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21.
Costa JC Neves JS de Souza MV Siqueira RA Romeiro NC Boechat N e Silva PM Martins MA 《Bioorganic & medicinal chemistry letters》2008,18(3):1162-1166
The present structure-activity relationship (SAR) study focused on chemical modifications of the structure of the local anesthetic lidocaine, and indicated analogues having reduced anesthetic potency, but with superior potency relative to the prototype in preventing anaphylactic or histamine-evoked ileum contraction. From the SAR analysis, 2-(diethylamino)-N-(trifluoromethyl-phenyl) and 2-(diethylamino)-N-(dimethyl-phenyl) acetamides were selected as the most promising compounds. New insights into the applicability of non-anesthetic lidocaine derivatives as templates in drug discovery for allergic syndromes are provided. 相似文献
22.
Carvalho SA Lopes FA Salomão K Romeiro NC Wardell SM de Castro SL da Silva EF Fraga CA 《Bioorganic & medicinal chemistry》2008,16(1):413-421
Megazol is a highly active compound against Trypanosoma cruzi, and has become a core structure for the design of new trypanocidal agents. Recently, we have identified the new potent trypanocide agent Brazilizone A, which presents an IC(50) twofold more potent than the prototype megazol. This result has encouraged us to further explore structurally-related 1,3,4-thiadiazole-2-arylhydrazone derivatives, in order to get a better understanding of their structural and antiprotozoal activity relationships. Herein we report the synthesis and trypanocidal profile of thirteen new Brazilizone A analogues, which supported the construction of 3D-QSAR models used for its structural optimization. 相似文献
23.
Pinheiro LC Abreu PA Afonso IF Leal B Corrêa LC Borges JC Marques IP Lourenço AL Sathler P dos Santos AL Medeiros CA Cabral LM Júnior ML Romeiro GA Ferreira VF Rodrigues CR Castro HC Bernardino AM 《Current microbiology》2008,57(5):463-468
Bacterial infections are a significant cause of morbidity and mortality among critically ill patients. The increase of antibiotic
resistance in bacteria from human microbiota—such as Staphylococcus
epidermidis, an important nosocomial pathogen that affects immunocompromised patients or those with indwelling devices—increased the
desire for new antibiotics. In this study we designed, synthesized, and determined the antimicrobial activity of 27 thieno[2,3-b]pyridines (1, 2, 2a–2m, 3, 3a–3m) derivatives against a drug-resistant clinical S. epidermidis strain. In addition, we performed a structure-activity relationship analysis using a molecular modeling approach, and discuss
the drug absorption, distribution, metabolism, excretion, and toxicity profile and Lipinski’s “rule of five,” which are tools
to assess the relationship between structures and drug-like properties of active compounds. Our results showed that compound
3b (5-(1H-tetrazol-5-yl)-4-(3`-methylphenylamino)thieno[2,3-b]pyridine) was as active as oxacillin and chloramphenicol but with
lower theoretical toxicity risks and a better drug likeness and drug score potential than chloramphenicol. All molecular modeling
and biological results reinforced the promising profile of 3b for further experimental investigation and development of new antibacterial drugs.
Electronic supplementary material The online version of this article (doi:) contains supplementary material, which is available to authorized users. 相似文献
24.
J. R. De Oliveira R. Da Silva Romeiro B. De Souza Leäo Lacerda 《Journal of Phytopathology》1994,140(4):363-366
Occurrence of crown gall on grape was observed in a vineyard in Minas Gerais State, Brazil. Isolations of the pathogen yielded a bacterium which incited galls on grapevine, tomato and bryophillum. The bacterium was confirmed as Agrobacterium tumefaciens and its characterization showed it to be biovar 3. This is the first report on the occurrence of the biovar 3 of A. tumefaciens on grapevine in Brazil. 相似文献
25.
Development of a Root Colonization Bioassay for Rapid Screening of Rhizobacteria for Potential Biocontrol Agents 总被引:4,自引:0,他引:4
Harllen Sandro Alves Silva Reginaldo da Silva Romeiro Ann Mounteer 《Journal of Phytopathology》2003,151(1):42-46
The ability to colonize roots is a sine qua non condition for a rhizobacteria to be considered a true plant growth‐promoting rhizobacteria (PGPR). A simple screening method to detect such a potential ability of PGPR is described. Tomato seeds were surface sterilized for 30 s in 50% ethanol and this was followed by 3 min dipping in 2% NaClO. They were then washed three times in sterile water, left immersed in a propagule suspension of the rhizobacteria for 24 h, and transferred onto sterile 0.6% water‐agar in tubes. The young, developing root system shows a tendency to grow downwards in the agar‐gel column. When the rhizobacterium has a potential ability to colonize roots it is possible to visualize, by transparency, bacterial growth (turbid, milky and narrow zone) along and around roots. Testing 500 rhizobacteria isolated from tomato rhizosphere for their ability to induce systemic resistance against Pseudomonas syringae pv. tomato, 28 of them did reduce infection to less than 40% and all 28 colonized roots according to the described bioassay. Therefore the bioassay may turn into an important auxiliary tool for helping in selecting rhizobacteria with PGPR potentiality. 相似文献
26.
