222404-25-3

Upstream product

• 32443-99-5 D-cysteine hydrochloride 
• 123-11-5 4-methoxy-benzaldehyde 
• 52-89-1 l-cysteine hydrochloride 
• 52-90-4 L-Cysteine 

Downstream Products

• 350035-37-9 (R)-3-[(R)-3-Hydroxy-2-(4-methoxy-benzylamino)-propyldisulfanyl]-2-(4-methoxy-benzylamino)-propan-1-ol 
• 1071689-48-9 dimethyl (3R)-3-(4-methoxyphenyl)-5-methyl-1H,3H-pyrrolo[1,2-c]thiazole-6,7-dicarboxylate 
• 1609535-71-8 (3R)-6,7-bis(hydroxymethyl)-3-(4-methoxyphenyl)-5-methyl-1H,3H-pyrrolo[1,2-c]thiazole 
• 2544-31-2 S-(4-methoxybenzyl)-L-cysteine 
• 72678-39-8 (R)-3-((S)-3-Benzoylsulfanyl-2-methyl-propionyl)-2-(4-methoxy-phenyl)-thiazolidine-4-carboxylic acid 
• 110078-94-9 (2S,4R)-3-Acetyl-2-(4-methoxy-phenyl)-thiazolidine-4-carboxylic acid 
• 110078-83-6 (2R,4R)-3-Acetyl-2-(4-methoxy-phenyl)-thiazolidine-4-carboxylic acid 
• 72678-37-6 (R)-3-(3-Benzoylsulfanyl-propionyl)-2-(4-methoxy-phenyl)-thiazolidine-4-carboxylic acid 
• 1148154-79-3 (2R,4R)-3-(tert-butoxycarbonyl)-2-(4-methoxyphenyl)-thiazolidine-4-carboxylic acid 
• 78979-46-1 (4R) ethyl 2-(4-methoxyphenyl)thiazolidine-4-carboxylate 
• 637032-07-6 (4R)-3-(tert-butoxycarbonyl)-2-(4-methoxyphenyl)thiazolidine-4-carboxylic acid 
• 65776-11-6 (R)-3-mercapto-2-(4-methoxy-benzylamino)-propionic acid 
• 69570-41-8 (R)-3-((S)-3-Mercapto-2-methyl-propionyl)-2-(4-methoxy-phenyl)-thiazolidine-4-carboxylic acid 
• 72678-38-7 (R)-3-(3-Mercapto-propionyl)-2-(4-methoxy-phenyl)-thiazolidine-4-carboxylic acid 

Relevant academic research and scientific papers

Discovery of cysteine and its derivatives as novel antiviral and antifungal agents

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

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.

Purple acid phosphatase inhibitors as leads for osteoporosis chemotherapeutics

Purple acid phosphatases (PAPs) are metalloenzymes that catalyse the hydrolysis of phosphate esters under acidic conditions. Their active site contains a Fe(III)Fe(II) metal centre in mammals and a Fe(III)Zn(II) or Fe(III)Mn(II) metal centre in plants. In humans, elevated PAP levels in serum strongly correlate with the progression of osteoporosis and metabolic bone malignancies, which make PAP a target suitable for the development of chemotherapeutics to combat bone ailments. Due to difficulties in obtaining the human enzyme, the corresponding enzymes from red kidney bean and pig have been used previously to develop specific PAP inhibitors. Here, existing lead compounds were further elaborated to create a series of inhibitors with Ki values as low as ～30 μM. The inhibition constants of these compounds were of comparable magnitude for pig and red kidney bean PAPs, indicating that relevant binding interactions are conserved. The crystal structure of red kidney bean PAP in complex with the most potent inhibitor in this series, compound 4f, was solved to 2.40 ? resolution. This inhibitor coordinates directly to the binuclear metal centre in the active site as expected based on its competitive mode of inhibition. Docking simulations predict that this compound binds to human PAP in a similar mode. This study presents the first example of a PAP structure in complex with an inhibitor that is of relevance to the development of anti-osteoporotic chemotherapeutics.

