6322-62-9

Upstream product

• 27757-85-3 2-Aminomethylthiophene 
• 6326-83-6 bis(carboxymethyl)trithiocarbonate 
• 75-15-0 carbon disulfide 
• 13558-70-8 methyl N-(chloroacetyl)carbamate 

Downstream Products

• 1370635-04-3 (Z)-5-(2-(5-chloro-1H-indol-3-yl)-2-oxoethylidene)-3-(thiophen-2-ylmethyl)-2-thioxothiazolidin-4-one 

Relevant academic research and scientific papers

A concise approach to n-substituted rhodanines through a base-assisted one-pot coupling and cyclization process

An efficient approach to obtain functionalized rhodanines was developed through a base-assisted one-pot coupling and continuous cyclization of a primary amine, carbon disulfide, and methyl (2-chloroacetyl)carbamate. This conversion tolerates a broad range of functional groups and can be used to scale the preparation of N-substituted rhodanines in excellent yields.

Design, synthesis and biological evaluation of imidazolidine-2,4-dione and 2-thioxothiazolidin-4-one derivatives as lymphoid-specific tyrosine phosphatase inhibitors

Lymphoid-specific tyrosine phosphatase (LYP), which exclusively exists in immune cells and down-regulates T cell receptor signaling (TCR), has becoming a potent target for various autoimmune diseases. Herein, we designed and synthesized imidazolidine-2,4-dione and 2-thioxothiazolidin-4-one derivatives as new LYP inhibitors. Among them, the cinnamic acids-based inhibitors (9p and 9r) displayed good LYP inhibitory activities (IC50 = 2.85–6.95 μM). Especially, the most potent inhibitor 9r was identified as competitive inhibitor (Ki = 1.09 μM) and bind LYP reversibly. Meanwhile, 9r exhibited better selectivity over other phosphatases than known LYP inhibitor A15. Furthermore, compound 9r could regulate TCR associated signaling pathway in Jurkat T cell.

A facile synthesis of novel 3-(aryl/alkyl-2-ylmethyl)-2-thioxothiazolidin- 4-ones using microwave heating

(Z)-5-(2-(1H-Indol-3-yl)-2-oxoethylidene)-3-(aryl/alkyl-2-ylmethyl) -2-thioxothiazolidin-4-ones (7a-w) have been synthesized by the Knoevenagel condensation reaction of 3-(aryl/alkyl-2-ylmethyl)-2-thioxothiazolidin-4-ones (3a-d) with suitably substituted 2-(1H-indol-3-yl)2-oxoacetaldehydes (6a-g) under microwave conditions. The thioxothiazolidin-4-ones were prepared from the corresponding aryl/alkyl amines (1a-d) and di-(carboxymethyl)-trithiocarbonyl (2). The aldehydes (6a-g) were synthesized from the corresponding acid chlorides (5a-g) using HsnBu3.

USE OF THIAZOLIDINONE DERIVATIVES AS ANTIANGIOGENIC AGENTS

The invention relates to the use of compounds of general formula (I), in which R1, R2 and X are as defined in the description for the preparation of pharmaceutical compositions for the treatment of pathologies in which inhibition of the interaction between HIF-1α and p300 is beneficial, in particular as antiangiogenic medicaments for the therapy of solid tumors.

Phospholipase D inhibitors and uses thereof

The invention is directed to thiazolidinones and the use thereof to inhibit phospholipase D (PLD) activity. The invention further relates to methods of treating cancer and inflammatory diseases using thiazolidinones.