Analogues Synthesis
Mostrando 1-12 de 286 artigos, teses e dissertações.
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1. Expedient Microwave-Assisted Synthesis of Bis(n)-lophine Analogues as Selective Butyrylcholinesterase Inhibitors: Cytotoxicity Evaluation and Molecular Modelling
In the brain of patients with chronic Alzheimer’s disease (AD), the butyrylcholinesterase (BuChE) levels rise while the acetylcholinesterase (AChE) levels decrease. Therefore, development of new selective BuChE inhibitors is of vital importance. Here we present a series of bis(n)-lophine analogues, where two lophine derivatives are connected by a methylene
J. Braz. Chem. Soc.. Publicado em: 2021-06
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2. Linear Peptide Analogues from Jatropha’s Orbitides Promote Migration of Human Neonatal Foreskin Fibroblasts in vitro and Collagen Deposition
Orbitides are a class of small naturally occurring cyclic peptides with structural and functional diversities. Their chemical properties make this class feasible to be obtained by solid phase peptide synthesis (SPPS). Therefore, this synthetic accessibility enables useful application and facilitates the identification of analogues, bioactivity studies, and t
J. Braz. Chem. Soc.. Publicado em: 21/10/2019
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3. Inibição do crescimento de microrganismos patogênicos induzida por butenolídeos análogos aos cadiolídeos
The increasing number of antibiotic resistant microorganisms requires the development of new drugs. In this context, natural cadiolides are promising leads as they present potent antimicrobial activity and low cytotoxicity. In this work we report the synthesis of 21 new cadiolide analogues. The synthesis involved a Diels−Alder cycloaddition/ cycloreversion
Quím. Nova. Publicado em: 15/08/2019
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4. Oxone®-Mediated Direct α-Hydroxylation of β-Dicarbonyl Compounds: Racemic Synthesis of Harzialactone A
An environmentally benign method is described for the α-hydroxylation of malonates and cyclic analogues in aqueous medium at room temperature under mild conditions, based on the in situ generation of dimethyldioxirane through the combination of acetone and Oxone®. This procedure was found to be substrate-dependent and was successfully performed to provide
J. Braz. Chem. Soc.. Publicado em: 12/08/2019
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5. Studies Toward the Synthesis of Caramboxin Analogues
Intrigued by the recent discovery of caramboxin by Brazilian researchers, we present the results from our studies toward the racemic synthesis of caramboxin analogs through the ortho-carboxylation of 3,5-dimethoxy benzyl derivatives. Three different approaches were tested, and the route involving a Vilsmeier-Haack formylation followed by a Lindgren oxidation
J. Braz. Chem. Soc.. Publicado em: 2019-03
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6. Biodiesel Synthesis: Influence of Alkaline Catalysts in Methanol-Oil Dispersion
Biodiesel synthesis from soybean oil using methanol and alkaline catalysts occurs in the following two consecutive steps: dispersion of methanol in the oil and methanolysis. The effect of the alkaline catalysts NaOCH3, KOCH3, NaOH, and KOH in the dispersion step at 30-60 ºC and under mechanical stirring at 400 rpm was evaluated. The dispersion step accounts
J. Braz. Chem. Soc.. Publicado em: 2019-02
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7. Synthesis, Antimicrobial Activity and Structure-Activity Relationship of Some 5-Arylidene-thiazolidine-2,4-dione Derivatives
Derivatives of the thiazolidine-2,4-dione core represent a heterocyclic class with several correlated properties. In this context, the synthesis of structural analogues of these bioactive substances becomes attractive in the field of medicinal chemistry. These analogues act as antimicrobial agents against Gram-positives pathogens. The present work aimed to s
J. Braz. Chem. Soc.. Publicado em: 2019-01
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8. Synthesis and in vitro anti-HIV-1 evaluation of some N-arylsulfonyl-3-formylindoles
As our ongoing work on research of anti-HIV-1 inhibitors, fifteen N-arylsulfonyl-3-formylindoles (3a-o) were designed and prepared through two step synthetic route. Firstly, 3-formylindoles (2a-c) were synthesized via the Vilsmeier-Haack reaction. Subsequently, treatment of 2a-c with the appropriate arylsulfonyl chlorides led to the corresponding target comp
Braz. J. Pharm. Sci.. Publicado em: 29/11/2018
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9. Synthesis and Antibacterial Evaluation of 2-Ethyl-1-(4-substituted)phenyl-1 H-imidazole Derivatives as Open-Chain Analogues of 7-Alkoxyl-4,5-dihydro-imidazo[1,2-a]quinolines
A novel series of 2-ethyl-1-(4-substituted)phenyl-1H-imidazole derivatives was designed, synthesized, and tested for its antibacterial activity against various bacterial strains. Most of the synthesized compounds showed potent inhibition of several Gram-positive and Gram-negative bacterial strains with minimum inhibitory concentration (MIC) values in the ran
J. Braz. Chem. Soc.. Publicado em: 2018-04
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10. Molecular docking, synthesis and in vitro antimalarial evaluation of certain novel curcumin analogues
ABSTRACT The receptor protein PfATP6 has been identified as the common target of artemisinin and curcumin. The work was initiated to assess the antimalarial activity of six curcumin derivatives based on their binding affinities and correlating the in silico docking outcome with in vitro antimalarial screening results. A ligand library of thirty two Knoevenag
Braz. J. Pharm. Sci.. Publicado em: 08/01/2018
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11. Design, Synthesis and Anticancer Biological Evaluation of Novel 1,4-Diaryl-1,2,3-triazole Retinoid Analogues of Tamibarotene (AM80)
We report herein the design and synthesis via click chemistry of twelve novel triazole retinoid analogues of tamibarotene (AM80) and the evaluation of their anticancer activities against six cancer cell lines: HL60, K562, 786, HT29, MCF7 and PC3. Among the synthesized compounds, two were more potent than tamibarotene against solid tumor cells, and one of the
J. Braz. Chem. Soc.. Publicado em: 2018-01
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12. Chiral Bistacrine Analogues: Synthesis, Cholinesterase Inhibitory Activity and a Molecular Modeling Approach
Cholinesterase enzymes are important targets for the therapy of Alzheimer’s disease. Tacrine-based dual binding site cholinesterases inhibitors are potential disease-modifying anti-Alzheimer drug candidates. In the present work, we described the synthesis of a series of chiral homo- and heterodimers of bis(7)-tacrine connected by a heptylene chain as a spa
J. Braz. Chem. Soc.. Publicado em: 2017-11