79116-08-8

Upstream product

• 2227-79-4 benzenecarbothioamide 
• 22900-83-0 ethyl 2-bromo-4-methyl-1,3-thiazole-5-carboxylate 
• 7210-76-6 ethyl-2-amino-4-methylthiazole-5-carboxylate 

Downstream Products

• 88469-80-1 ethyl 4-[(acetyloxy)methyl]-2-phenyl-1,3-thiazole-5-carboxylate 
• 1235473-99-0 ethyl 4-((dimethylamino)methyl)-2-phenylthiazole-5-carboxylate 
• 88469-78-7 7-Morpholino-2-phenyl-thiazolo<4,5-d>pyridazin 
• 88469-75-4 2,6-Diphenyl-thiazolo<4,5-d>pyridazin-7-on 
• 88469-73-2 5-Ethoxycarbonyl-4-formyl-2-phenyl-thiazol 
• 88469-79-8 7-Methylthio-2-phenyl-thiazolo<4,5-d>pyridazin 
• 88469-77-6 2-Phenyl-thiazolo<4,5-d>pyridazin-7-thion 
• 88469-74-3 2-Phenyl-thiazolo<4,5-d>pyridazin-7-on 
• 88469-76-5 7-chloro-2-phenylthiazolo<4,5-d>pyridazine 
• 440107-18-6 2-phenyl-4-(1-pyrrolylmethyl)thiazole-5-carbonyl azide 
• 440107-17-5 2-phenyl-4-(1-pyrrolylmethyl)thiazole-5-carboxylic acid 
• 952394-61-5 4-{[(2,4-dimethoxy-benzyl)-ethoxycarbonylmethyl-amino]-methyl}-2-phenyl-thiazole-5-carboxylic acid ethyl ester 
• 440107-15-3 ethyl 2-phenyl-4-(1-pyrrolylmethyl)thiazole-5-carboxylate 
• 79116-09-9 ethyl 2-phenyl-4-phenoxymethylthiazole-5-carboxylate 

Relevant academic research and scientific papers

Discovery of Novel TRPM8 Blockers Suitable for the Treatment of Somatic and Ocular Painful Conditions: A Journey through p Kaand LogD Modulation

Transient receptor potential melastatin 8 (TRPM8) is crucially involved in pain modulation and perception, and TRPM8 antagonists have been proposed as potential therapeutic approaches for pain treatment. Previously, we developed two TRPM8 antagonists and proposed them as drug candidates for topical and systemic pain treatment. Here, we describe the design and synthesis of these two TRPM8 antagonists (27 and 45) and the rational approach of modulation/replacement of bioisosteric chemical groups, which allowed us to identify a combination of narrow ranges of pKa and LogD values that were crucial to ultimately optimize their potency and metabolic stability. Following the same approach, we then pursued the development of new TRPM8 antagonists suitable for the topical treatment of ocular painful conditions and identified two new compounds (51 and 59), N-alkoxy amide derivatives, that can permeate across ocular tissue and reduce the behavioral responses induced by the topical ocular menthol challenge in vivo.

Design and synthesis of novel triazole derivatives containing γ-lactam as potential antifungal agents

A series of novel triazole derivatives containing γ-lactam were designed and synthesized, and their structures were confirmed by 1H NMR, 13C NMR and HRMS. The in vitro antifungal activities of the target compounds were evaluated. The results showed that all of the compounds exhibited stronger activity against the six clinically important fungi tested than fluconazole. 3D and 3E showed comparative activity against the fungi tested except for Candida glabrata and Aspergillus fumigatus as voriconazole. In addition, the docking model for 2A and CYP51 was investigated.

Thiazole and oxazole derivatives as activators of human peroxisome proliferator activated receptors

The present invention provides a compound of formula (1) wherein R1-R5, R25, R26, Y and X2 are defined as in claim 1. The compounds activate human peroxisome proliferator activated receptors (hPPARs) and arc useful for the treatment of associated disorders such as cardiovascular disease and hypercholesteremia.