84352-95-4

Usage

Chemical compound

5-(4-chlorophenyl)-1,3,4-thiadiazol-2(3H)-one

Heterocyclic compound

Contains a thiadiazole ring

Biological activities

Antimicrobial, antiviral, anticancer

Potential use

Herbicide

Structural diversity

Potential pharmaceutical applications

Interest for research

Medicinal and agricultural chemistry

Upstream product

• 32315-10-9 bis(trichloromethyl) carbonate 
• 50487-61-1 4-chlorothiobenzoylhydrazine 
• 536-40-3 4-chlorobenzoic acid hydrazide 
• 530-62-1 1,1'-carbonyldiimidazole 
• 97051-24-6 2-ethylsulfonyl-5-p-chlorophenyl-1,3,4-thiadiazole 

Downstream Products

• 97051-22-4 5-(4-Chloro-phenyl)-3-(4-morpholin-4-yl-but-2-ynyl)-3H-[1,3,4]thiadiazol-2-one; hydrochloride 
• 97051-20-2 5-(4-Chloro-phenyl)-3-[4-((2S,6R)-2,6-dimethyl-piperidin-1-yl)-but-2-ynyl]-3H-[1,3,4]thiadiazol-2-one; hydrochloride 
• 97064-77-2 3-(4-Azepan-1-yl-but-2-ynyl)-5-(4-chloro-phenyl)-3H-[1,3,4]thiadiazol-2-one; hydrochloride 
• 97051-19-9 5-(4-Chloro-phenyl)-3-[4-(2-methyl-piperidin-1-yl)-but-2-ynyl]-3H-[1,3,4]thiadiazol-2-one; hydrochloride 
• 97051-18-8 5-(4-Chloro-phenyl)-3-(4-piperidin-1-yl-but-2-ynyl)-3H-[1,3,4]thiadiazol-2-one; hydrochloride 
• 97051-17-7 5-(4-Chloro-phenyl)-3-(4-pyrrolidin-1-yl-but-2-ynyl)-3H-[1,3,4]thiadiazol-2-one; hydrochloride 
• 97050-90-3 5-(4-Chloro-phenyl)-3-[4-(4-methyl-piperazin-1-yl)-but-2-ynyl]-3H-[1,3,4]thiadiazol-2-one 
• 97051-28-0 5-(4-Chloro-phenyl)-3-prop-2-ynyl-3H-[1,3,4]thiadiazol-2-one 

Relevant academic research and scientific papers

5-Phenyl-1,3,4-oxadiazol-2(3 H)-ones Are Potent Inhibitors of Notum Carboxylesterase Activity Identified by the Optimization of a Crystallographic Fragment Screening Hit

Carboxylesterase Notum is a negative regulator of the Wnt signaling pathway. There is an emerging understanding of the role Notum plays in disease, supporting the need to discover new small-molecule inhibitors. A crystallographic X-ray fragment screen was performed, which identified fragment hit 1,2,3-Triazole 7 as an attractive starting point for a structure-based drug design hit-To-lead program. Optimization of 7 identified oxadiazol-2-one 23dd as a preferred example with properties consistent with drug-like chemical space. Screening 23dd in a cell-based TCF/LEF reporter gene assay restored the activation of Wnt signaling in the presence of Notum. Mouse pharmacokinetic studies with oral administration of 23dd demonstrated good plasma exposure and partial blood-brain barrier penetration. Significant progress was made in developing fragment hit 7 into lead 23dd (>600-fold increase in activity), making it suitable as a new chemical tool for exploring the role of Notum-mediated regulation of Wnt signaling.

Tetrazolinone compound and application for same

Provided is a tetrazolinone compound given by formula (1) (wherein E represents a 5-membered aromatic hetero group, such as the pyrazolyl group, the thiazolyl group, or the imidazolyl group; R4 and R5 represent hydrogen atoms or the like; R6 represents a C1-12 alkyl group; R7, R8, and R9 represent hydrogen atoms or the like; R10 represents a C1-3 alkyl group, or a C1-3 haloalkyl group; Y represents an oxygen atom or the like; and Q represents an oxygen atom or the like), and having exceptional efficacy in controlling harmful organisms.

Synthesis and biological evaluation of 5-aryl-3-(4-tert-amino-2-butynyl)-1,3,4-thiadiazol-2 (3H)-ones

A series of 5-aryl-3-(4-tert-amino-2-butynyl)-1,3,4-thiadiazol-2 (3H)-ones has been prepared and investigated for blocking motor effects of oxotremorine in intact mice and for their antagonistic activity towards acetylcholine on isolated guinea pig ileal