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排序方式: 共有139条查询结果,搜索用时 31 毫秒
31.
Fátima M.F. Vergara Maria das G.M.O. Henriques André L.P. Candea Jim L. Wardell Marcus V.N. De Souza 《Bioorganic & medicinal chemistry letters》2009,19(17):4937-4938
A series of 11 α,ω-diaminoalkanes, (H2N(CH2)nNH2, n = 2–12) have been evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv. Compounds, (H2N(CH2)nNH2, n = 9–12), exhibited a very good activities in the range 2.50–3.12 μg/mL, which can be compared with that of the first line drug, ethambutol (3.12 μg/mL). These results and a preliminary QSAR study can be considered an important start point for the rational design of new leads for anti-TB compounds. 相似文献
32.
Costa MS Boechat N Rangel EA da Silva Fde C de Souza AM Rodrigues CR Castro HC Junior IN Lourenço MC Wardell SM Ferreira VF 《Bioorganic & medicinal chemistry》2006,14(24):8644-8653
The aim of this work was to describe the synthesis, the in vitro anti-Mycobacterium tuberculosis profile, and the structure–activity relationship (SAR) study of new N-substituted-phenyl-1,2,3-triazole-4-carbaldehydes (3a–l). The reactions of aromatic amine hydrochlorides with diazomalonaldehyde (1) produced several N-substituted-phenyl-1,2,3-triazole-4-carbaldehydes (3a–l) in moderate-to-good yields. In order to investigate the influence of the difluoromethylene group on the anti-Mycobacterium activity of these compounds, fluorination of triazoles with DAST converted the corresponding carbaldehyde compounds into new difluoromethyl derivatives (4a–l) in excellent yield. Characterization of all compounds was achieved by spectroscopic means and additional for 1-(4-methylphenyl)-1,2,3-triazole-4-carbaldehyde, 3k by X-ray crystallography. Compounds (3a–l) and (4a–l) have been screened for the inhibitory activity against Mycobacterium tuberculosis H37Rv strain (ATCC 27294) and all of them were able to inhibit the growth of the bacterium. Interestingly, 3a and 3k exhibited the best inhibition with MIC values of 2.5 μg/mL, similar to pharmaceuticals currently used in the treatment of tuberculosis. Our SAR study indicated the importance of the hydrogen bond acceptor subunit (3a–l), the position in the aromatic ring, the planarity of triazole and phenyl rings in these compounds, and a correlation between the uniform HOMO coefficient distribution and the anti-tubercular activity. The significant activity of 3a and 3k pointed them as promising lead molecules for further synthetic and biological exploration. 相似文献
33.
Question: Can species compositional dissimilarity analyses be used to assess and improve the representation of biodiversity patterns in a priori ecological classifications? Location: The case study examined the northern‐half of the South‐east Queensland Bioregion, eastern Australia. Methods: Site‐based floristic presence–absence data were used to construct species dissimilarity matrices (Kulczynski metric) for three levels of Queensland's bioregional hierarchy – subregions (1:500 000 scale), land zones (1:250 000 scale) and regional ecosystems (1:100 000 scale). Within‐ and between‐class dissimilarities were compiled for each level to elucidate species compositional patterns. Randomized subsampling was used to determine the minimum site sampling intensity for each hierarchy level, and the effects of lumping and splitting illustrated for several classes. Results: Consistent dissimilarity estimates were obtained with five or more sites per regional ecosystem, 10 or more sites per land zone, and more than 15 sites per subregion. On average, subregions represented 4% dissimilarity in floristic composition, land zones approximately 10%, and regional ecosystems over 19%. Splitting classes with a low dissimilarity increased dissimilarity levels closer to average, while merging ecologically similar classes with high dissimilarities reduced dissimilarity levels closer to average levels. Conclusions: This approach demonstrates a robust and repeatable means of analysing species compositional dissimilarity, determining site sampling requirements for classifications and guiding decisions about ‘lumping’ or ‘splitting’ of classes. This will allow more informed decisions on selecting and improving classifications and map scales in an ecologically and statistically robust manner. 相似文献
34.
Simple cyclic fed-batch culture (cfbc), consisting of a constant medium feed with periodic withdrawals of culture, resulted in a product yield (13.4 mg protein per gram biomass) similar to that obtained using the complex multiphase industrial production strategy (13.7 mg protein per gram biomass). In cfbc, productivity was ultimately limited by the rate at which the cells could assimilate methanol. Glycerol was inhibitory to growth at high concentrations. However, product yield continued to increase as the glycerol concentration was increased. In chemostat culture, dissolved oxygen concentration influenced product yield independently of any detectable influence on cell growth. 相似文献
35.
36.
