reações de ciclocondensação com trifluoracetil enol éteres na síntese de N-(pirimidinil)-1H-(benzo[d]azolil)aminas e N-derivados." Universidade Federal de Santa Maria, 2014. http://repositorio.ufsm.br/handle/1/10590.

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Conselho Nacional de Desenvolvimento Científico e Tecnológico<br>The present research describes a simple and efficient procedure to synthesize a novel series of twenty N-(pyrimidinyl)-1H-(benzo[d]azolyl)amines, from the cyclocondensation reaction of (benzo[d]azolyl)guanidines with 4-alkoxy-4-alkyl(aryl/heteroaryl)-1,1,1-trifluoroalk-3-en-2-ones and 2,2,2-trifluor-1-(2-methoxycyclohexen-1-en-1-yl)ethanone. The (benzo[d]azolyl)guanidines precursors were further obtained from reactions of cyanoguanidine with o-phenylenediamine or 2-aminothiophenol and the trifluoromethylated vinyl ketones from tr
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43

Albertí, Aguiló Francisca M. "Complejos con ligandos derivados de purinas y pirimidinas N-sustituidas e iones metálicos de transición: Contribución a la Química Bioinorgánica y a la Arquitectura Molecular." Doctoral thesis, Universitat de les Illes Balears, 2009. http://hdl.handle.net/10803/9459.

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El principal objetivo de la Tesis ha consistido en la síntesis y caracterización de ligandos derivados de purinas y pirimidinas N-sustituidas y el posterior estudio de su química de coordinación con iones metálicos de transición. Los resultados obtenidos pueden dividirse en tres apartados. En el primero se aborda la síntesis y caracterización de poli(2-pirimidil)poliazaalcanos y sus respectivos complejos de Ag(I), estudiando todas las estructuras cristalinas obtenidas por difracción de rayos X. El segundo bloque ha consistido en la preparación de adeninas N6-sustituidas y el posterior estudio
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44

Martins, Demétrius Bernardes. "Síntese de 2-[3h-pirazol-2-il]trifluormetilpirimidinas Alquil, aril e heteroaril substituidas." Universidade Federal de Santa Maria, 2004. http://repositorio.ufsm.br/handle/1/10391.

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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior<br>This work describes a general methodology for the synthesis of a novel series of 4-alkyl, 4-aryl, heteroaryl-2-[5-methyl-4-(2-hidroxyethyl)-3-oxo-1,2-dihydro-3H-pyrazol-2-yl]-6(4)-trifluoromethylpyrimidines. The precursors β-alkoxyvinyl trihalomethyl ketones of the general formula, F3C-C(O)-C(R2)=C(R)OR1, where R= H, CH3, i-Pr, Ph, 4-OCH3Ph, 2-C4H3O, 2-C4H3S, R1= CH3, C2H5 and R2 = H, CH3, R-R2= -(CH2)3-, were obtained from trifluoroacetylation reactions of enoleters and acetals derived from alkyl, cicloalkyl, methyl Ketones and 4-
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45

Cabeza, Brasa María del Carmen. "Implicación de los polimorfismos de las enzimas del metabolismo de las pirimidinas en los trastornos metabólicos y morfológicos asociados a la infección por VIH-1 y al targa." Doctoral thesis, Universitat Autònoma de Barcelona, 2013. http://hdl.handle.net/10803/129130.

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ANTECEDENTES: Desde la introducción de los primeros fármacos antirretrovirales inhibidores de la transcriptasa inversa análogos timidínicos de los nucleótidos (ITINs) como AZT y d4T, el mayor problema ha sido tratar de evitar el desarrollo de efectos secundarios como los asociados a la toxicidad mitocondrial (lipodistrofia, neuropatía periférica o pancreatitis) HIPÓTESIS: Los polimorfismos de las enzimas de la vía de las pirimidinas, como la Timidilato Sintasa (TS), que se asocian con menor actividad enzimática, se relacionan a su vez con mayores concentraciones intracelulares de fármacos y p
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46

Fiss, Gabriela Fehn. "Síntese de heterociclos via reações de ciclocondensação de a-etiloxalil e -pirazolil(alquil) b-dimetilaminoenonas com1,2- OU 1,3-Dinucleófilos." Universidade Federal de Santa Maria, 2009. http://repositorio.ufsm.br/handle/1/4175.

