7255-58-5Relevant articles and documents
Insights into supramolecular assembly formation of diethyl aryl amino methylene malonate (DAM)derivatives assisted via non-covalent interactions
Shaik, Althaf,Angira, Deekshi,Thiruvenkatam, Vijay
, p. 178 - 185 (2019/05/14)
The crystal structures of four derivatives of diethyl 2-(((aryl)amino)methylene)malonate (DAM)have been studied by single crystal X-ray diffraction. The molecular structures of all the four derivatives were found to be in co-planar conformation. The detailed analysis of molecular conformation in four derivatives reveals the presence of a common strong intramolecular N–H?O hydrogen bonding, forming a ring of graph-set motif S1 1 (6). The effect of chloro and nitro substitution on their relative strengths of hydrogen bonding are analyzed here. Particularly, in compound 1, additional intramolecular hydrogen bonding between –NO2 and N–H was observed that results in the formation of another six-membered chelate ring. On the other hand in case of compound 3, we have observed type-I Cl?Cl interaction for the first time in this class of compounds. Further, Hirshfeld surface has been generated that is mapped with dnorm shape index and curvedness to summarize the weak interactions and examine the molecular shapes in all four derivatives. Effect of nitro (1 and 2)and chloro (3 and 4)substitution on the C?H, N?O and C?O interaction is highlighted in molecular contour and 2D fingerprint plots.
QUINOLINE DERIVATIVES AS CASPASE-3 INHIBITOR, PREPARATION PROCESS FOR THE SAME AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Page/Page column 88-90, (2008/12/07)
Provided is a quinoline derivative represented by the following Formula (1) for use in treating a caspase- mediated disease by inhibition of caspase-3 activity. Further provided are a method for preparing the quinoline derivative or a pharmaceutically acceptable salt thereof and a pharmaceutical composition containing the same.
QUINOLINE DERIVATIVES AS CASPASE-3 INHIBITOR, PREPARATION FOR PRODUCING THE SAME AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Page/Page column 26-27, (2008/06/13)
The present invention relates to new quinoline derivatives of formula (1) or their pharmaceutically acceptable salts with caspase-3 inhibitory activity and their preparation methods, wherein R2 is H; halogen; C1-6alkyl; C 1-6 alkoxy; C1-6 alkoxyalkyl; or C3-6cycloalkyl; R1 is formula (a); -CN; or formula (b); R is H; C6-14aryl unsubstituted or substituted by halogen, C1-6 alkyl, C1-6 alkoxy or amino; 5 - 15 membered heterocyclic group unsubstituted or substituted by halogen, C1-6 alkyl, C1-6 alkoxy or amino; or -(CH2)n-CHR4R5. The present invention relates to a pharmaceutical composition for treating caspase-associated diseases by inhibiting the activity of caspase-3 which comprises the compound of formula (1) or its pharmaceutically acceptable salt.