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Recentes avanços na funcionalização seletiva de quinolinas

Ferreira,Dartagnan S. P.; Murie,Valter E.; Santos,Thiago dos; Vieira,Paulo C.; Clososki,Giuliano C.

Heterocyclic compounds form an important and extensive group of organic substances. Among nitrogenous heterocyclic molecules, quinolines stand out for exhibiting attractive chemical and biological properties. These substances can be used as ligands, sensors, luminescent and agrochemical materials. In addition, quinoline-containing compounds can exhibit a wide spectrum of pharmacological properties, allowing the...

Date: 2021   |   Origin: Oasisbr

New Synthetic Quinolines as Cathepsin K Inhibitors

Silva,Taynara L.; Bartolomeu,Aloisio de A.; Jesus,Hugo C. R. de; Oliveira,Kleber T. de; Fernandes,João B.; Brömme,Dieter; Vieira,Paulo C.

Cathepsin K is a papain-like cysteine protease and is responsible for collagen degradation in bone tissue and thus represents an important target for the development of new therapies for treating diseases such as osteoporosis. Quinolines are an important class of heterocyclic molecular leads with a great pharmacological potential and represent a relevant scaffold to explore the chemical space of cathepsin K (Ca...

Date: 2020   |   Origin: Oasisbr

NEW DEGRADED QUINONE DITERPENOID FROM THE STEMS OF Byrsonima coccolobifolia Kun...

Sousa,Lorena R. F. de; Santos,Marcos H. F.; Severino,Vanessa G. P.; Severino,Richele P.; Vieira,Paulo C.

A chemical investigation of two specimens of Byrsonima coccolobifolia collected in the southeast cerrado and from central Brazil was performed. A new degraded diterpenoid, byrsonimaquinone, was isolated from the stems along with known compounds. This is the first study on the roots of B. coccolobifolia, and several triterpenes, such as α-amyrin, β-amyrin, oleanolic acid, and glochidonol, along with a mixture of...

Date: 2018   |   Origin: Oasisbr

A QUÍMICA DE PRODUTOS NATURAIS DO BRASIL DO SÉCULO XXI

Berlinck,Roberto G. S.; Borges,Warley de S.; Scotti,Marcus T.; Vieira,Paulo C.

The chemistry of natural products in Brazil has experienced a rapid development during the 21st century, with a diversification of lines of research, methodological approaches, exploration of diverse natural sources for the isolation of secondary metabolites and establishment of several multidisciplinary initiatives. These topics are critically discussed, evidencing achievements and new challenges to be faced f...

Date: 2017   |   Origin: Oasisbr

Isolation of Tiliroside from Spiranthera odoratissima as Inhibitor of Trypanoso...

Cornelio,Vivian E.; Maluf,Fernando V.; Fernandes,João B.; Silva,Maria Fátima G. F. da; Oliva,Glaucius; Guido,Rafael V. C.; Vieira,Paulo C.

Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) is a key enzyme involved in the Trypanosoma cruzi glycolytic pathway, parasite that causes Chagas' disease. There are only few drugs available to treat this disease, most of which present strong side effects. Natural products constitute a prime source for the discovery of new scaffolds potentially useful for the treatment of several diseases, including Chagas' di...

Date: 2017   |   Origin: Oasisbr

ALCALOIDES ACRIDÔNICOS INIBEM CATEPSINA L E V

Marques,Emerson F.; Vieira,Paulo C.; Severino,Richele P.

Cathepsins represent a class of enzymes that has the primary function of randomly degrading proteins in the lysosomes, although are also involved in different pathologies. The aim of this paper was to evaluate the capacity of acridone alkaloids isolated from Swinglea glutinosa (Rutaceae) to inhibit cathepsin L in vitro . The IC50 values found were in the 0.8-57 µM range and the most promising compounds were alk...

Date: 2016   |   Origin: Oasisbr

Rapid Detection of ACTG- and AK-Toxins in Alternaria alternata by LC-ESI-MS/MS ...

Prieto,Kátia R.; Medeiros,Lívia S. de; Isidoro,Marsele M.; Toffano,Leonardo; Silva,Maria Fátima G. F. da; Fernandes,João B.; Vieira,Paulo C.

A methanol-soluble fraction of the dichloromethane extract from the culture broth of A. alternata AT4303 strain afforded the following five known mycotoxins: alternariol, alternariol monomethyl ether, altenusin, altenuene and altertoxin I. A hexane-soluble fraction of the dichloromethane extract yielded the steroids ergosterol and ergosterol peroxide, and alternariol monomethyl ether. The concentrated ethyl ace...

Date: 2016   |   Origin: Oasisbr

Leishmanicidal galloylquinic acids are noncompetitive inhibitors of arginase

Sousa,Lorena R. F. de; Ramalho,Suelem D.; Fernandes,João B.; Silva,Maria Fátima das G. F. da; Iemma,Mônica R. da C.; Corrêa,Caroindes J.

Leishmanicidal galloylquinic acids were isolated from the ethyl acetate extract of Byrsonima coccolobifolia. These phenols and gallic acid showed to be a new class of potent noncompetitive inhibitors of arginase ARG (Ki ranging from 0.10 to 0.68 µmol L-1) from Leishmania amazonensis. Quinic acid did not exhibit significant inhibition of ARG, indicating that galloyl moiety has important features that allows the ...

Date: 2014   |   Origin: Oasisbr

Química sem fronteiras

Pinto,Angelo C.; Zucco,César; Galembeck,Fernando; Andrade,Jailson B. de; Vieira,Paulo C.

The main objective of this paper is to start and stimulate reflection, discussion and proposing actions that allow Chemistry in Brazil contribute to a prosperous, safer and better future for the nation.

Date: 2012   |   Origin: Oasisbr

Trypanocidal activity of flavonoids and limonoids isolated from Myrsinaceae and...

Leite,Ana C.; Placeres Neto,Artur; Ambrozin,Alessandra R. P.; Fernandes,João B.; Vieira,Paulo C.; Silva,Maria F. das G. F. da; de Albuquerque,Sérgio

The activity of crude extracts of three Rapanea species (Myrsinaceae) and Cipadessa fruticosa (Meliaceae) was evaluated in vitro against the trypomastigote forms of Trypanosoma cruzi. Thirty-three extracts from different organs of these species were assayed and eleven of them showed significant activity (lysis % >50). The fractionation of an active extract from branches of R. lancifolia (99.5%) led to the isola...

Date: 2010   |   Origin: Oasisbr

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