98069-56-8Relevant academic research and scientific papers
Design and synthesis in silico drug-like prediction and pharmacological evaluation of cyclopolymethylenic homologous of lassbio-1514
Alexandre-Moreira, Magna Suzana,Aparecida-Silva, Cristiane,Barreiro, Eliezer J.,Bispo Júnior, Walfrido,Lima, Lidia Moreira,Zapata-Sudo, Gisele,da Silva Monteiro, Carlos Eduardo,da Silva, Tiago Fernandes,de Queiroz, Aline Cavalcanti
, (2021/08/19)
Acylhydrazones are still an important framework to the design of new bioactive com-pounds. As treatment of chronic pain represents a clinical challenge, we decided to modify the structure of LASSBio-1514 (1), previously described as anti-inflammatory and analgesic proto-type. Applying the homologation as a strategy for molecular modification, we designed a series of cyclopentyl-(2a–e), cyclobutyl-(3a–e), and cyclopropylacylhydrazones (4a–e) that were synthetized and evaluated in murine models of inflammation and pain. A comparison of their in silico physico-chemical and drug-like profile was conducted, as well as their anti-inflammatory and analgesic effect. Compounds 4a (LASSBio-1755) and 4e (LASSBio-1757) displayed excellent in silico drug-like profiles and were identified as new analgesic lead-candidates in acute and chronic model of pain, through oral administration.
SSAO INHIBITOR
-
Paragraph 0427; 0428; 0429, (2020/04/02)
The present invention provides an SSAO inhibitor and an application thereof in preparing a drug for treating a disease related to SSAO. In particular, the present invention provides a compound shown in formula (IV) and a pharmaceutically acceptable salt thereof.
Synthesis of 3-hydroxyindanones via potassium salt of amino acid catalyzed regioselective intramolecular aldolization of ortho-diacylbenzenes
Chanda, Tanmoy,Chowdhury, Sushobhan,Anand, Namrata,Koley, Suvajit,Gupta, Ashutosh,Singh, Maya Shankar
, p. 981 - 985 (2015/03/04)
First organocatalytic intramolecular aldolization of ortho-diacylbenzenes to construct highly functionalized 3-hydroxyindanones is described. In this transformation a high trans-selectivity is achieved by the use of metal salt of amino acid. This method allows an easy access to the strained spirocyclic 3-hydroxyindanones related to a number of natural product frameworks. Synthesis of a new class of indole skeleton substituted by 3-hydroxyindanones added an extra essence to this new protocol.
