41013-93-8Relevant academic research and scientific papers
Design, synthesis and biological evaluation of benzamide derivatives as novel NTCP inhibitors that induce apoptosis in HepG2 cells
Zhao, Shuangmei,Zhen, Yongqi,Fu, Leilei,Gao, Feng,Zhou, Xianli,Huang, Shuai,Zhang, Lan
supporting information, (2019/08/20)
Sodium taurocholate cotransport polypeptide (NTCP) plays an important role in the development of hepatitis and acts as a switch to allow hepatitis virus to enter hepatic cells. As the entry receptor protein of hepatitis virus, NTCP is also an effective ta
Inhibition of Ebola virus infection: Identification of niemann-pick C1 as the target by optimization of a chemical probe
Lee, Kyungae,Ren, Tao,Co?té, Marceline,Gholamreza, Berahman,Misasi, John,Bruchez, Anna,Cunningham, James
supporting information, p. 239 - 243 (2013/03/28)
A high-throughput screen identified adamantane dipeptide 1 as an inhibitor of Ebola virus (EboV) infection. Hit-to-lead optimization to determine the structure-activity relationship (SAR) identified the more potent EboV inhibitor 2 and a photoaffinity labeling agent 3. These antiviral compounds were employed to identify the target as Niemann-Pick C1 (NPC1), a host protein that binds the EboV glycoprotein and is essential for infection. These studies establish NPC1 as a promising target for antiviral therapy.
Design and synthesis of novel N-benzylidenesulfonohydrazide inhibitors of murC and murD as potential antibacterial agents
Frlan, Rok,Kovac, Andreja,Blanot, Didier,Gobec, Stanislav,Pecar, Slavko,Obreza, Ales
, p. 11 - 30 (2008/09/16)
A series of novel N-benzylidenesulfonohydrazide compounds were designed and synthesized as inhibitors of UDP-N-acetylmuramic acid:L-alanine ligase (MurC) and UDP-N-acetylmuramoyl-L-alanine:D-glutamate ligase (MurD) from E. coli, involved in the biosynthes
New arylsulfonohydrazide inhibitors of enzymes MurC and MurD
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Page/Page column 32, (2008/06/13)
This invention belongs to the field of pharmaceutical chemistry and relates to new arylsulfonohydrazides as inhibitors of UDP-N-acetylmuramyl:L-alanine ligaze (MurC) and UDP-N-acetylmuramyl-L-alanine:D-glutamate ligaze (MurD), to procedures for their preparation and pharmaceutical preparations containing the same. The enzymes MurC and MurD are the key enzymes involved in the synthesis of bacterial peptidoglycan, so arylsulfonohydrazide inhibitors possess antibacterial activity. Compounds of general formula I and the pharmaceutically acceptable salts are described. The appropriate substituents are clearly presented in the body of the text and in claims.
Synthesis of heterocycles with MF/Al2O3 base-systems: 2-arylbenzofuranes and 2,3-diarylisoquinolin-1(2H)-ones
Hellwinkel,Goke
, p. 1135 - 1141 (2007/10/02)
2-Benzyloxybenzaldehydes, -acetophenones and -benzophenones substituted in the benzyl part with electron-withdrawing groups, cyclize easily to 2-arylbenzofuranes by using a standardized KF- or CsF-Al2O3 base system. An efficient one-pot synthesis for 2,3-diarylisoquinolin-1(2H)-ones is possible by reacting a variety of arene carbaldehyde anils with phthalides under the same reaction conditions.
Pyridine derivatives
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, (2008/06/13)
The invention concerns novel, pharmaceutically useful 1,3-dioxane alkenoic acid derivatives of the formula I containing a pyridyl moiety at position 4 of the dioxane ring and in which the groups at positions 2, 4 and 5 have cis-relative stereochemistry, X is hydrogen, alkoxy or hydroxy, Y is vinylene, n is 1 or 2, A1 is alkylene, the substituents R1 and R2 at position 2 of the dioxane ring have a variety of values defined hereinafter, and R4 is hydroxy, a physiologically acceptable alcohol residue or alkanesulphonamido, and the pharmaceutically acceptable salts thereof. The invention also includes processes for the manufacture and use of the acid derivatives as well as pharmaceutical compositions for therapeutic use in one or more of a variety of diseases such as ischaemic heart disease, cerebrovascular disease, asthmatic disease and/or inflammatory disease.
Development and Application of Organic Reagents for Analysis. VI. Synthesis and Fluorescence Spectral Properties of 2-(4-Substituted phenyl)benzofurans
Akiyama, Shuzo,Akimoto, Hiroyuki,Nakatsuji, Shin'ichi,Nakashima, Kenichiro
, p. 2192 - 2196 (2007/10/02)
A synthesis of fifteen kinds of 2-(4-substituted phenyl)benzofurans (4n) was carried out and their fluorescence spectral properties were investigated concerning their applicability as organic reagents for analyses.
