186343-07-7

Upstream product

• 71404-25-6 2,4-dichlorobenzoyl isothiocyanate 
• 89-75-8 2,4-dichlorobenzoyl chloride 

Downstream Products

• 186342-85-8 3-(2,4-dichlorophenyl)-5-(N-propyl-N-bis(cyclopropyl)methylamino)-1H-[1,2,4]triazole 
• 186342-85-8 3-(2-dichlorophenyl)-5-(N-propyl-N-[bis(cyclopropyl)methyl]amino)-1H-[1,2,4]triazole 

Relevant academic research and scientific papers

Rational design, synthesis, and structure-Activity relationships of aryltriazoles as novel corticotropin-releasing factor-1 receptor antagonists

Following the discovery of the very high binding affinity of 4-anilinopyrimidines against corticotropin-releasing factor receptor-1 (CRF 1) (e.g., 1, Ki = 2 nM), a new series of triazoles bearing different groups has been synthesized

1-Alkyl-3-amino-5-aryl-1H-[1,2,4]triazoles: Novel synthesis via cyclization of N-Acyl-S-methylisothioureas with alkylhydrazines and their potent corticotropin-Releasing factor-1 (CRF1) receptor antagonist activities

Cyclizations of alkylhydrazines with N-acyl-S-methylisothioureas, readily synthesized from acyl chlorides, sodium thioisocyanate, dialkylamines then methyl iodide in a one-pot reaction, gave 1-alkyl-3-dialkylamino-5-phenyltriazoles 7 as major products. The regioisomers were assigned through the use of NOE NMR experiments. While bearing a N-bis(cyclopropyl)methyl-N-propylamino group, this series of compounds shows very good binding affinity on the human CRF1 receptor. Among them, 1-methyl-3-[N-bis(cyclopropyl)methyl-N-propylamino]-5-(2,4-dichlorophenyl)- 1H-[1,2,4]triazole 7a had the best binding affinity for the CRF1 receptor (Ki=9 nM).

CRF receptor antagonists and methods relating thereto

CRF receptor antagonists are disclosed. Such receptor antagonists are thiadiazole-, pyrimidine-, triazine-, and triazole-containing compounds substituted with both a C3-C14 monocyclic or fused, homoaryl or heteroaryl group and a substituted amine group. The CFR receptor antagonists have utility in the treatment of a variety of disorders, including disorders associated with the hypersecretion of CRF.