- Discovery of cysteine and its derivatives as novel antiviral and antifungal agents
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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
- Lu, Aidang,Shi, Li,Wang, Tienan,Wang, Ziwen,Yang, Shan,Zhou, Yanan
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- Synthesis, characterization and antibacterial activities of N-tert-butoxycarbonyl-thiazolidine carboxylic acid
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A possible mechanism of dynamic kinetic resolution by the formation of N-tert-butoxycarbonyl-thiazolidine carboxylic acid was proposed and validated by a quantitative density functional theoretical calculation according to Curtin-Hammett principle. Such a
- Song, Zhong-Cheng,Ma, Gao-Yuan,Zhu, Hai-Liang
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p. 24824 - 24833
(2015/03/30)
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- Synthesis, structure and structure-activity relationship analysis of 3-tert-butoxycarbonyl-2-arylthiazolidine-4-carboxylic acid derivatives as potential antibacterial agents
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Nine 2-arylthiazolidine-4-carboxylic acid derivatives and nine 3-tert-butoxycarbonyl-2-arylthiazolidine-4-carboxylic acid derivatives were synthesized to screen for their antibacterial activities. Compounds 5, 14-18 were first reported. Their chemical str
- Song, Zhong-Cheng,Ma, Gao-Yuan,Lv, Peng-Cheng,Li, Huan-Qiu,Xiao, Zhu-Ping,Zhu, Hai-Liang
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experimental part
p. 3903 - 3908
(2009/12/04)
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- Discovery of 2-arylthiazolidine-4-carboxylic acid amides as a new class of cytotoxic agents for prostate cancer
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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.
- Gududuru, Veeresa,Hurh, Eunju,Dalton, James T.,Miller, Duane D.
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p. 2584 - 2588
(2007/10/03)
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- Synthesis and Chiroptical Properties of N-Acetyl-2-aryl-4-thiazolidinecarboxylic Acids
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(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
- Gyoergydeak, Zoltan,Kajtar-Peredy, Maria,Kajtar, Judit,Kajtar, Marton
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p. 927 - 934
(2007/10/02)
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