218944-01-5Relevant academic research and scientific papers
Discovery of cysteine and its derivatives as novel antiviral and antifungal agents
Lu, Aidang,Shi, Li,Wang, Tienan,Wang, Ziwen,Yang, Shan,Zhou, Yanan
, (2021/06/25)
Based on the structure of the natural product cysteine, a series of thiazolidine-4-carboxylic acids were designed and synthesized. All target compounds bearing thiazolidine-4-carboxylic acid were characterized by1 H-NMR,13 C-NMR, and
GLUCOSE-SENSITIVE PEPTIDE HORMONES
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Page/Page column 26-27, (2020/01/11)
The present invention relates to a conjugate of the formula P-L-I, wherein P is a peptide hormone effecting the metabolism of carbohydrates in vivo, L is a hydrolysable linker molecule consisting of Lp and Lj, and I is a molecule capable of inhibiting the effect of the peptide hormone P on the metabolism of carbohydrates in vivo. Under in vivo conditions, the conjugate is the major compound. When the concentration of glucose increases in v/vo,the concentration of the peptide hormone effecting the metabolism of carbohydrates in vivo also increases.
Synthesis and in vitro studies of thiazolidine-4-carboxylic acid hydrazones as potential antitubercular agents
Nagasree, Kurre Puma,Kumar, Muthyala Murali Krishna,Prasad, Yejella Rajendra,Sriram, Dharmarajan,Yogeeswari, Perumal
, p. 538 - 555 (2019/05/21)
A series of forty six 2-substituted aryl-thiazolidine-4-carboxylic acid hydrazones (6a-c, 7a-c, 8a-c, 9a-c series) have been synthesized and isolated in their pure isomeric form (2R, 4R and 2S, 4R). Purity and structures have been ascertained by chromatographic and, IR, NMR and mass spectral data analysis. Antitubercular activity screening of these synthesized compounds against Mycobacterium tuberculosis H37Rv (MTB) and multi-drug resistant Mycobacterium tuberculosis (MDR-TB) has resulted in identification of three active compounds (6a 11, 6a 13, 6a 15) with MIC 10 μM against MTB and MDR-TB. The compound 6a 11 (2R, 4R isomer) shows the highest potency with MIC 1.33 μM against MDR-TB. It is observed that the antitubercular activity of 2R isomer is four times more than the corresponding 2S isomer.
Discovery of 2-arylthiazolidine-4-carboxylic acid amides as a new class of cytotoxic agents for prostate cancer
Gududuru, Veeresa,Hurh, Eunju,Dalton, James T.,Miller, Duane D.
, p. 2584 - 2588 (2007/10/03)
To improve the selectivity and antiproliferative activity of previously reported serine amide phosphates (SAPs), we designed a new series of 4-thiazolidinone amides, in which the 4-thiazolidinone moiety was introduced as a phosphate mimic. However, these 4-thiazolidinone derivatives demonstrated less cytotoxicity in prostate cancer cells despite improved selectivity over RH7777 cells. To further optimize the thiazolidinone analogues in terms of cytotoxicity and selectivity, we made closely related structural modifications, which led us to the discovery of a new class of 2-arylthiazolidine-4-carboxylic acid amides. These compounds were potent cytotoxic agents with IC50 values in the low micromolar concentration range and demonstrated enhanced selectivity in receptor-negative cells compared to SAPs and 4-thiazolidinone amides.
Derivatives of 2-(iminomethyl)amino-phenyl, their preparation, their use as medicaments and the pharmaceutical compositions containing them
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Page column 97, (2008/06/13)
A compound selected from the group consisting of a compound of the formula wherein A is selected from the group consisting of and the other substituents are defined in the specification having an inhibitory activity of NO-synthase enzymes producing nitrogen mono-oxide and/or an activity which traps the reactive oxygen species.
Synthesis and Chiroptical Properties of N-Acetyl-2-aryl-4-thiazolidinecarboxylic Acids
Gyoergydeak, Zoltan,Kajtar-Peredy, Maria,Kajtar, Judit,Kajtar, Marton
, p. 927 - 934 (2007/10/02)
(4R)-2-Aryl-4-thiazolidinecarboxylic acids 3, derived from aromatic aldehydes 1 and L-cysteine (2), could be diastereoselectively converted into (2R,4R)- or (2S,4R)-N-acetyl-2-aryl-4-thiazolidinecarboxylic acids (4 and 5, resp.).The diastereomers can be d
