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1.
MycoKeys ; (45): 41-56, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30728745

RESUMO

A new Talaromyces species, T.amyrossmaniae, isolated from decaying fruit and litter of Terminalia bellerica, is described and illustrated. On the natural substrate, the new species produces determinate synnemata, with a well-defined, vivid orange red to orange red cylindrical stipe, and a greyish green capitulum. Conidiophores are typically biverticillate, or sometimes have subterminal branches, with acerose phialides that produce globose to subglobose, smooth to slightly roughened conidia. Multigene phylogenetic analyses based on the internal transcribed spacer region (ITS), and partial sequences of ß-tubulin (BenA), calmodulin (CaM), and DNA directed RNA polymerase second large subunit (RPB2) genes, along with morphological characterization, revealed that these isolates are distinct and form a unique lineage of Talaromyces in section Trachyspermi, closely allied to T.aerius, T.albobiverticillius, T.heiheensis, T.erythromellis, and T.solicola. The new species T.amyrossmaniae is the first species in section Trachyspermi with determinate synnemata.

2.
Bioorg Med Chem Lett ; 25(4): 874-80, 2015 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-25592714

RESUMO

Herein, we report the synthesis and screening of linezolid-like Schiff bases as inhibitors of biofilm formation. The result of biofilm inhibition of Pseudomonas aeruginosa suggested that compounds 5h (IC50 value=12.97±0.33µM) and 5i (IC50 value=15.63±0.20µM) had more inhibitory activity when compared with standard linezolid (IC50=15.93±0.18µM) without affecting the growth of cells (and thus behave as anti-quorum sensing agents). The compounds 5h (MIC range=2.5-10µg/mL) and 5i (MIC range=3.5-10µg/mL) with 2-chloroquinolinyl and 2-chloro-8-methylquinolinyl motif, respectively, showed antibacterial activity in comparable range of linezolid (MIC range=2-3µg/mL) and were more potent when compared with ciprofloxacin (MIC range=25-50µg/mL). Thus, the active derivatives were not only potent inhibitors of P. aeruginosa biofilm growth but also efficient antibacterial agents. The docking study of most active compounds 5h and 5i against PqsD enzyme of P. aeruginosa exhibited good binding properties. In silico ADME properties of synthesized compounds were also analyzed and showed potential to develop as good oral drug candidates.


Assuntos
Acetamidas/farmacologia , Anti-Infecciosos/farmacologia , Biofilmes , Oxazolidinonas/farmacologia , Bases de Schiff/química , Acetamidas/química , Anti-Infecciosos/química , Simulação por Computador , Linezolida , Testes de Sensibilidade Microbiana , Microscopia Eletrônica de Varredura , Simulação de Acoplamento Molecular , Oxazolidinonas/química
3.
Bioorg Med Chem Lett ; 24(6): 1605-10, 2014 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-24513045

RESUMO

A series of N'-substitutedbenzylidene-2-(6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)acetohydrazide derivatives is synthesized and evaluated for antileishmanial activity against Leishmania donovani promastigotes. Compounds 9a and 9i were shown significant antileishmanial when compared with standard sodium stilbogluconate. Antimicrobial study revealed that compound 9b has potent as well as broad spectrum antibacterial activity when compared with ampicillin and compound 9e showed promising antifungal activity when compared with miconazole. Also, none of the synthesized compounds showed cytotoxicity up to tested concentration. Further, docking study against pteridine reductase 1 enzyme of L. donovani showed good binding interactions. ADME properties of synthesized compounds were also analyzed and showed potential to develop as good oral drug candidates.


Assuntos
Antiprotozoários/síntese química , Antiprotozoários/farmacologia , Compostos de Benzilideno/química , Hidrazinas/química , Hidrazinas/farmacologia , Leishmania donovani/efeitos dos fármacos , Piridinas/química , Administração Oral , Anti-Infecciosos/síntese química , Anti-Infecciosos/farmacocinética , Anti-Infecciosos/farmacologia , Antiprotozoários/farmacocinética , Sítios de Ligação , Desenho de Fármacos , Meia-Vida , Hidrazinas/farmacocinética , Leishmania donovani/enzimologia , Testes de Sensibilidade Microbiana , Simulação de Acoplamento Molecular , Oxirredutases/antagonistas & inibidores , Oxirredutases/metabolismo , Estrutura Terciária de Proteína , Proteínas de Protozoários/antagonistas & inibidores , Proteínas de Protozoários/metabolismo
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