5538-95-4Relevant academic research and scientific papers
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 (2020/09/29)
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.]
Diamine derivative anti-Trichomonas vaginalis and anti-Tritrichomonas foetus activities by effect on polyamine metabolism
Rigo, Graziela Vargas,Trein, Márcia Rodrigues,da Silva Trentin, Danielle,Macedo, Alexandre José,de Oliveira, Bruno Assis,de Almeida, Angelina Maria,Giordani, Raquel Brandt,de Almeida, Mauro Vieira,Tasca, Tiana
, p. 847 - 855 (2017/09/13)
Human and bovine trichomoniasis are sexually transmitted diseases (STD) caused by Trichomonas vaginalis and Tritrichomonas foetus, respectively. Human trichomoniasis is the most common non-viral STD in the world and bovine trichomoniasis causes significant economic losses to breeders. Considering the significant impact of the infections caused by these protozoa and the treatment failures, the search for new therapeutic alternatives becomes crucial. In this study the effect of diamines and amino alcohols in the in vitro viability of trichomonads was evaluated. Screening demonstrated the high activity of diamine 4 against these protozoa. Although cytotoxicity against HMVII cell line and slight hemolysis were observed in vitro, the compound showed no toxic effect on the Galleria mellonella in vivo model. Importantly, diamine 4 was active against both trichomonads species at 6 h and 24 h of incubation, and these effects was reverted by putrescine, a polyamine, suggesting competition for the same metabolic pathway. These findings indicate that the mechanism of action of diamine 4 is through the polyamine metabolism, a pathway distinct from that presented by metronidazole, the drug usually used to treat trichomoniasis and to which resistance is widely reported. These data demonstrate the importance of diamines as potential novel candidates as anti-T. vaginalis and anti-T. foetus agents.
Synthesis and evaluation of antibacterial and antitumor activities of new galactopyranosylated amino alcohols
De Souza Fernandes, Fábio,Fernandes, Tayrine Silva,Da Silveira, Lígia Souza,Caneschi, Wiliam,Louren?o, Maria Cristina S.,Diniz, Claudio G.,De Oliveira, Pollyanna Francielli,Martins, Sabrina De Paula Lima,Pereira, Daiane Eleutério,Tavares, Denise Crispim,Le Hyaric, Mireille,De Almeida, Mauro V.,Couri, Mara Rubia C.
, p. 203 - 210 (2015/12/08)
Three series of d-galactose derivatives linked to a lipophilic aminoalcohol moiety were synthesized and their antibacterial activity was evaluated against Mycobacterium tuberculosis and representative species of Gram positive and Gram negative bacteria. Five out of the thirteen tested compounds displayed activity against M. tuberculosis, with a minimal inhibitory concentration (MIC) of 12.5 μg/mL and seven compounds were active against the four bacterial strains tested. The best results were obtained for amino alcohols 10 and 11 against Staphylococcus epidermidis (MIC Combining double low line 2 μg/mL). The antitumor activity was evaluated against three tumor cell lines (MCF-7, HeLa and MO59J) and compared to the normal cell line GM07492A. The results showed that the lowest IC50 values were observed for the amino alcohol 16 against MCF-7 (11.9 μM) and MO59J (10.0 μM).
Synthesis and antitubercular activity of lipophilic moxifloxacin and gatifloxacin derivatives
de Almeida, Mauro V.,Saraiva, Mauricio F.,de Souza, Marcus V.N.,da Costa, Cristiane F.,Vicente, Felipe R.C.,Lourenco, Maria C.S.
, p. 5661 - 5664 (2008/03/14)
Fluoroquinolone (FQ) has a broad spectrum of activity against several bacteria, mycobacteria, parasites, and other diseases. Moxifloxacin and gatifloxacin are a new generation of fluoroquinolone agents with improved activity against Gram-negative and positive bacteria. As lipophilicity is an important consideration in the design and activity of novel antibacterial agents, we report in this work the synthesis and biological evaluation of 12 lipophilic moxifloxacin or gatifloxacin derivatives, by reaction of 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxoquinoline-3-carboxylic acid 13 with severals N-monoalkyl 1,2-ethanediamine or 1,3-propanediamine.
