65136-87-0Relevant articles and documents
Toll-like receptor-7 small molecule inhibitor and preparation method thereof
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Paragraph 0168-0170, (2021/02/24)
The invention belongs to the field of chemical small molecules, and particularly relates to a Toll-like receptor-7 small molecule inhibitor. The invention provides the Toll-like receptor-7 small molecule inhibitor, which takes a co-inhibitor of TLR7 and TLR8 obtained by screening as a research object, realizes selective regulation and control of TLR7 and TLR8 through the research on the structureoptimization and structure-activity relationship (SAR) of a parent compound, and further develops a high-efficiency, non-toxic and specific small molecule inhibitor with certain selectivity on TLR 7.The TLR7 small molecule inhibitor has a certain effect and potential medicinal value in autoimmune diseases (systemic lupus erythematosus).
N-Acylbenzotriazole: convenient approach for protecting group-free monoacylation of symmetric diamines
Agha, Khalid A.,Abo-Dya, Nader E.,Ibrahim, Tarek S.,Abdel-Aal, Eatedal H.,Abdel-Samii, Zakaria K.
, p. 589 - 598 (2020/05/06)
Abstract: An efficient green route for monoacylation of aromatic diamines, namely o-phenylenediamine and p-phenylenediamine and aliphatic diamines ethylenediamine and piperazine using N-acylbenzotriazoles (NABs) in n-butanol was developed. The new protocol does not require prior selective protection of the diamine and comprises simple conditions, short reaction times, an easy work up as well as high isolated yields (69–94%). Moreover, the method described herein enable stepwise acylation of aliphatic diamines such as ethylenediamine and piperazine with two different N-acylbenzotriazoles affording unsymmetrical substituted diamines that can be used for construction of pharmaceutically important targets such as drugs, foldamers, and drug conjugates. Graphic abstract: [Figure not available: see fulltext.]
Biofilm inhibition and anti-Candida activity of a cationic lipo-benzamide molecule with twin-nonyl chain
Jain, Tushar,Muktapuram, Prathap Reddy,Sharma, Komal,Ravi, Owk,Pant, Garima,Mitra, Kalyan,Bathula, Surendar Reddy,Banerjee, Dibyendu
supporting information, p. 1776 - 1780 (2018/04/23)
A series of cationic lipo-benzamide compounds with varying lengths of hydrocarbon chains (C2M–C18M) were evaluated for anti-Candida activity. Four compounds harbouring 8–11 hydrocarbon chains demonstrated concentration-dependent inhibition of fungal cell