7661-12-3Relevant academic research and scientific papers
Arylamide as Potential Selective Inhibitor for Matrix Metalloproteinase 9 (MMP9): Design, Synthesis, Biological Evaluation, and Molecular Modeling
Al-Najjar, Belal,Dewa, Sangga P.,Hariono, Maywan,Jati, Benedictus W.,Jenie, Riris I.,Julianus, Jeffry,Nugroho, Ervan S.,Nuwarda, Rina F.,Putra, Kevin C.,Qodria, Lailatul,Ramadani, Ratna D.,Rollando, Rollando,Tiara, Reynaldo,Wahab, Habibah A.,Wisnumurti, Yohanes K.,Yusuf, Muhammad
, (2020/01/21)
Previous studies have reported that compounds bearing an arylamide linked to a heterocyclic planar ring have successfully inhibited the hemopexin-like domain (PEX9) of matrix metalloproteinase 9 (MMP9). PEX9 has been suggested to be more selectively targe
Synthesis of new tricyclic 5,6-dihydro-4H-benzo[b][1,2,4]tri-azolo[1,5-d][1,4]diazepine derivatives by [3+ + 2]-cyclo-addition/rearrangement reactions
Luan, Lin-bo,Song, Zi-jie,Li, Zhi-ming,Wang, Quan-rui
supporting information, p. 1826 - 1833 (2018/08/21)
Two new series of tricyclic heterocycles, namely 5,6-dihydro-4H-benzo[b][1,2,4]triazolo[1,5-d][1,4]diazepinium salts 10 and the related neutral, free bases 13 were synthesized from 4-acetoxy-1-acetyl-4-phenylazo-1,2,3,4-tetrahydroquinolines 8 and nitriles 9 in the presence of aluminium chloride by the [3+ + 2]-cycloaddition reaction of the in situ generated azocarbenium intermediates 14 followed by a ring-expansion rearrangement. In the rearrangement reaction, the phenyl substituent in the initially formed spiro-triazolium adducts 16 underwent a [1,2]-migration from C(3) to the electron-deficient N(2). This led to the ring expansion from 6-membered piperidine to 7-membered diazepine furnishing the tricyclic 1,2,4-triazole-fused 1,4-benzodiazepines.
Formation of acridones by ethylene extrusion in the reaction of arynes with β-lactams and dihydroquinolinones
Fang, Yuesi,Rogness, Donald C.,Larock, Richard C.,Shi, Feng
experimental part, p. 6262 - 6270 (2012/09/22)
N-Unsubstituted β-lactams react with a molecule of aryne by insertion into the amide bond to form a 2,3-dihydroquinolin-4-one, which subsequently reacts with another molecule of aryne to form an acridone by extrusion of a molecule of ethylene. 2,3-Dihydroquinolin-4-ones react under the same reaction conditions to afford identical results. This is the first example of ethylene extrusion in aryne chemistry.
Design, synthesis and biological evaluation of hydroxamic acid derivatives as potential high density lipoprotein (HDL) receptor CLA-1 up-regulating agents
Chen, Xiaofang,Wang, Li,Du, Yu,Wu, Yanbin,Jia, Xiaojian,Yang, Yuan,Hong, Bin
experimental part, p. 9178 - 9193 (2012/01/12)
Trichostatin A (TSA) and suberoylanilide hydroxamic acid (SAHA) were reported in our recent publication as novel human high density lipoprotein (HDL) receptor CD36 and Lysosomal integral membrane protein-II Analogous-1 (CLA-1) up-regulators. As part of a
Design, synthesis and prostate cancer cell-based studies of analogs of the Rho/MKL1 transcriptional pathway inhibitor, CCG-1423
Evelyn, Chris R.,Bell, Jessica L.,Ryu, Jenny G.,Wade, Susan M.,Kocab, Andrew,Harzdorf, Nicole L.,Hollis Showalter,Neubig, Richard R.,Larsen, Scott D.
scheme or table, p. 665 - 672 (2010/06/21)
We recently identified bis(amide) CCG-1423 (1) as a novel inhibitor of RhoA/C-mediated gene transcription that is capable of inhibiting invasion of PC-3 prostate cancer cells in a Matrigel model of metastasis. An initial structure-activity relationship study focusing on bioisosteric replacement of the amides and conformational restriction identified two compounds, 4g and 8, with improved selectivity for inhibition of RhoA/C-mediated gene transcription and attenuated cytotoxicity relative to 1. Both compounds were also capable of inhibiting cell invasion with equal efficacy to 1 but with less attendant cytotoxicity.
Synthesis and biological evaluation of a new series of berberine derivatives as dual inhibitors of acetylcholinesterase and butyrylcholinesterase
Huang, Ling,Luo, Zonghua,He, Feng,Lu, Jing,Li, Xingshu
experimental part, p. 4475 - 4484 (2010/08/22)
A series of novel berberine derivatives were designed, synthesized, and biologically evaluated as inhibitors of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Among these derivatives, compound 48a, berberine linked with 3-methylpyridi
Synthesis of some substituted pyrazinopyridoindoles and 3D QSAR studies along with related compounds: Piperazines, piperidines, pyrazinoisoquinolines, and diphenhydramine, and its semi-rigid analogs as antihistamines (H1)
Saxena, Mridula,Gaur, Stuti,Prathipati, Philip,Saxena, Anil K.
, p. 8249 - 8258 (2007/10/03)
3D QSAR studies on the title compounds led to the development of a model with three biophoric sites and six secondary sites viz. H-acceptor (ACC), H-donor (DON), heteroatom (presence), hydrophobic (hydrophobicity), steric (refractivity), and a ring (prese
A Convenient Synthesis of Monocyclic β-Lactams by Means of Solid-Liquid Phase Transfer Reactions
Takahata, Hiroki,Ohnishi, Yoshinori,Takehara, Hiroyuki,Tsuritani, Kazuko,Yamazaki, Takao
, p. 1063 - 1068 (2007/10/02)
The intramolecular N-alkylation of β-bromopropionamides (1) under phase transfer conditions afforded monocyclic N-substituted β-lactams (2) in high yields.In a similar manner, cyclization by N1-C4 bond formation gave 4-benzoyl-2-azet
