845781-29-5

Usage

Structure

A thiazole ring attached to a chlorobenzoyl group

Type

A chemical compound and a derivative of thiazole

Applications

+ As a building block for the preparation of pharmaceutical and agrochemical compounds
+ As an intermediate in the manufacturing of dyes and other organic compounds
+ Potential use in the development of new drugs or biologically active molecules due to its studied biological activities

Need for further research

To explore its potential uses and properties.

Upstream product

• 10200-59-6 Thiazole-2-carbaldehyde 
• 36229-42-2 (3-chlorophenyl)magnesium bromide 
• 288-47-1 1,3-thiazole 
• 618-46-2 m-Chlorobenzoyl chloride 

Downstream Products

• 949934-43-4 (3-chlorophenyl)[4-(pyrrolidin-1-ylmethyl)phenyl](thiazol-2-yl)methanol 

Relevant academic research and scientific papers

DMAP-catalyzed regel-type direct C-2 (Hetero)aroylation of oxazoles and thiazoles derivatives with acid chlorides

A Regel-type transition-metal-free direct C-2 aroylation of (benzo)oxazoles, (benzo)thiazoles and 1,3,4-oxadiazoles with acid chlorides catalyzed by N,N-dimethyl-4-aminopyridine (DMAP) is described. This methodology is effective with several aroyl and het

Clotrimazole scaffold as an innovative pharmacophore towards potent antimalarial agents: Design, synthesis, and biological and structure-activity relationship studies

We describe herein the design, synthesis, biological evaluation, and structure-activity relationship (SAR) studies of an innovative class of antimalarial agents based on a polyaromatic pharmacophore structurally related to clotrimazole and easy to synthesize by low-cost synthetic procedures. SAR studies delineated a number of structural features able to modulate the in vitro and in vivo antimalarial activity. A selected set of antimalarials was further biologically investigated and displayed low in vitro toxicity on a panel of human and murine cell lines. In vitro, the novel compounds proved to be selective for free heme, as demonstrated in the β-hematin inhibitory activity assay, and did not show inhibitory activity against 14-α-lanosterol demethylase (a fungal P450 cytochrome). Compounds 2, 4e, and 4n exhibited in vivo activity against P. chabaudi after oral administration and thus represent promising antimalarial agents for further preclinical development.