69389-13-5

Usage

Uses

Used in Pharmaceutical Industry:
1-(4,5-Dimethyl-2-thiazolyl)-piperazine is used as a building block for the synthesis of various bioactive compounds due to its potential pharmacological activities.
Used in Antiviral Applications:
1-(4,5-Dimethyl-2-thiazolyl)-piperazine is used as an antiviral agent for its potential to combat viral infections.
Used in Antifungal Applications:
1-(4,5-Dimethyl-2-thiazolyl)-piperazine is used as an antifungal agent for its potential to treat fungal infections.
Used in Antibacterial Applications:
1-(4,5-Dimethyl-2-thiazolyl)-piperazine is used as an antibacterial agent for its potential to fight bacterial infections.
Used in Central Nervous System Depressant Development:
1-(4,5-Dimethyl-2-thiazolyl)-piperazine is used as a candidate for the development of new drugs for neurological disorders, given its potential as a central nervous system depressant.

InChI:InChI=1/C9H15N3S/c1-7-8(2)13-9(11-7)12-5-3-10-4-6-12/h10H,3-6H2,1-2H3

Upstream product

• 110-85-0 piperazine 
• 29947-24-8 2-bromo-4,5-dimethyl-1,3-thiazole 
• 675149-74-3 tert-butyl 4-(4,5-dimethyl-1,3-thiazol-2-yl)-1-piperazinecarboxylate 

Relevant academic research and scientific papers

Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition

The discovery of nitrile compound 4, a potent inhibitor of Cathepsin K (Cat K) with good bioavailability in dog is described. The compound was used to demonstrate target engagement and inhibition of Cat K in an in vivo dog PD model. The margin to hERG ion channel inhibition was deemed too low for a clinical candidate and an optimisation program to find isosteres or substitutions on benzothiazole group led to the discovery of 20, 24 and 27; all three free from hERG inhibition.

Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group

A series of (4β-substituted)-l-prolylpyrrolidine analogs lacking the electrophilic nitrile function were synthesized and their dipeptidyl peptidase IV (DPP-IV) inhibitory activity and duration of ex vivo activity were evaluated. Structural optimization of a N-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine analog 8, which was found by high-speed analog synthesis, was carried out to improve the potency and duration of action. A representative compound 26 was evaluated to assess its effect on the plasma glucose level after the oGTT (oral glucose tolerance test) in normal rats. Structure-activity relationships (SAR) are also presented.

Substituted 1-propiolylpiperazine compounds, their preparation and use

Substituted 1-propiolylpiperazine compounds corresponding to formula I in which X denotes N or C—R2, and n is an integer from 0 to 8, a method for producing such substituted 1-propiolylpiperazine compounds, pharmaceutical compositions containing such substituted 1-propiolylpiperazine compounds, and the use of such substituted 1-propiolylpiperazine compounds for modulating mGluR5 receptor activity or for treating or inhibiting pain and various other conditions, especially conditions at least partly mediated by the mGluR5 receptor.

[4-(HETEROARYL) PIPERAZIN-1-YL]-(2,5-SUBSTITUTED -PHENYL)METHANONE DERIVATIVES AS GLYCINE TRANSPORTER 1 (GLYT-1) INHIBITORS FOR THE TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS

The present invention relates to compounds of the general formula (I) wherein R1 is-OR1’,-SR1’ or is a heterocycloalkyl group; R1’ is lower alkyl, lower alkyl substituted by halogen or is -(CH2)n