915920-85-3Relevant academic research and scientific papers
COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
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Paragraph 0055; 0060; 0071, (2022/01/03)
The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the present disclosure, and their use as a medicament, in particular for the treatment of ne
Synthesis and evaluation of the in vitro antimicrobial activity of triazoles, morpholines and thiosemicarbazones
Andradeb, Jéssica T.,Araújoc, Marcelo G. F.,Carmo, Lucas F.,Fernandesa, Joice S.,Ferreirab, Jaqueline M. S.,Santosa, Felipe R. S.,Sousab, Carla D. F.,Villar, José A. F. P.
, p. 38 - 50 (2019/07/12)
Background: Microbial infections is a global public health problem. The aim of this work was to synthesize and evaluate the antimicrobial activity of novel triazoles, morpholines and thiosemicarbazones. Methods: Compounds were synthesized using 2,4-Dihydroxyacetophenone and 4-hydroxybenzaldehyde as starting materials. The antimicrobial activity of these compounds against bacteria and yeast was evaluated by the broth microdilution method. Results: The proposed route for synthesis gave high to moderate yields, moreover these compounds were successfully characterized by 1H NMR, 13C NMR and LC-MS. Antimicrobial testing indicated that the thiosemicarbazone and morphine derivatives had the best antimicrobial activity against the microorganisms tested with minimum inhibitory concentrations (MIC) between 0.29 and 5.30 μM. Thiosemicarbazone derivative (12) was able to inhibit the growth of C. tropicalis, with minimum fungicidal concentration (MFC) of 0.55 μM. In addition, this compound was active against E. coli, S. aureus and S. epidermidis, with MIC values ranging from 0.29 to 1.11 μM. Moreover, the morpholine derivative (15) had an MIC value of 0.83 μM against C. albicans and E. coli. Conclusion: We have efficiently synthesized a series of eleven novel triazoles, thiosemicarbazones and morpholine derivatives using 2,4-Dihydroxyacetophenone and 4-hydroxybenzaldehyde as starting materials. Thiosemicarbazone derivative (12) showed promising antifungal and antibacterial activity and these findings suggest that this compound can be used as scaffolds to design new antimicrobial drugs.
Synthesis, antimalarial activity and cytotoxic potential of new monocarbonyl analogues of curcumin
Manohar, Sunny,Khan, Shabana I.,Kandi, Shamseer Kulangara,Raj, Kranthi,Sun, Guojing,Yang, Xiaochuan,Calderon Molina, Angie D.,Ni, Nanting,Wang, Binghe,Rawat, Diwan S.
supporting information, p. 112 - 116 (2013/02/23)
A series of novel monocarbonyl analogues of curcumin have been designed, synthesized and tested for their activity against Molt4, HeLa, PC3, DU145 and KB cancer cell lines. Six of the analogues showed potent cytotoxicity towards these cell lines with IC50 values below 1 μM, which is better than doxorubicin, a US FDA approved drug. Several analogues were also found to be active against both CQ-resistant (W2 clone) and CQ-sensitive (D6) strains of Plasmodium falciparum in an in-vitro antimalarial screening. This level of activity warrants further investigation of the compounds for development as anticancer and antimalarial agents.