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Conselho Nacional de Desenvolvimento Científico e Tecnológico<br>Chemoselective synthesis of ethyl 4-pirimidinecarboxylates and/or ethyl 5-pirimidineoxalates via cyclocondensation reaction of b-dimethylaminoenones [R1C(=O)C(=CNMe2)C(=O)CO2Et, where R1 = Ph, 4-MeC6H4, 4-MeOC6H4, 4-BrC6H4, 4-ClC6H4, 4-FC6H4, 4-O2NC6H4, 2-thienyl, benzo[b]furan-2-yl and CF3] with NCN 1,3- dinucleophiles such as benzamidine hydrochloride or 1H-1-pyrazolyl-carboxamidine hydrochloride (50-86%); utilization of ethyl 4-pirimidinecarboxylates (when R1 = Ph, 4-MeOC6H4, 4-FC6H4 and 2-thienyl) in the cyclization reaction
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47

Frigo, Leandro Marcon. "Obtenção de novos heterociclos derivados do ácido levulínico." Universidade Federal de Santa Maria, 2013. http://repositorio.ufsm.br/handle/1/4263.

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Conselho Nacional de Desenvolvimento Científico e Tecnológico<br>This study describes the attainment of twenty three (23) bis-heterocycles derived from the Levulinic Acid: Bis-Pyrazoles (6a-k) by the reaction of cyclecondensation between the 3-(5-(trifluoromethyl)-4,5-dihydro-1H-pyrazol-3-il)propanohidrazidamand a series of replaced β-alcoxiviniltrifluorometilcetonas. 1,3,4-oxadiazole 2-5-disubstituted (8-11) by reactions like [4 + 1] [OCNN+C], through the reactions of cyclecondensation between the 3-(5-(trifluoromethyl)-4,5-dihydro-1H-pyrazol-3-yl)propanohidrazida with different orthoesters a
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48

Juškėnas, Robertas. "Synthesis of tricyclic heterosystems based on pyrazolo[3,4-d]pyrimidine framework. Study of intramolecular reaction of pyrimidine nitrogen atom with O,O-acetals." Doctoral thesis, Lithuanian Academic Libraries Network (LABT), 2014. http://vddb.library.lt/obj/LT-eLABa-0001:E.02~2014~D_20140630_154044-28576.

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The development of heterocyclic chemistry is important for various science areas and for the industry. The main task of this branch of chemistry is the search for the new, more effective synthetic methods for obtaining heterocyclic derivatives. That covers not only the formation of heterocycles, but also their functionalization, which leads to the creation of compounds having various chemical and physical properties. The accomplishments of this area are applied in biochemistry, pharmacochemistry, photophysics and other branches of science and industry. The creation of effective heterocycles sy
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49

Moresco, Rafael Noal. "Associação entre os níveis de D-dímero, produtos de degradação da fibrina/fibrinogênio (PDF) e troponina cardíaca T na investigação dos distúrbios tromboembólicos." reponame:Biblioteca Digital de Teses e Dissertações da UFRGS, 2005. http://hdl.handle.net/10183/5216.

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Armelin, Paulo Roberto Gabbai. "Modelagem molecular de derivados pirimidínicos e estudos de docking nas enzimas ciclooxigenase 1 e ciclooxigenase 2." Universidade Federal de São Carlos, 2010. https://repositorio.ufscar.br/handle/ufscar/6975.

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Made available in DSpace on 2016-08-17T18:39:37Z (GMT). No. of bitstreams: 1 3649.pdf: 6160139 bytes, checksum: e2fc962eefef9b03fa83e0311a505531 (MD5) Previous issue date: 2010-11-23<br>Financiadora de Estudos e Projetos<br>In this research molecular docking was used to study enzime-ligand complexes of Cyclooxygenase 1 (COX-1) and Cyclooxygenase 2 (COX-2) with pyrimidine derivatives, aiming at understanding the possible mechanisms of action of these compounds and, thus, suggest modifications that could increase their specificity. The chosen ligands were a series of 25 substituted pyrimidines
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