14 documents found, page 1 of 2

Medicamentos e tratamentos para a Covid-19

resumo Existem no mundo cerca de 2.000 registros de ensaios clínicos para a investigação de medicamentos aprovados e outros candidatos para a Covid-19, incluindo moléculas pequenas e medicamentos biológicos, sem contar as vacinas. O reposicionamento de fármacos, estratégia mais explorada até o momento, não levou a qualquer novo tratamento antiviral contra a Covid-19. O remdesivir, apesar de sua aprovação emerge...

Linear Peptide Analogues from Jatropha’s Orbitides Promote Migration of Human N...

Orbitides are a class of small naturally occurring cyclic peptides with structural and functional diversities. Their chemical properties make this class feasible to be obtained by solid phase peptide synthesis (SPPS). Therefore, this synthetic accessibility enables useful application and facilitates the identification of analogues, bioactivity studies, and thus, enables them to be applied to obtain peptide libr...

Synthetic Analogue of the Natural Product Piperlongumine as a Potent Inhibitor ...

Piperlongumine is a natural amide alkaloid isolated from several species of Piper and is described in the literature as selectively cytotoxic to several cancer cell lines. Inhibiting cell migration has gained considerable interest as an approach for discovering antimetastatic agents because this process is fundamental to metastasis. Piperlongumine, selected from cell-based assay screening of NuBBE Database, inh...

Structure-based drug design studies on a series of aldolase inhibitors

Human African trypanosomiasis, also known as sleeping sickness, is a major cause of death in Africa, and for which there are no safe and effective treatments available. The enzyme aldolase from Trypanosoma brucei is an attractive, validated target for drug development. A series of alkyl-glycolamido and alkyl-monoglycolate derivatives was studied employing a combination of drug design approaches. Three-dimension...

Doenças tropicais negligenciadas: uma nova era de desafios e oportunidades

In an article recently published in Química Nova, entitled "Chemistry Without Borders" ("Química Sem Fronteiras") [Pinto, A. C.; Zucco, C.; Galembeck, F.; Andrade, J. B.; Vieira, P. C. Quim. Nova 2012, 35, 2092], the authors highlighted the important aspects of science and technology with special emphasis on the field of Chemistry and its contributions toward a more prosperous Brazil of future. As a second step...

Nobel de química 2012: receptores acoplados à proteína G

A fragment-based approach for the in silico prediction of blood-brain barrier p...

Blood-brain barrier (BBB) permeation is an essential property for drugs that act in the central nervous system (CNS) for the treatment of human diseases, such as epilepsy, depression, Alzheimer's disease, Parkinson disease, schizophrenia, among others. In the present work, quantitative structure-property relationship (QSPR) studies were conducted for the development and validation of in silico models for the pr...

Planejamento de fármacos, biotecnologia e química medicinal: aplicações em doen...

Estratégias modernas de planejamento de fármacos se fundamentam no conhecimento da fisiopatologia das doenças, no estudo de vias bioquímicas e na seleção de alvos moleculares. As ferramentas biotecnológicas modernas têm fornecido informações valiosas para a descoberta e o desenvolvimento de novos fármacos. A química medicinal possui papel central em vários processos que visam à identificação de substâncias bioa...

Biochemical evaluation of a series of synthetic chalcone and hydrazide derivati...

Chagas' disease, a parasitic infection widely distributed throughout Latin America, is a major public health problem with devastating consequences in terms of human morbidity and mortality. The enzyme cruzain is the major cysteine protease from Trypanosoma cruzi, the etiologic agent of American trypanosomiasis or Chagas' disease, and has been selected as an attractive target for the development of novel trypano...

Structural insights into the molecular basis responsible for the effects of imm...

The development of fast and reliable methods for the identification of new bioactive compounds is of utmost importance to boost the process of drug discovery and development. Immobilized enzyme reactors (IMERs), integrated with high performance liquid chromatography (HPLC), are attractive and versatile tools for screening collections consisting of natural products and synthetic small molecules. Standard kinetic...