3-Propionyl-thiazolidine-4-carboxylic acid ethyl esters: A family of antiproliferative thiazolidines

Cancer results from unregulated cell growth. Reactivating the process of the programmed cell death, i.e. apoptosis, is a classical anticancer therapeutic strategy. The apoptosis-inducing property of the (2RS,4R)-2-phenyl-3-propionyl-thiazolidine-4-carboxylic acid ethyl ester (ALC 67) molecule has recently been discovered. We analyzed in this study the impact of the phenyl moiety of this molecule on its biological activity by synthesizing and evaluating analogues where this substituent was replaced by a series of aromatic and aliphatic groups. The results demonstrated that the molecule's antiproliferative property resisted such modifications. Thus, in addition to developing a family of thiazolidine compounds with promising anticancer properties; our investigation revealed that the second position of the thiazolidine ring can be used either to tune the physicochemical properties of ALC67 or to introduce a fluorescent tag to the structure in order to track it in cells and determine its exact molecular mechanism of action.

Synthesis, characterization and antibacterial activities of N-tert-butoxycarbonyl-thiazolidine carboxylic acid

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

NOVEL COMPOUND HAVING SKIN-WHITENING, ANTI-OXIDIZING AND PPAR ACTIVITIES AND MEDICAL USE THEREFOR

Provided are a novel compound having skin-whitening, anti-oxidizing and PPAR activities and a medical use thereof, and the compound has skin-whitening activities for the suppression of tyrosinase, and accordingly, is useful for use in skin-whitening pharmaceutical composition or cosmetic products; has anti-oxidant activities, and accordingly, is useful for the prevention and treatment of skin-aging; and has PPAR activities, and in particular, PPARα and PPARγ activities, and accordingly, is useful for use in pharmaceutical compositions or health foods which are effective for the prevention and treatment of obesity, metabolic disease, or cardiovascular disease.

Substituent-dependent reactivity in aldehyde transformations: 4-(phenylethynyl)benzaldehydes versus simple benzaldehydes

Effects of substituents on transformations of 4-(phenylethynyl) benzaldehydes and related benzaldehydes were analyzed in aldol and thiazolidine formation reactions. The aldol reaction of 4-cyanobenzaldehyde was 54-fold faster than that of 4-methoxybenzald

Design, synthesis and biological evaluation of 2-(substituted phenyl)thiazolidine-4-carboxylic acid derivatives as novel tyrosinase inhibitors

Herein we describe the design, synthesis and biological activities of 2-(substituted phenyl)thiazolidine-4-carboxylic acid derivatives as novel tyrosinase inhibitors. The target compounds 2a-2j were designed and synthesized from the structural characteristics of N-phenylthiourea, tyrosinase inhibitor and tyrosine, and l-DOPA, the natural substrates of tyrosinase. Among them, (2R/S,4R)-2-(2,4-dimethoxyphenyl)thiazolidine-4-carboxylic acid (2g) caused the greatest inhibition 66.47% at 20 μM of l-DOPA oxidase activity of mushroom tyrosinase. Kinetic analysis of tyrosinase inhibition revealed that 2g is a competitive inhibitor. We predicted the tertiary structure of tyrosinase, and simulated the docking of mushroom tyrosinase with 2g. These results suggest that the binding affinity of 2g with tyrosinase is high. Also, 2g effectively inhibited tyrosinase activity and reduced melanin levels in B16 cells treated with α-MSH. These data strongly suggest that 2g can suppress the production of melanin via the inhibition of tyrosinase activity.

BIOMOLECULAR LABELLING USING MULTIFUNCTIONAL BIOTIN ANALOGUES

Novel biotin analogues, such as 2-Azidobiotin, comprising the ureido ring of natural biotin with the thiophene ring, optionally modified, and a modified sidechain having a functional end group, preferably selected from the group consisting of a carboxylic

Synthesis, in vitro structure-activity relationship, and in vivo studies of 2-arylthiazolidine-4-carboxylic acid amides as anticancer agents

A series of (2RS,4R)-2-arylthiazolidine-4-carboxylic acid amide (ATCAA) was synthesized. Antiproliferative activity against melanoma and prostate cancer cells compared with control cells (fibroblast and RH7777, respectively) was evaluated. Compound 3id sh