Molecular features of the prazosin molecule required for activation of Transport-P

Silva, Joaquim Fernando Mendes da; Walters, Marcus; Al-Damluji, Saad; Ganellin, C. Robin

doi:10.1016/j.bmc.2008.06.037

Cited by 71 publications

(34 citation statements)

References 19 publications

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“…[1][2][3] These structures have been conventionally prepared by the Bischler cyclization between dicarbonyls and diamines. [1][2][3] These structures have been conventionally prepared by the Bischler cyclization between dicarbonyls and diamines.…”

Section: Introductionmentioning

confidence: 99%

Expanding applications of zeolite imidazolate frameworks in catalysis: synthesis of quinazolines using ZIF-67 as an efficient heterogeneous catalyst

et al. 2015

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A cobalt zeolite imidazolate framework (ZIF-67) was successfully synthesized and characterized by several techniques. The ZIF-67 was used as an efficient heterogeneous catalyst for the cyclization reaction of 2aminobenzoketones and benzylamine derivatives to form quinazoline products. The optimal conditions involved the use of TBHP oxidant in toluene solvent at 80 C. Remarkably, the ZIF-67 catalyst exhibited better performance in the cyclization reaction than common cobalt salts such as Co(NO 3 ) 2 , CoCl 2 , and Co(OAc) 2 and other Co-MOFs such as ZIF-9, Co-MOF-74, and Co 2 (BDC) 2 (DABCO). In addition, the cyclization reaction could only proceed in the presence of the solid Co-ZIF catalyst and there was no contribution from leached active sites present in the solution. The catalyst could be recovered and reused several times without a significant degradation in catalytic activity.

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Section: Introductionmentioning

confidence: 99%

Expanding applications of zeolite imidazolate frameworks in catalysis: synthesis of quinazolines using ZIF-67 as an efficient heterogeneous catalyst

et al. 2015

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“…Os primeiros resultados deste projeto conjunto foram publicados recentemente. 15 Um dos principais parâmetros de interação da prazosina e seus derivados com o receptor α 1 -adrenérgico é a basicidade do anel heterocíclico, uma vez que a forma protonada é a que efetivamente se liga ao receptor. Por outro lado, dados de relação estrutura-atividade obtidos pelo Prof. Ganellin sugerem que o anel benzênico não é fundamental para a capacidade de ligação ao Transporte P. Assim, pretendemos sintetizar e avaliar a atividade de piridinas 2,4,6-trissubstituídas, derivadas da 4-dimetilaminopiridina, que devem apresentar os maiores valores de pK a entre todos os análogos de prazosina já sintetizados.…”

Section: • Ligação De Grupamentos Alquila Ou Arila Em N-4;unclassified

The Medicinal Chemistry at the “Polo de Xistoquímica” of the IQ‐UFRJ

Silva¹,

Gonçalves²,

Estrada³

et al. 2009

Revista Virtual De Química

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Abstract:The Medicinal Chemistry laboratory of the "Polo de Xistoquímica" of the IQ-UFRJ has been developing projects in the area of Medicinal Chemistry for seven years, conducting research on new anti-hypertensive, antidepressant, antibiotic and antiviral agents. In the last five years, a doctor and six masters in science developed their works in this laboratory, and at this moment, four undergraduate and a master student are working there. Fourteen scientific articles were published in the last five years and two patents are in the process of filing.Keywords: medicinal chemistry, anti-hypertensive, antidepressant, transport P ResumoO laboratório de Química Medicinal do Polo de Xistoquímica do IQ-UFRJ vem desenvolvendo projetos na área de Química Medicinal há sete anos, realizando pesquisas acerca de novos agentes anti-hipertensivos, antidepressivos, antimicrobianos e antivirais. Nos últimos cinco anos, formamos um doutor e seis mestres em ciências, e contamos, no momento, com quatro doutorandos e um mestrando. Foram publicados 14 artigos científicos nos últimos cinco anos e duas patentes estão em processo de depósito. palavras-chave: química medicinal, anti-hipertensivos, antidepressivos, transporte P Joaquim Fernando Mendes da Silva cursou graduação em Farmácia na UFRJ e obteve seu doutoramento em Química Orgânica no Instituto de Química da UFRJ. Realizou estágio pós-doutoral no University College London (UCL) sob a supervisão do Prof. C. Robin Ganellin, FRS. Atualmente orienta teses na área de Química Medicinal, sendo credenciado no Programa de Pós-Graduação em Química. Além da atuação na pós-graduação strictu sensu, é também coordenador do curso

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“…Quinazoline derivatives have been attracting increased attention due to their well-pronounced biological (e.g., anti-malaria, 1 antitumor, 2 anti-inflammatory, 3,4 and anti-hypertensive) 5 activity, as exemplified by Afatinib and Elotinib, both of which are tyrosine kinase inhibitors used for cancer treatment. 6 Further examples include Prazosin (anti-hypertensive), reactivity of NHCs allows aldehyde carbonyls to react with electrophiles, with this type of reaction being mediated exclusively by NHCs and the cyanide ion.…”

Section: Introductionmentioning

confidence: 99%

Nucleophilic Aroylation on Fluoroquinazolines Catalyzed by N-Heterocyclic Carbenes

Suzuki¹,

Tachikawa²,

Nakagawa³

2018

HETEROCYCLES

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-We report on the synthesis of 7-benzoyl-and 7-heteroaroylquinazolines from 7-fluoroquinazolines and aromatic aldehydes by N-heterocyclic carbene (NHC)-catalyzed nucleophilic aromatic substitution, showing that the NHC derived from 1,3-dimethylimidazolium iodide outperformed those originating from other azolium (e.g., thiazolium and triazolium) salts. Additionally, the developed methodology allowed the preparation of 5-and 8-aroylquinazolines from the corresponding fluoroquinazolines.

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Molecular features of the prazosin molecule required for activation of Transport-P

Cited by 71 publications

References 19 publications

Expanding applications of zeolite imidazolate frameworks in catalysis: synthesis of quinazolines using ZIF-67 as an efficient heterogeneous catalyst

Expanding applications of zeolite imidazolate frameworks in catalysis: synthesis of quinazolines using ZIF-67 as an efficient heterogeneous catalyst

The Medicinal Chemistry at the “Polo de Xistoquímica” of the IQ‐UFRJ

Nucleophilic Aroylation on Fluoroquinazolines Catalyzed by N-Heterocyclic Carbenes

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