3400-07-5Relevant articles and documents
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.
Synthesis, Dissociation Constants, and Antimicrobial Activity of Novel 2,3-Disubstituted-1,3-thiazolidin-4-one Derivatives
Popiolek, Lukasz,Stefaska, Joanna,Kielczykowska, Malgorzata,Musik, Irena,Biernasiuk, Anna,Malm, Anna,Wujec, Monika
, p. 393 - 402 (2016/04/19)
In this article, a new series of 2,3-disubstituted-1,3-thiazolidin-4-one derivatives have been designed, synthesized, and evaluated as antimicrobial agents. New compounds were prepared by the cyclization reaction of N-substituted carboxylic acid hydrazide derivatives with mercaptoacetic acid. The structures of the obtained compounds were confirmed by means of IR, 1H NMR, and 13C NMR spectra. The dissociation constants were determined using spectrophotometric method. All synthesized compounds were tested for their in vitro antibacterial and antifungal activities using the broth microdilution method.
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
supporting information, 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.