505082-83-7Relevant academic research and scientific papers
Design, synthesis, and structure-activity relationship studies of L-amino alcohol derivatives as broad-spectrum antifungal agents
Zhao, Liyu,Tian, Linfeng,Sun, Nannan,Sun, Yin,Chen, Yixuan,Wang, Xinran,Zhao, Shizhen,Su, Xin,Zhao, Dongmei,Cheng, Maosheng
, p. 374 - 385 (2019/06/05)
To discover broad spectrum antifungal agents, two strategies were applied, and a novel class of L-amino alcohol derivatives were designed and synthesized. 3-F substituted compounds 14i, 14n, 14s and 14v exhibited excellent antifungal activities with broad antifungal spectra against C. albicans and C. tropicalis, with MIC values in the range of 0.03–0.06 μg/mL, and against A. fumigatus and C. neoformans, with MIC values in the range of 1–2 μg/mL. Notably, Compounds 14i, 14n, 14s and 14v also displayed moderate activities against fluconazole-resistance strains 17# and CaR that were isolated from AIDS patients. Moreover, only compounds in the S-configuration showed antifungal activity. Preliminary mechanistic studies showed that the potent antifungal activity of compound 14v stemmed from inhibition of C. albicans CYP51. Compounds 14n and 14v were almost nontoxic to mammalian A549 cells, and their stability in human plasma was excellent.
Design, synthesis and evaluation of biphenyl imidazole analogues as potent antifungal agents
Zhao, Shizhen,Zhao, Liyu,Zhang, Xiangqian,Wei, Peng,Wu, Mengya,Su, Xin,Sun, Bin,Zhao, Dongmei,Cheng, Maosheng
supporting information, p. 2448 - 2451 (2019/07/30)
To further explore the structure activity relationships (SARs) of our previously discovered antifungal lead compound (1), a series of biphenyl imidazole analogues were designed, synthesized and evaluated for their in vitro antifungal activity. Many of the
Rational development of 4-aminopyridyl-based inhibitors targeting trypanosoma cruzi CYP51 as anti-chagas agents
Choi, Jun Yong,Calvet, Claudia M.,Gunatilleke, Shamila S.,Ruiz, Claudia,Cameron, Michael D.,McKerrow, James H.,Podust, Larissa M.,Roush, William R.
, p. 7651 - 7668 (2013/11/06)
A new series of 4-aminopyridyl-based lead inhibitors targeting Trypanosoma cruzi CYP51 (TcCYP51) has been developed using structure-based drug design as well as structure-property relationship (SPR) analyses. The screening hit starting point, LP10 (KD ≤ 42 nM; EC50 = 0.65 μM), has been optimized to give the potential leads 14t, 27i, 27q, 27r, and 27t, which have low-nanomolar binding affinity to TcCYP51 and significant activity against T. cruzi amastigotes cultured in human myoblasts (EC50 = 14-18 nM for 27i and 27r). Many of the optimized compounds have improved microsome stability, and most are selective against human CYPs 1A2, 2D6, and 3A4 (50% inhibition at 1 μM). A rationale for the improvement in microsome stability and selectivity of inhibitors against human metabolic CYP enzymes is presented. In addition, the binding mode of 14t with the Trypanosoma brucei CYP51 (TbCYP51) orthologue has been characterized by X-ray structure analysis.
Amine Compounds
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Page/Page column 180, (2008/12/08)
There is provided a compound exhibiting an activity of suppressing immune response with reduced adverse drug reactions, which compound is useful in the chemotherapy for preventing or treating, for example, a wide range of various autoimmune diseases including systemic erythematodes, chronic rheumatoid arthritis, Type I diabetes, inflammatory bowel disease, biliary cirrhosis, uveitis, multiple sclerosis or other disorders, or chronic inflammatory diseases, or cancers, lymphoma or leukemia, or resistance to organ or tissue transplantation or rejection against transplantation. Novel amine compounds having an S1P1/Edg1 receptor agonist effect, possible stereoisomers or racemic bodies of the compounds, or pharmacologically acceptable salts, hydrates or solvates of the compound, the stereoisomers or the racemic bodies, or prodrugs of the compounds, the stereoisomers, the racemic bodies, the salts, the hydrates or the solvates, are provided.
INDANE DERIVATES AS MUSCARINIC RECEPTOR AGONISTS
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Page 13, (2010/02/10)
The present invention relates to compounds of Formula I: I which are agonists of the M-1 muscarinic receptor.
MUSCARINIC AGONISTS
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Page 14, (2010/02/09)
The present invention relates to compounds of Formula (I): which are agonists of the M-1 muscarinic receptor.
MUSCARINIC AGONISTS
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Page 14, (2010/02/09)
The present invention relates to compounds of Formula (I): which are agonists of the M-1 muscarinic receptor.
