The present article describes a series of 21 N '-benzylidene-2-oxo-2H-chromene-3-carbohydrazides 4a-4v, which were synthesized and evaluated for their cell viabilities in non-infected and Mycobacterium bovis Bacillus Calmette-Guerin-infected macrophages. Subsequently, the non-cytotoxic compounds 4c, 4g, 4h, 4j, 4l and 4t were assessed against Mycobacterium tuberculosis ATCC 27294 using the microplate Alamar Blue assay and the activity expressed as the minimum inhibitory concentration in μg/mL. These compounds exhibited a significant activity (50-100 μg/mL) when compared to the first-line drugs, such as pyrazinamide (PZA >100 μg/mL). These results could be considered a good starting point for further studies to develop new lead compounds to treat multidrug-resistant tuberculosis.
Recebido em 17/8/12; aceito em 26/11/12; publicado na web em 6/3/13 FLAVONOIDS AND TERPENOIDS FROM Croton muscicarpa (Euphorbiaceae). A new sesquiterpene and twelve known compounds comprising eight flavonoids and four terpenoids, were isolated from the leaves, stems, roots and exudate of Croton muscicarpa Müll. Arg.. Their structures were identified as the terpenoids 6α-methoxy-cyperene, dammaradienol, squalene, acetyl aleuritolic acid and spathulenol, and as the flavonoids retusin, 3,7,4'-trimethoxy kaempferol, ombuine, pachipodol, kaempferol, casticin, 5-hydroxy-3,6,7,4'-tetramethoxyflavone and artemetin. All isolated compounds were characterized based on IR, MS, 1 H and 13 C NMR, including 2D analyses (COSY, HSQC, HMBC, NOESY) and comparison with data from the literature.
RESUMO:O estudo fitoquímico do extrato etanólico das folhas de Moringa oleifera Lam., Moringaceae, resultou no isolamento dos derivados benzilnitrilas niazirina, niazirinina e 4-hidroxifenil-acetonitrila, enquanto que das cascas dos frutos somente o octacosano foi obtido. Os óleos essenciais das folhas, flores e frutos foram analisados por cromatografia gasosa acoplada a espectrometria de massa. Os constituintes principais identificados foram: fitol (21,6%) e timol (9,6%) nas folhas, octadecano (27,4%) e ácido hexadecanóico (18,4%) nas flores e docosano (32,7%) e tetracosano (24,0%) nos frutos. As estruturas dos compostos isolados foram identificadas a partir de técnicas espectroscópicas (RMN, IV e EM). A 4-hidroxifenil-acetonitrila está sendo citada pela primeira vez para o gênero Moringa e os óleos essenciais das flores e frutos estão sendo citados pela primeira vez para a espécie M. oleifera. Unitermos:Moringa oleifera, Moringaceae, óleos essenciais, nitrilas, niazirina, niazirinina.ABSTRACT: "Volatile and non-volatile chemical constituents of Moringa oleifera Lam., Moringaceae". Phytochemical analysis of the ethanol extract from leaves of Moringa oleifera Lam., Moringaceae, yield the benzylnitriles: niazirine, niazirinine and 4-hydroxyphenylacetonitrile, while of fruit shells only octacosane was isolated. The essential oils from leaves, flowers and fruits were examined by gas chromatography-mass spectrometry. The major constituents identified were: phytol (21.6%) and thymol (9.6%) in the leaves oil, octadecane (27.4%) and hexadecanoic acid (18.4%) in the flowers oil, docosane (32.7%) and tetracosane (24.0%) in the fruits oil. The structures of all compounds were identified by spectroscopic analyses (NMR, IR and MS). 4-hydroxyphenylacetonitrile is reported for the first time to the Moringa genus and the essential oils of flowers and fruits are reported for the first time to the species M. oleifera.
Atualmente, os fármacos disponíveis no combate ao vírus da AIDS podem ser classificados em seis categorias: (a) inibidores da transcriptase reversa análogos de nucleosídeos (ITRNs), (b) inibidores da transcriptase reversa não nucleosídeos (ITRNNs), (c) inibidores de protease (IPs), (d) inibidores de fusão (IFs), (e) inibidores de entrada (IEs) e (f) inibidores da integrase (IIs). Devido à rápida disseminação do vírus HIV resistente aos diversos fármacos disponíveis no mercado, é necessário e urgente o desenvolvimento de novos fármacos na luta contra a AIDS. Neste contexto, o objetivo desse artigo é destacar promissores produtos naturais capazes de atuar na enzima trascriptase reversa, a qual é essencial para a replicação do vírus HIV.
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