66892-28-2

Upstream product

• 3218-02-8 cyclohexylmethylamine 
• 145012-90-4 N-benzoyl-N'-(cyclohexylmethyl)thiourea 
• 52395-66-1 cyclohexylmethyl isothiocyanate 

Downstream Products

• 870711-18-5 2-((cyclohexylmethyl)amino)-5-ethyl-5-methyl-1,3-thiazol-4(5H)-one 
• 870711-09-4 2-((cyclohexylmethyl)amino)-5-methyl-5-propyl-1,3-thiazol-4(5H)-one 
• 1505452-87-8 3-(cyclohexylmethyl)-2-imino-5,5-bis(4-methoxyphenyl)imidazolidin-4-one 
• 138460-19-2 N-(cyclohexylmethyl)-N'-(carboxymethyl)guanidine 
• 138460-22-7 aminomethanesulfonic acid 
• 145231-36-3 N-(cyclohexylmethyl)-S-<3-(4(5)-imidazolyl)propyl>isothiourea 
• 145012-91-5 C₁₃H₂₄N₂O₂S 
• 870707-75-8 5-[(cyclohexylmethyl)amino]-4-thia-6-azaspiro[2.4]hept-5-en-7-one 
• 870707-69-0 2-[(cyclohexylmethyl)amino]-5-(2-hydroxyphenyl)-1,3-thiazol-4(5H)-one 
• 145012-96-0 C₂₀H₃₈N₄O₃ 
• 145013-04-3 (R)-2-(Cyclohexylmethyl-amino)-5-methyl-1,5-dihydro-imidazol-4-one 
• 145012-98-2 C₂₂H₄₂N₄O₃ 
• 145012-97-1 C₂₁H₄₀N₄O₃ 

Relevant academic research and scientific papers

COMPOSITIONS AND METHODS FOR THE TREATMENT OF MALARIA

The present invention provides aminohydantoin anti-malarial agents. In some embodiments, these agents have the property of functions of targeting malarial aspartic proteases while at the same time having low activity against human BACE. Methods of employing such agents are also provided.

2-Amino-1,3-thiazol-4(5H)-ones as potent and selective 11β- hydroxysteroid dehydrogenase type 1 inhibitors: Enzyme-ligand co-crystal structure and demonstration of pharmacodynamic effects in C57Bl/6 mice

11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) has attracted considerable attention during the past few years as a potential target for the treatment of diseases associated with metabolic syndrome. In our ongoing work on 11β-HSD1 inhibitors, a series of new 2-amino-1,3-thiazol-4(5H)-ones were explored. By inserting various cycloalkylamines at the 2-position and alkyl groups or spirocycloalkyl groups at the 5-position of the thiazolone, several potent 11β-HSD1 inhibitors were identified. An X-ray cocrystal structure of human 11β-HSD1 with compound 6d (Ki = 28 nM) revealed a large lipophilic pocket accessible by substitution off the 2-position of the thiazolone. To increase potency, analogues were prepared with larger lipophilic groups at this position. One of these compounds, the 3-noradamantyl analogue 8b, was a potent inhibitor of human 11β-HSD1 (Ki = 3 nM) and also inhibited 11β-HSD1 activity in lean C57Bl/6 mice when evaluated in an ex vivo adipose and liver cortisone to cortisol conversion assay.

A Mild and Efficient Method for the Preparation of Guanidines

A mild and efficient method for the preparation of guanidines by reaction of an acylated thiourea with an amine followed by removal of the acyl groups(s) from the intermediate acylguanidine is reported.Key Words: acylguanidine, acylthiourea, guanidine, water soluble carbodiimide

Isothiourea analogues of histamine as potent agonists or antagonists of the histamine H3-receptor

The synthesis and H3-activity of a series of isothiourea analogues of histamine have been described. It has been shown that S-[2-(4(5)-imidazolyl)ethylisothiourea (VUF 8325) is a potent H3-agonist measured as the electrically evoked contraction of the guinea-pig ileum. Upon methylation of the imidazole system or the isothiourea moiety a decrease in affinity was observed leading to either weak agonists or weak antagonists. Introduction of N-(phenylalkyl) substituents at the isothiourea part gives rise to highly potent H3-antagonists. Particularly the 4-chlorobenzyl group appeared to be favourable in the series described resulting in a histamine H3-antagonist with a pA2-value of 9.9.

N,N'-disubstituted guanidine high-potency sweeteners

The role and function of the aryl group in the highly potent trisubstituted guanidine sweeteners 7a-d was investigated. Four disubstituted guanidines, lacking the aryl group, were prepared. These guanidines contain a hydrophobic substituent on one nitroge