96690-02-7Relevant articles and documents
Synthesis, biological evaluation, and molecular docking studies of deoxygenated C-glycosides as LpxC inhibitors
Dreger, Alexander,Hoff, Katharina,Agoglitta, Oriana,Bülbül, Emre F.,Melesina, Jelena,Sippl, Wolfgang,Holl, Ralph
, (2021/11/11)
The bacterial deacetylase LpxC is a promising target for the development of novel antibiotics being selectively active against Gram-negative bacteria. In chiral pool syntheses starting from D- and L-ribose, a series regio- and stereoisomeric monohydroxyte
Highly regioselective and stereoselective synthesis of C-Aryl glycosidesvianickel-catalyzedortho-C-H glycosylation of 8-aminoquinoline benzamides
Chen, Xi,Ding, Ya-Nan,Gou, Xue-Ya,Liang, Yong-Min,Luan, Yu-Yong,Niu, Zhi-Jie,Shi, Wei-Yu,Zhang, Zhe,Zheng, Nian
supporting information, p. 8945 - 8948 (2021/09/10)
C-Aryl glycosides are of high value as drug candidates. Here a novel and cost-effective nickel catalyzedortho-CAr-H glycosylation reaction with high regioselectivity and excellent α-selectivity is described. This method shows great functional group compatibility with various glycosides, showing its synthetic potential. Mechanistic studies indicate that C-H activation could be the rate-determining step.
Stereoselective synthesis of selenium-containing glycoconjugates via the mitsunobu reaction
Cermola, Flavio,De Nisco, Mauro,Manfra, Michele,Pedatella, Silvana,Serpico, Luigia
, (2021/05/26)
A simple and efficient route for the synthesis of new glycoconjugates has been developed. The approach acts as a model for a mini-library of compounds with a deoxy-selenosugar core joined to a polyphenolic moiety with well-known antioxidant properties. An unexpected stereocontrol detected in the Mitsunobu key reaction led to the most attractive product showing a natural Dconfiguration. Thus, we were able to obtain the target molecules from the commercially available D-ribose via a shorter and convenient sequence of reactions.
POLYMORPHIC COMPOUNDS AND USES THEREOF
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Paragraph 0279-0280, (2020/04/10)
The present invention provides compounds and methods of use thereof for treatment of certain disorders and conditions, for example brain injuries such as stroke or traumatic brain injuries.
DERIVATIVES OF GLYCERO-MANNO-HEPTOSE ADP FOR USE IN MODULATING IMMUNE RESPONSE
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Paragraph 295; 296, (2020/11/04)
The disclosure provides compounds, compositions and methods related to activating alpha-kinase 1 (ALPK1) for modulating an immune response and treating or preventing cancer, infection, inflammation and related diseases and disorders as well as potentiating an immune response to a target antigen. The disclosure also provides heterocyclic compounds of formula (I) as agonists of alpha protein kinase 1 (ALPK1) and their use in activating ALPK1, modulating an immune response and treating diseases such as cancer, wherein A1, A2, L1, L2, L3, Z1, Z2, W1, W2, R1, R2, R3, R4, R5, R6 and R7 are as defined herein.
COMPOUNDS AND METHODS FOR TREATING ADDICTION AND RELATED DISORDERS
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Paragraph 00168, (2019/08/29)
The present invention relates to compounds and methods of use thereof for treatment of certain disorders and conditions, for example an addiction or compulsive disorder.
Chiral Pool Synthesis, Biological Evaluation and Molecular Docking Studies of C-Furanosidic LpxC Inhibitors
Dreger, Alexander,Kharwb, Omar,Agoglitta, Oriana,Bülbül, Emre F.,Melesina, Jelena,Sippl, Wolfgang,Holl, Ralph
, (2019/03/17)
Inhibitors of the bacterial deacetylase LpxC are a promising class of novel antibiotics, being selectively active against Gram-negative bacteria. To improve the biological activity of reported C-furanosidic LpxC inhibitors, the stereochemistry at positions 3 and 4 of the tetrahydrofuran ring was varied. In chiral pool syntheses starting from d-gulono-γ-lactone and d-ribose, a series of (3S,4R)-configured dihydroxytetrahydrofuran derivatives was obtained, of which the (2S,5S)-configured hydroxamic acid 15 ((2S,3S,4R,5S)-N,3,4-trihydroxy-5-(4-{[4-(morpholinomethyl)phenyl]ethynyl}phenyl)tetrahydrofuran-2-carboxamide) was found to be the most potent LpxC inhibitor (Ki=0.4 μm), exhibiting the highest antibacterial activity against E. coli BL21 (DE3) and the D22 strain. Additionally, molecular docking studies were performed to rationalize the obtained structure–activity relationships.
Compounds and methods for treating neurological and cardiovascular conditions
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Page/Page column 101; 102, (2017/11/09)
The present invention relates to compounds and methods of use thereof for treatment of certain disorders and conditions, for example brain injuries such as stroke or traumatic brain injuries.
NON-RIBOSE CONTAINING INHIBITORS OF HISTONE METHYLTRANSFERASE DOT1L FOR CANCER TREATMENT
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Paragraph 0062; 0063, (2015/02/19)
A compound of Formula I, a pharmaceutically acceptable salt thereof, a prodrug thereof, or combinations thereof: wherein R1 is H, methyl, or benzyl: R2 is 2-cyanoethyl, 2-methoxycarbonylethyl, or 2-iodoethyl; X is N or S; wherein if
Synthesis, activity and metabolic stability of non-ribose containing inhibitors of histone methyltransferase DOT1L
Deng, Lisheng,Zhang, Li,Yao, Yuan,Wang, Cong,Redell, Michele S.,Dong, Shuo,Song, Yongcheng
, p. 822 - 826 (2013/08/26)
Histone methyltransferase DOT1L is a drug target for MLL leukemia. We report an efficient synthesis of a cyclopentane-containing compound that potently and selectively inhibits DOT1L (Ki = 1.1 nM) as well as H3K79 methylation (IC50 ～
