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1.
J Med Chem ; 67(6): 4251-4258, 2024 Mar 28.
Artigo em Inglês | MEDLINE | ID: mdl-38456628

RESUMO

As we celebrate International Women's Day 2024 with the theme "Inspire Inclusion", the women of the ACS Medicinal Chemistry Division (MEDI) want to foster a sense of belonging, relevance, and empowerment by sharing uplifting stories of what inspired them to become medicinal chemists. In this editorial, we are featuring female medicinal chemistry scientists to provide role models, encouragement, and inspiration to others. We asked women medicinal chemists to contribute a brief paragraph about what inspired them to become medicinal chemists or what inspires them today as medicinal chemists. The responses and contributions highlight their passions and motivations, such as their love of the sciences and their drive to improve human health by contributing to basic research and creating lifesaving drugs.


Assuntos
Química Farmacêutica , Poder Psicológico , Humanos , Feminino
2.
ACS Med Chem Lett ; 15(4): 424-431, 2024 Apr 11.
Artigo em Inglês | MEDLINE | ID: mdl-38628790

RESUMO

As we celebrate International Women's Day 2024 with the theme "Inspire Inclusion", the women of the ACS Medicinal Chemistry Division (MEDI) want to foster a sense of belonging, relevance, and empowerment by sharing uplifting stories of what inspired them to become medicinal chemists. In this editorial, we are featuring female medicinal chemistry scientists to provide role models, encouragement, and inspiration to others. We asked women medicinal chemists to contribute a brief paragraph about what inspired them to become medicinal chemists or what inspires them today as medicinal chemists. The responses and contributions highlight their passions and motivations, such as their love of the sciences and their drive to improve human health by contributing to basic research and creating lifesaving drugs.

3.
Bioorg Med Chem Lett ; 23(3): 779-84, 2013 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-23273521

RESUMO

In a recent disclosure, we described the discovery of dimeric, prolinamide-based NS5A replication complex inhibitors exhibiting excellent potency towards an HCV genotype 1b replicon. That disclosure dealt with the SAR exploration of the peripheral region of our lead chemotype, and herein is described the SAR uncovered from a complementary effort that focused on the central core region. From this effort, the contribution of the core region to the overall topology of the pharmacophore, primarily vector orientation and planarity, was determined, with a set of analogs exhibiting <10 nM EC(50) in a genotype 1b replicon assay.


Assuntos
Antivirais/química , Proteínas não Estruturais Virais/antagonistas & inibidores , Antivirais/farmacologia , Carbamatos , Hepacivirus/efeitos dos fármacos , Imidazóis/química , Imidazóis/farmacologia , Concentração Inibidora 50 , Estrutura Molecular , Prolina/análogos & derivados , Prolina/química , Prolina/farmacologia , Pirrolidinas , Relação Estrutura-Atividade , Valina/análogos & derivados , Proteínas não Estruturais Virais/química , Replicação Viral/efeitos dos fármacos
4.
ACS Chem Neurosci ; 13(13): 1849-1856, 2022 07 06.
Artigo em Inglês | MEDLINE | ID: mdl-35738565

RESUMO

The kappa agonist structure-activity relationship around the novel, pyrrolidinyl substituted pyranopiperazine scaffold was developed. More specifically, the dichloroPhenylAcetamide-Pyrrolidinyl-PyranoPiperazine (PAPPP) core A was the focus of our work. The modulation of kappa receptor potency/G-protein activation and arrestin recruitment with respect to changes of the piperazine R group in A was demonstrated. Reduced ß2-arrestin recruitment and differential G-protein bias were observed for select analogues. To better understand the subtlety in receptor signaling, analogues were profiled as the resolved enantiomers. To determine in vivo target engagement, a subset of compounds was tested in mice for stimulation of serum prolactin, a neuroendocrine biomarker of KOR-agonist effects. Additional in vivo characterization included measurement of potential unwanted effects of kappa receptor activation such as sedation. These studies demonstrate a novel kappa receptor agonist scaffold with potential for G-protein signaling bias to probe in vivo pharmacology.


Assuntos
Analgésicos Opioides , Receptores Opioides kappa , Analgésicos Opioides/farmacologia , Animais , Arrestinas/metabolismo , Proteínas de Ligação ao GTP/metabolismo , Camundongos , Receptores Opioides kappa/metabolismo , Transdução de Sinais
5.
Org Lett ; 5(9): 1531-3, 2003 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-12713316

RESUMO

Isonitriles and ureas undergo a condensation reaction in the presence of acid chlorides to give formamidine ureas, for which no general synthetic routes currently exist. A mechanism is proposed in which the key intermediate is an electrophilic adduct of isonitrile and acid chloride. The process is tolerant of moderate variability in the nature of the components, and access to formamidine ureas of varying substitution patterns is further enhanced by a facile exchange reaction with amines. [reaction: see text]


Assuntos
Amidinas/síntese química , Ureia/análogos & derivados , Ureia/síntese química , Aminas/química , Modelos Moleculares , Nitrilas/química
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