669015-01-4Relevant 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.
SUBSTITUTED PYRIMIDINE COMPOUND AND USES THEREOF
-
, (2015/09/23)
Disclosed is a substituted pyrimidine compound having a structure as represented by formula PY. See the description for the definition of each substituent in the formula.The compound of the present invention provides broad-spectrum bactericidal, pesticidal, and acaricidal activities, provides great control effects against plant diseases such as cucumber downy mildew,corn rust,wheat powdery mildew, rice blast,and cucumber gray mold, specifically provides improved control effects against cucumber downy mildew, corn rust, wheat powdery mildew, and rice blast, provides great control effects against aphid, carmine spider mite, diamondback moth, and armyworm, and acquires great effects at a minimal dosage.The compound of the present invention aloso provides characteristics such as a simplified preparation method.
2,5-DIOXOIMIDAZOLIDIN-4-YL ACETAMIDES AND ANALOGUES AS INHIBITORS OF METALLOPROTEINASE MMP12.
-
Page 59, (2010/02/06)
The invention provides compounds of formula (I) in which L, X, Y, Z1, Z2, R1, R2, R3 and G2 have the meanings defined in the specification; processes for their preparation; pharmaceutical c
