Synthetic Analogs Biological Activity
Mostrando 1-12 de 25 artigos, teses e dissertações.
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1. Synthesis of Hydroxybenzodiazepines with Potential Antioxidant and Antifungal Action
Benzodiazepines derivatives are nitrogen heterocyclic compounds that have various industrial, synthetic, and medicinal applications. Therefore, its potential fully justifies every effort towards the improvement of new, selective, and competent production of these heterocyclic compounds. The novelty of this study encompasses the synthesis of new hydroxylated
J. Braz. Chem. Soc.. Publicado em: 2021-03
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2. Síntese de análogos da papulacandina D por simplificação molecular e avaliação de sua atividade antifúngica
The papulacandins are a family of glycolipids isolated, by fermentation, from Papularia spherosperma, and that have shown potent in vitro antifungal activity against different strains of Candida sp. These compounds inhibit the enzyme â(1,3)-Dglucan synthase preventing the â(1,3)-D-glucan synthesis, a vital constituent of fungal cell wall. The papulacandins
Publicado em: 2010
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3. Biological activity of amides and analogs from Piper species and synthetic analogs / Atividade biológica de amidas e análogos de espécies de Piper e estudos biossintéticos
Six amides were isolated from Piper scutifolium and P. corcovadensis including piperovatine, piperlonguminine, isopiperlonguminine and corcovadine, the new scutifoliamide A and scutifoliamide B and also two aristolactams (piperolactam C and stigmalactam). From P. tuberculatum the amides piplartine and pellitorine and two esters, ethyl (E)-3,4,5-trimethoxycin
Publicado em: 2009
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4. Effects of Analogs of the Fungal Sexual Pheromone Sirenin on Male Gamete Motility in Allomyces macrogynus1
The ability of various structural analogs of the sexual pheromone sirenin to attract male gametes of the aquatic fungus Allomyces macrogynus was determined. Previous studies had shown that several structural analogs and stereoisomers of natural l-sirenin were devoid of activity at physiological concentrations. We now report the discovery of a structural anal
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5. Expression of endotoxic activities by synthetic monosaccharide lipid A analogs with alkyl-branched acyl substituents.
Synthetic monosaccharide lipid A analogs with alkyl-branched acyl substituents instead of the usual ester-branched acyl substituents were investigated for their biological activities. The activities were compared with those of a representative synthetic monosaccharide lipid A analog with an ester branch (GLA-60) and synthetic complete lipid A (506) to estima
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6. Modulation of the immune response by a synthetic adjuvant and analogs.
N-Acetylmuramyl-L-alanyl-D-isoglutamine increases the humoral immune response of mice when given in aqueous media instead of the usual water-in-oil emulsions. Moreover, this compound is adjuvant active even by the oral route. In view of studying the relation between chemical structure and biological activity, several synthetic analogs were tested. The immune
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7. Biological activity of synthetic phosphonooxyethyl analogs of lipid A and lipid A partial structures.
We investigated the biological activity of four new synthetic analogs of lipid A, termed PE-1, PE-2, PE-3, and PE-4. All compounds contain an alpha-oxyethyl-linked (-O-CH2-CH2-) phosphoryl group in position 1 of the reducing glucosaminyl residue (GlcN I) of lipid A. PE-1 is a hexaacylated analog of Escherichia coli lipid A (compound 506). PE-2 differs from P
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8. Enantioselective syntheses and biological studies of aeruginosin 298-A and its analogs: Application of catalytic asymmetric phase-transfer reaction
Aeruginosin 298-A was isolated from the freshwater cyanobacterium Microcystis aeruginosa (NIES-298) and is an equipotent thrombin and trypsin inhibitor. A variety of analogs were synthesized to gain insight into the structure–activity relations. We developed a versatile synthetic process for aeruginosin 298-A as well as several attractive analogs, in which
National Academy of Sciences.
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9. The design, computer modeling, solution structure, and biological evaluation of synthetic analogs of bryostatin 1
The bryostatins are a unique family of emerging cancer chemotherapeutic candidates isolated from marine bryozoa. Although the biochemical basis for their therapeutic activity is not known, these macrolactones exhibit high affinities for protein kinase C (PKC) isozymes, compete for the phorbol ester binding site on PKC, and stimulate kinase activity in vitro
The National Academy of Sciences.
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10. Biological activities of synthetic lipid A analogs: pyrogenicity, lethal toxicity, anticomplement activity, and induction of gelation of Limulus amoebocyte lysate.
Chemically synthesized lipid A analogs were investigated for several endotoxic activities, including pyrogenicity, lethal toxicity, anticomplement activity, and the capacity to gelate Limulus amoebocyte lysate in comparison to natural lipid A. The synthetic preparations contained D-glucosamine or D-glucosamine-beta-1,6-D-glucosamine disaccharide substituted
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11. Endotoxic induction of prostaglandin release from macrophages by nontoxic lipid A analogs synthesized chemically.
The ability of synthetic lipid A analogs to induce prostaglandin synthesis in macrophages was compared with that of native lipopolysaccharide. The synthetic preparations comprised monomeric or dimeric derivatives of D-glucosamine with different patterns of substitution by phosphate and tetradecanoic, (R)-3-hydroxytetradecanoic, and (R)-3-tetradecanoyloxytetr
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12. Synthetic peptides with the biological activities and specificity of human C3a anaphylatoxin.
Two peptides identical to the COOH-terminal sequence of human C3a anaphylatoxin and two analogs were synthesized by the solid-phase method and tested for biological activity. The synthetic COOH-terminal octapeptide, C3a-(70-77) or Ala-Ser-His-Leu-Gly-Leu-Ala-Arg, caused contraction of guinea pig ileum and uterus, release of vasoactive amines from rat mast ce