Can labels suggestively influence sensory perceptions and taste? Using a “ Phantom Ingredient” taste test, we show that the presence or absence of a labeled ingredient (soy) and the presence or absence of a health claim negatively bias taste perceptions toward a food erroneously thought to contain soy. We found a label highlighting soy content made health claims believable but negatively influenced perceptions of taste for certain segments of consumers. Our results and discussion provide better direction for researchers who work with ingredient labeling as well as for those who work with soybean products. 相似文献
37.
The transport of free polymannose-type oligosaccharides from the lumen of
the endoplasmic reticulum into the cytosol has been recently demonstrated
(Moore,S.E.H., et al., 1995, EMBO J., 14, 6034-6042), but at present little
is known of the characteristics of this process. Here, it is shown that
inhibition of the transport of endogenously synthesized metabolically
radiolabeled free oligosaccharides out of the endoplasmic reticulum into
the cytosol of permeabilized HepG2 cells occurs when assays are conducted
in the presence of mannose (IC50, 4.9 mM), or its derivatives modified at
the first carbon (C1) of the sugar ring; alpha-methyl mannoside (IC50, 2.0
mM), mannoheptulose (IC50, 1.6 mM), and alpha-benzyl mannoside (IC50, 0.8
mM), whereas other monosaccharides (50 mM), differing from mannose at
position; C2 (glucose), C3 (altrose), C4 (talose), C5 (l-rhamnose), and C6
(mannoheptose), have little effect. N-Acetylglucosamine does not inhibit
oligosaccharide transport and, furthermore, although mannobioses and a
mannotriose inhibit free oligosaccharide transport, di-N-acetylchitobiose
is without effect. It is also shown that if the transport assay buffer is
either depleted of calcium ions, or supplemented with the Ca2+/Mg2+ATPase
inhibitor, thapsigargin, or with calcium ionophores, free oligosaccharide
transport out of the endoplasmic reticulum is inhibited. These results
demonstrate that the terminal nonreducing mannosyl residues of free
polymannose-type oligosaccharides and not their
N-acetylglucosamine-containing reducing termini, play an important role in
the interaction of the free oligosaccharide with the transport machinery,
and that this transport process requires the presence of calcium
sequestered in the lumen of the endoplasmic reticulum.
相似文献
38.
Thus far the life cycle of Trypanosoma (Megatrypanum) theileri has not been studied. We collected tabanids during the mass hatching, when only few tabanids are infected with trypanosomes. Tabanids were caught immediately after attacking a bait cow to serve as controls or after they had been allowed to engorge on the Trypanosoma (M.) theileri-infected cow. Tabanids were kept in the laboratory and used to study the developmental cycle of T. (M.) theileri in the tabanid gut. From day 1 to day 10 the presumably unfed controls and the engorged tabanids were dissected and cytological smears made from the mid- and hindgut. In total 2.6% (1/38) of the controls and 39% (23/59) of the engorged tabanids were positive for trypanosomes in the 1991 season. From day 1 to day 4 after engorgement trypanosomes were found in the midgut. Epimastigotes with a length of 29 μm on day 1 after infection multiplied by inequal division to form smaller epimastigotes of 26 μm on day 3. On day 4 morphologically indistinguishable trypanosomes of 21 μm total length were found in both mid- and hindgut. From day 5 to day 10 trypanosomes were found only in the hindgut in which the transformation to metacyclics was demonstrated, i.e. epimastigotes transformed to amastigote stages of 5 μm in total length. 相似文献
39.
40.
We have shown previously that the β-adrenergic agonist isoproterenol (2μM) and the phosphodiesterase inhibitor isobutylmethylxanthine (1 mM) produce a much greater increase in cyclic AMP in human leukocytes that have been pretreated with colchicine (or with other agents that affect microtubule assembly) than in control leukocytes. The effects of colchicines were both time- and dose-dependant. These and other data suggested that the generation of cyclic AMP is normally restricted by an intact system of cytoplasmic microtubules. If so, then the same time and dose dependencies might apply to other colchicines-induced changes in leukocyte function. We have now assayed the distribution of concanavalin A (Con A)-receptor complexes on the leukocyte membrane, taking into account that leukocytes competent to assemble microtubules show a uniform distribution of surface- bound Con A whereas microtubule-deficient cells accumulate Con A in surface caps. We have found that the effect of colchicine on capping is also both time- and dose dependent, and that the dose-response relationships conform to those required to increase cyclic AMP levels. These findings provide further evidence that both colchicine-induced Con-A capping and colchicine- induced cyclic AMP generation depend upon the relaxation of constraints normally imposed by cytoplasmic microtubules upon the plasma membrane, which limit, respectively, lateral mobility of the lectin-receptor complexes, and expression of hormone-sensitive adenylate cyclase. Moreover, colchicine-induced Con-A cap formation is not affected even by very large changes in leukocyte cyclic AMP levels. Thus, elevated cyclic AMP levels do not appear to promote the dissolution of microtubules; rather, the dissolution of microtubules permits the generation of increased amounts of cyclic AMP. 相似文献