864528-04-1Relevant articles and documents
An efficient synthesis of 4,6-diarylnicotinonitrile-acetamide hybrids via 1,2,3-triazole linker as multitarget microbial inhibitors
El-Sayed, Hassan A.,Moustafa, Ahmed H.,Masry, Asmaa A.,Amer, Atef M.,Mohammed, Samar M.
, p. 275 - 285 (2021/10/21)
An efficient and smart approach for design and synthesis of a novel series of nicotinonitrile-1,2,3-triazole-acetamide hybrids was described. The synthetic methodology was commenced with preparation of acetylene derivatives via alkynylation of 2-oxonicotinonitrile with propargyl bromide under mild basic catalyst (pot. carbonate). The facile click cycloaddition reaction of alkynes 2a-f and azido-acetamides 3-5 in the presence of catalytic Cu(I) in H2O/tetrahydrofuran (THF) was utilized for the synthesis of target molecules 6a-l. Triazoles 6c, d, f, and 6i have highly activity against the four pathogenic bacteria (Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, and Staphylococcus aureus) and two pathogenic fungi (Candida albicans and Aspergillus flavus) with minimum inhibitory concentration (MIC) in between 0.5 and 4?μg/ml for bacteria and 0.5 and 8?μg/ml for fungi.
Synthesis of arylfuran derivatives as potential antibacterial agents
Andrade, Marina M. S.,Protti, ícaro F.,Maltarollo, Vinícius G.,da Costa, Ygor F. G.,de Moraes, Wesley G.,Moreira, Nicole F.,Garcia, Giovana G.,Caran, Gabriel F.,Ottoni, Flaviano M.,Alves, Ricardo J.,Moreira, Carolina P. S.,Martins, Helen R.,Alves, Maria Silvana,de Oliveira, Renata B.
, p. 1074 - 1086 (2021/02/26)
Bacterial infections represent a serious health care problem mainly due to the misuse and overuse of antibiotics, with consequent emergence of multidrug resistant bacterial strains. Then, because the urgent need to find novel and alternative antibacterial agents, the present work focuses on the synthesis of arylfuran derivatives with potential antimicrobial activity. Eighteen arylfuran derivatives were synthesized and evaluated for their antibacterial activity against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. Among them, seven compounds containing an amino group in their structure showed activity, with compound 24 being the most effective against both Gram-negative (E. coli, MIC = 49 μM) and Gram-positive (S. aureus, MIC = 98 μM) bacteria, besides having exhibited a modest activity against P. aeruginosa (MIC = 770 μM). In addition, based on in silico studies, this is a druglike compound since it does not violate any rules for predicting oral bioavailability. In this context, the significant antibacterial potential and the low similarity with known antibiotics indicate the innovative aspect of compound 24.
Identification of Phenylphthalazinones as a New Class of Leishmania infantum Inhibitors
Sijm, Maarten,de Heuvel, Erik,Matheeussen, An,Caljon, Guy,Maes, Louis,Sterk, Geert-Jan,de Esch, Iwan J. P.,Leurs, Rob
supporting information, p. 219 - 227 (2019/12/27)
Leishmaniasis is a neglected parasitic disease caused by over 20 different Leishmania species. Current treatments often rely on harsh regimes of pentavalent antimonials such as sodium stibogluconate, while more recent drugs suffer other shortcomings such
