Within this work, we describe the design and synthesis of a range of novel thiochromanones based on natural products reported to possess anti-leishmanial action, and their synthetic derivatives. All compounds were elaborated via the key intermediate 2,2,6-trimethoxythiochromanone, which was modified at the benzylic position to afford various ester, amine and amide analogues, substituted by chains of varying lipophilicity. Upon testing in Leishmania, IC50 values revealed the most potent compounds to be phenylalkenyl and haloalkyl amides 11a and 11e, with IC50 values of 10.5 and 7.2 μM, respectively.
This work describes a systematic and bibliometric review of the factors that contribute to the expansion of leishmaniasis in urban areas. Three scientific databases were used: Scientific Electronic Library (Sci ELO), Scopus and Web of Science, encompassing all original and review articles between 1959 and 2021. Three descriptors were used: “leishmaniasis” AND “urban” AND “rural.” Planning, execution, summarization, and selection processes were performed using StArt ( State of the Art through Systematic Review) software. We obtained a total of 304 articles, 60 of which concerned canine leishmaniasis. The factors associated with the expansion of leishmaniasis in urban areas are interrelated, including socioenvironmental and economic complexity, the type of leishmaniasis, the reservoirs, vectors, deforestation, disorderly occupation of space, poor sanitary conditions, and human migration trends. A lack of diagnosis and underreporting of cases in some regions may reflect the increase of cases seen in urban areas. A majority ( n = 121) of studies were conducted in Brazil, followed by Iran ( n = 43). In relation to publications; in general, output has increased over the years, particularly in 2021. The majority of published studies were in the area of epidemiology ( n = 158).
Reações de acoplamento do tipo Heck, Sonogashira-Hagihara, Suzuki-Miyaura e reação de aldolisação catalizadas por metal foram utilizadas para a obtenção de três séries de d-valerolactonas substituídas em posições 3, 4, 5 e 6 do anel lactônico. As 26 d-valerolactonas sintetizadas foram testadas contra três linhagens celulares e cinco delas exibiram uma moderada atividade citotóxica.Palladium-catalyzed cross coupling reactions (Sonogashira-Hagihara, Suzuki-Miyaura, and Heck) coupling and nickel hydride-mediated tandem isomerization aldolisation have been used for the synthesis of three series of d-valerolactones substituted in positions 3, 4, 5 and 6 of the lactone ring. The 26 kavaïn-like derivatives were tested against three cell lines and five of them exhibited a weak cytotoxic activity.
O conhecimento popular sobre os vegetais para uso medicinal e alimentício cresce exponencialmente, sendo repassado principalmente através de gerações. Este estudo objetivou relatar o saber popular sobre espécies medicinais utilizadas contra doenças do trato gastrointestinal (TGI) e seus potenciais alimentícios. Realizou-se um estudo minucioso com uma conhecedora de plantas medicinais, reconhecida por seus saberes por moradores do município de Cocal do Sul, SC. Foi aplicado a ela um formulário sobre as plantas indicadas para o tratamento de doenças no TGI (parte usada, formas de preparo e aplicação medicinal/alimentícia). Foram registradas 17 espécies pertencentes a 17 gêneros e a 12 famílias botânicas. Todas as 17 espécies são para uso medicinal e, dessas, 15 também são alimentícias. As folhas das espécies foram as mais utilizadas para fins medicinais, na forma de chá ou infusão e, de acordo com a preparação, deu-se destaque às saladas e sucos na forma de alimento. Das espécies indicadas como medicinais nove são validadas pela Agência Nacional de Vigilância Sanitária (ANVISA), sendo duas nativas do Brasil, remetendo à necessidade de mais estudos científicos sobre o potencial medicinal de espécies nacionais. Do total, cinco das espécies foram categorizadas como plantas alimentícias não convencionais (PANC). O presente estudo confirma o saber popular/tradicional sobre as plantas medicinais e alimentícias, contribuindo de forma concisa sobre informações dessas espécies no TGI. Palavras-chave: Fitoterapia. Plantas Alimentícias. Conhecimento Popular e Tradicional. Sistema TGI. Abstract Folk knowledge about plants for medicinal and food use grows exponentially, being reposted mainly through generations. This study aims to highlight the ethno-medicinal information regarding medicinal plants, their nutritional properties and how they are used for treating various Gastrointestinal diseases (GI diseases). A detailed study was carried out with an expert on medicinal plants, recognized locally by people of the municipality of Cocal do Sul (Santa Catarina) for her herbal knowledge. Data regarding the treatment of GI diseases with wild vegetables were collected using a questionnaire (i.e., which plant resources are use and how are they prepared). Seventeen species belonging to seventeen genera and twelve botanical families were mentioned. All plants mentioned are medicinal and fifteen out of them are edible. The leaves are mostly used medicinally, in the form of tea or infusion and, according to their food preparation culture, it is necessary to use them mostly on salads and juices. The Brazilian Health Regulatory Agency (ANVISA) approves only nine of the species indicated as medicinal, two of which are native to Brazil. Five of these species have been qualified in Non-Conventional Food Plants (PANC). These numbers show that further documentation of traditional knowledge of native medicinal flora is needed. The present study confirms the popular/traditional knowledge about medicinal and edible plants, contributing in a concise way to information about these species in the TGI. Keywords: Phytotherapy. Edible Plants. Folk and Traditional Knowledge. GI Diseases System.
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