1115-59-9Relevant articles and documents
Silver ion-induced chiral enhancement by argentivorous molecules
Lee, Eunji,Hosoi, Yasuhiro,Temma, Honoka,Ju, Huiyeong,Ikeda, Mari,Kuwahara, Shunsuke,Habata, Yoichi
, p. 3373 - 3376 (2020)
Optically active tetra-armed cyclens with an asymmetric chiral centre in the cyclen moiety were synthesized and were shown to enhance chirality and control of enantiomers on complexation with Ag+. Binding studies of the Ag+ complex demonstrated that Ag+ preferentially interacts with electron-rich substituents over other aromatic substituents.
Synthesis of 2-(5-Hydroxymethyl-2-formylpyrrol-1-yl)propionic acid lactone
Bu, Xiaolin,Li, Yueqing,Liu, Jihong,Zeng, Debin,Zhao, Weijie
, p. 194 - 197 (2012)
2-(5-Hydroxymethyl-2-formylpyrrol-1-yl)propionic acid lactone was synthesized in six steps with a 17.0% overall yield, starting from L-alanine. The synthetic route involved the Clauson-Kaas reaction, Vilsmeier reaction, and transesterification. The transesterification was the key step in the formation of the target compound.
Evidence for the optical signalling of changes in bicarbonate concentration within the mitochondrial region of living cells
Smith, David G.,Law, Ga-Lai,Murray, Benjamin S.,Pal, Robert,Parker, David,Wong, Ka-Leung
, p. 7347 - 7349 (2011)
Image and spectral intensity from bicarbonate-selective europium(iii) probes localised in the mitochondria of cells is modulated reversibly by variation of external pCO2, and is suppressed by addition of the carbonic anhydrase inhibitor, acetazolomide.
Novel naphthylamide derivatives as dual-target antifungal inhibitors: Design, synthesis and biological evaluation
An, Yunfei,Dong, Yue,Liu, Min,Han, Jun,Zhao, Liyu,Sun, Bin
, (2020/11/13)
Fungal infections have become a serious medical problem due to the high infection rate and the frequent emergence of drug resistance. Squalene epoxidase (SE) and 14α-demethylase (CYP51) are considered as the important antifungal targets, they can show the synergistic effect on antifungal therapy. In the study, a series of active fragments were screened through the method of De Novo Link, and these active fragments with the higher Ludi_Scores were selected, which can show the obvious binding ability with the dual targets (SE, CYP51). Subsequently, three series of target compounds with naphthyl amide scaffolds were constructed by connecting these core fragments, and their structures were synthesized. Most of compounds showed the antifungal activity in the treatment of pathogenic fungi. It was worth noting that compounds 10b-5 and 17a-2 with the excellent broad-spectrum antifungal properties also exhibited the obvious antifungal effects against drug-resistant fungi. Preliminary mechanism study has proved these target compounds can block the biosynthesis of ergosterol by inhibiting the activity of dual targets (SE, CYP51). Furthermore, target compounds 10–5 and 17a-2 with low toxicity side effects also demonstrated the excellent pharmacological effects in vivo. The molecular docking and ADMET prediction were performed, which can guide the optimization of subsequent lead compounds.
Potent arylamide derivatives as dual-target antifungal agents: Design, synthesis, biological evaluation, and molecular docking studies
An, Yunfei,Dong, Yue,Han, Jun,Liu, Min,Liu, Xinyong,Sun, Bin
, (2020/03/27)
Fungal infections have become a serious medical problem due to the high infection rate and the frequent emergence of drug resistance. Ergosterol is an important structural component of the fungal cell membrane, its synthetases (squalene epoxidase (SE) and 14α-demethylase (CYP51)) are considered as the key points to block the ergosterol synthesis. In this study, we designed a series of dual-target arylamides derivatives based on the analysis of active sites (SE, CYP51). Subsequently, these target compounds were synthesized, and their antifungal activity was evaluated. Most of compounds demonstrate the potent antifungal activity against multiple Candida spp. and A. fum. In particular, the antifungal activities of compounds 10b and 11c are not only superior to positive control drugs, but also have significant inhibitory effects on drug-resistant fungi (C.alb. Strain100, C.alb. Strain103). Therefore, their action mechanism was further studied. Cellular uptake and electron microscopy observation showed that target compounds were able to enter fungal cytoplasmic region through free diffusion, and destroyed cell membrane structure. At the same time, preliminary mechanisms have demonstrated that they can affect the synthesis of ergosterol by inhibiting the activity of dual targets. It is worth noting that they also can exhibit excellent antifungal activity and low toxic side effects in vivo. Their ADMET properties and binding models were established will be useful for further lead optimization.