Properties of the sliding disintegration response of demembranated tetrahymena cilia have been studied by measuring the spectrophotomeric response or turbidity of cilia suspensions at a wavelength of 350 nm relative to changes in the dynein substrate (MgATP(2-)) concentration. The maximum decrease in turbidity occurs in 20 muM ATP, and 90 percent of the decrease occurs in approximately 5.9 s. At lower ATP concentrations (1-20 muM), both the velocity and magnitude of the turbidity decreases are proportional to ATP concentration. The velocity data for 20 muM ATP permit construction of a reaction velocity curve suggesting that changes in turbidity are directly proportional to the extent and velocity of disintegration. At ATP concentrations more than 20 muM (50muM to 5mM), both velocity and magnitude of the turbidimetric response are reduced by approximately 50 percent. This apparent inhibition results in a biphasic response curve that may be related to activation of residual shear resistance or regulatory components at the higher ATP concentrations. The inhibitory effects of elevated ATP can be eliminated by mild trypsin proteolysis, whereupon the reaction goes to completion at any ATP concentration. The turbidimetric responses of the axoneme-substrate suspensions are consistent with the extent and type of axoneme disintegration revealed by electron microscope examination of the various suspensions, suggesting that the turbidimetric assay may prove to be a reliable means for assessing the state of axoneme integrity. 相似文献
27.
28.
Veloso MP Romeiro NC Silva GM Alves Hde M Doriguetto AC Ellena J Miranda AL Barreiro EJ Fraga CA 《Chirality》2012,24(6):463-470
This work describes the atropisomeric relationships of 3-methyl-5-(3-methyl-5-phenyl-1H-pyrazol-1-yl)-1-phenyl-1H-pyrazol-4-amine (2d), which belongs to series 4-aminobipyrazole derivatives designed as anti-inflammatory agents. The (1)H nuclear magnetic resonance spectra obtained in the presence of a chiral lanthanide shift salt associated to chiral high-performance liquid chromatography analysis, X-ray diffraction, and molecular modeling tools confirmed that ortho bis-functionalized bipyrazole 2d exists as a mixture of aR,aS-atropisomers. These results provide useful information to understand the pharmacological profile of this derivative and of other 4-aminobipyrazole analogs. 相似文献
29.
Medeiros MN Oliveira DM Paiva-Silva GO Silva-Neto MA Romeiro A Bozza M Masuda H Machado EA 《Insect biochemistry and molecular biology》2002,32(5):537-545
The participation of eicosanoids and second messengers on the regulation of RHBP endocytosis by the ovaries was investigated, using [(125)I]RHBP in experiments in vivo and in vitro. Addition of PGE(2) (one of the products of the cyclooxygenase pathway) decreased in vitro the uptake of RHBP by 35%. The rate of RHBP endocytosis increased in the presence of indomethacin, a potent cyclooxigenase inhibitor, up to 50% in vitro and up to 55% in vivo, thus giving support to the role of cyclooxygenase derivatives on endocytosis regulation. The amount of PGE(2) secreted to the culture medium by the cells of Rhodnius prolixus ovaries was 1.1 ng/ovary following RHBP uptake assay. The amount of PGE(2) decreases approximately 25% in the presence of 5 microM indomethacin. Using a scanning electron microscope we have observed that neither the surface area nor the patencies of follicle cells were affected by treatment with indomethacin, thus suggesting that, its effect is elicited in the oocyte. Finally, we have identified two ovarian peptides that were dephosphorylated after the indomethacin treatment (18 and 25 kDa). Taken together these data show that local mediators such as eicosanoids act upon the oocytes controlling RHBP endocytosis, perhaps using the protein phosphorylation signal transduction pathway. 相似文献
30.
Dirceu Macagnan Reginaldo da S. Romeiro Alan W.V. Pomella Jorge T. deSouza 《Biological Control》2008,47(3):309-314
Streptomyces albovinaceus, Streptomyces caviscabies, Streptomyces griseus, Streptomyces setonii, and Streptomyces virginiae selected as antagonists of Moniliophthora (ex Crinipellis) perniciosa, the causal agent of cacao Witches’ broom, were examined in vitro to detect production of chitinases, β-1,3-glucanases, and cellulases. All the species produced chitinases, but not β-1,3-glucanases or cellulases, when grown on a liquid mineral medium containing glucose, colloidal chitin, or cell walls of M. perniciosa as a carbon source. There were no quantitative differences among species in the production of chitinase, however, the germination inhibition of basidiospores of M. perniciosa was higher when they were cultivated using glucose as a carbon source, followed by colloidal chitin and cell walls. All the species also produced hydroxymate type siderophores in similar quantities, and the quantity of siderophores did not correlate with the inhibition of basidiospore germination. The germination inhibition was more pronounced when S. albovinaceus, S. griseus, and S. virginiae were cultivated on iron-deficient medium, suggesting involvement of siderophores in the antagonism by these species of actinomycetes. 相似文献