15196-28-8Relevant articles and documents
Synthesis and antileishmanial activity of lipidic amino alcohols
Coimbra, Elaine S.,De Almeida, Mauro V.,Junior, Celso O. R.,Taveira, Aline F.,Da Costa, Cristiane F.,De Almeida, Ana C.,Reis, Elaine F. C.,Da Silva, Adilson D.
, p. 233 - 235 (2010)
In this work, a number of lipidic amino alcohols wereas synthesized and evaluated in vitro on cultures of Leishmania amazonensis and Leishmania chagasi. Nine amino alcohols showed inhibition of L. chagasi growth, and seven of them showed inhibition of L. amazonensis with IC50 below 10 μm. Compound 11f was more active than the reference drug amphotericin B against L. chagasi promastigote forms.
Antifungal activity of aminoalcohols and diamines against dermatophytes and yeast
Caneschi, César A.,de Oliveira, Bruno A.,de Almeida, Angelina M.,do Carmo, Renata P.,Martins, Francislene J.,de Almeida, Mauro V.,Raposo, Nádia R. B.
, p. 2164 - 2169 (2020)
Dermatomycoses are infections caused by fungi and yeasts and the drug treatment is considered expensive and extensive. Researchers are synthesizing new organic compounds in order to obtain more effective molecules that provide reduced adverse effects. Our research group has synthesized and evaluated the biological activities of aminoalcohol and diamine derivatives, which were considered active against human pathogenic fungi. Therefore, the objective of this study was to evaluate the in vitro antifungal activity of aminoalcohols and diamine derivatives against fungi and yeasts that cause dermatomycoses. The minimum inhibitory concentrations (MICs) and the minimum fungicidal concentration (MFC) of aminoalcohol (1–4) and diamine (5–13) derivatives was determined against Trichophyton mentagrophytes, T. rubrum, Epidermophyton floccosum, and Candida albicans according to protocols from the Clinical and Laboratory Standards Institute. All molecules exhibited fungicidal activity against the evaluated fungal strains, with the MIC and MFC ranging between 0.12 and 1000 μg/mL for filamentous fungi and 0.6 and 1250 μg/mL for yeasts. The best activity was attributed to diamines compared to aminoalcohols, with an emphasis on molecules 6 and 7. These results demonstrate the antifungal potential of the evaluated aminoalcohols and diamines against the four primary fungal species that cause dermatomycoses. [Figure not available: see fulltext.]
VANCOMYCIN DERIVATIVE, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE THEREOF
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, (2019/03/13)
Provided are a class of vancomycin derivatives with a structure as shown in the general formula below and pharmaceutically acceptable salts thereof, a preparation method, a pharmaceutical composition containing the compound thereof, and the use of these compounds in preparing drugs for treating and/or preventing bacterial infection diseases, in particular drugs for treating infection diseases caused by Gram-positive bacteria.
Lipophilic gold(I) complexes with 1,3,4-oxadiazol-2-thione or 1,3-thiazolidine-2-thione moieties: synthesis and their cytotoxic and antimicrobial activities
de Almeida, Angelina Maria,de Oliveira, Bruno Assis,de Castro, Pedro P?ssa,de Mendon?a, Camille Carvalho,Furtado, Ricardo Andrade,Nicolella, Heloiza Diniz,da Silva, Vania Lúcia,Diniz, Cláudio Galuppo,Tavares, Denise Crispim,Silva, Heveline,de Almeida, Mauro Vieira
, p. 841 - 857 (2017/10/07)
Novel lipophilic gold(I) complexes containing 1,3,4-oxadiazol-2-thione or 1,3-thiazolidine-2-thione derivatives were synthesized and characterized by IR, high resolution mass spectrometry, and 1H, 13C 31P NMR. The cytotoxicity of the compounds was evaluated considering cisplatin and/or auranofin as reference in different tumor cell lines: colon cancer (CT26WT), metastatic skin melanoma (B16F10), breast adenocarcinoma (MCF-7), cervical carcinoma (HeLa), glioblastoma (M059?J). Normal human lung fibroblasts (GM07492-A) and kidney normal cell (BHK-21) were also evaluated. The gold(I) complexes were more active than their respective free ligands and cisplatin. Furthermore, antibacterial activity was evaluated against Gram-positive bacteria Staphylococcus aureus ATCC 25213, Staphylococcus epidermidis ATCC 12228 and Gram-negative bacteria Escherichia coli ATCC 11229 and Pseudomonas aeruginosa ATCC 27853 and expressed as the minimum inhibitory concentration (MIC). The complexes exhibited lower MIC values when compared to the ligands and chloramphenicol against Gram-positive bacteria and Gram-negative bacteria. Escherichia coli was sensitive one to the action of gold(I) complexes.