521286-38-4Relevant academic research and scientific papers
Optimization and Evaluation of Novel Antifungal Agents for the Treatment of Fungal Infection
Bahn, Yong-Sun,Cheong, Eunji,Choi, Ji Won,Jang, Bo Ko,Kim, Dahee,Kim, Hyeon Jeong,Kim, Hyeon Ji,Kim, Siwon,Lee, Dong-Gi,Lee, Jong-Seung,Lee, Kyung-Tae,Lee, Myung Ha,Lee, Ye Rim,Park, Jong-Hyun,Park, Ki Duk,Park, Sun Jun,Seo, Kyung Jin,Yeon, Seul Ki
supporting information, p. 15912 - 15935 (2021/11/10)
Due to the increased morbidity and mortality by fungal infections and the emergence of severe antifungal resistance, there is an urgent need for new antifungal agents. Here, we screened for antifungal activity in our in-house library through the minimum inhibitory concentration test and derived two hit compounds with moderate antifungal activities. The hit compounds' antifungal activities and drug-like properties were optimized by substituting various aryl ring, alkyl chain, and methyl groups. Among the optimized compounds, 22h was the most promising candidate with good drug-like properties and exhibited potent fast-acting fungicidal antifungal effects against various fungal pathogens and synergistic antifungal activities with some known antifungal drugs. Additionally, 22h was further confirmed to disturb fungal cell wall integrity by activating multiple cell wall integrity pathways. Furthermore, 22h exerted significant antifungal efficacy in both the subcutaneous infection mouse model and ex vivo human nail infection model.
FUNCTIONAL DERIVATIVE COMPOUNDS OF ALANINE AND PROLINE AMINO ACIDS AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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Paragraph 0043-0044; 0057; 0058, (2019/09/15)
The present invention relates to novel functional derivatives of alanine and proline amino acids. The compounds of the present invention were confirmed to have a very superior antifungal or fungicidal effect. In addition, the compounds of the present inve
RENIN INHIBITING COMPOUNDS
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, (2008/06/13)
Compounds which are amino acid derivatives and have the formula STR1 in which R 1 is hydrogen or methyl, R 2 is ethyl, propyl or imidazol-4-yl, R 3 is isobutyl, cyclohexylmethyl or benzyl, and A is defined as herein are useful as renin inhibitors.
