1005205-25-3

Usage

Uses

Used in Pharmaceutical Industry:
1H-INDAZOLE-5-CARBOHYDRAZIDE is used as a key intermediate in the synthesis of pharmaceuticals for its potential as an anti-tumor agent. It aids in the development of new drugs targeting cancer treatment, offering a promising avenue for research and medicinal chemistry.
Used in Organic Compounds and Derivatives Development:
1H-INDAZOLE-5-CARBOHYDRAZIDE is used as a versatile building block for the creation of various organic compounds and derivatives. Its role in chemical synthesis is crucial for a range of industrial processes, enhancing the compound's utility across different sectors.
Used in Corrosion Inhibition Studies:
1H-INDAZOLE-5-CARBOHYDRAZIDE has been studied for its potential as a corrosion inhibitor. It is used in research to explore its effectiveness in protecting materials from corrosion, which could have significant applications in industries where material durability and protection are critical.

Upstream product

• 473416-12-5 methyl 1H-indazole-5-carboxylate 
• 61700-61-6 1H-indazole-5-carboxylic acid 
• 192944-51-7 1H-indazole-5-carboxylic acid ethyl ester 
• 271-44-3 benzimidazole 

Downstream Products

• 1005205-29-7 N'-[3-[3-(trifluoromethyl)phenyl]propionyl]-1H-indazole-5-carbohydrazide 
• 1041481-22-4 C₁₆H₁₃N₅O 

Relevant academic research and scientific papers

Identification of N-acylhydrazone derivatives as novel lactate dehydrogenase A inhibitors

Abstract Glycolysis is drastically increased in tumors and it is the main route to energy production with a minor use of oxidative phosphorylation. Among the key enzymes in the glycolytic process, LDH is emerging as one of the most interesting targets for the development of new inhibitors. In this context, in the present work, we carried out a virtual screening procedure followed by chemical modifications of the identified structures according to a "hit-to-lead" process. The effects of the new molecules were preliminary probed against purified human LDH-A. The compounds active at low micromolar level were additionally characterized for their activity on some cellular metabolic processes by using Raji human cell line. Within the series, 1 was considered the best candidate, and a more detailed characterization of its biological properties was performed. In Raji cells exposed to compound 1 we evidenced the occurrence of effects usually observed in cancer cells after LDH-A inhibition: reduced lactate production and NAD/NADH ratio, apoptosis. The flow cytometry analysis of treated cells also showed cell cycle changes compatible with effects exerted at the glycolytic level. Finally, in agreement with the data obtained with other inhibitors or by silencing LDH-A expression, compound 1 was found to increase Raji cells response to some commonly used chemotherapeutic agents. Taken together, all these finding are in support of the LDH-A inhibiting activity of compound 1.

ASK1 inhibitor, derivative, preparation method, pharmaceutical composition and application thereof

The invention discloses an ASK1 inhibitor, a derivative, a preparation method, a pharmaceutical composition and application thereof. The structure of the compound is shown as a formula I. The ASK1 inhibitor derivative relates to an isomer, a diastereoisom

Design, synthesis and biological evaluation of 1H-indazole derivatives as novel ASK1 inhibitors

Apoptosis signal-regulating kinase 1 (ASK1, MAP3K5), a member of the mitogen-activated protein kinase (MAPK) signaling pathway, is involved in cell survival, differentiation, stress response, and apoptosis. ASK1 kinase inhibition has emerged as a promisin

The optimization of aminooxadiazoles as orally active inhibitors of Cdc7

A series of aminooxadiazoles was optimized for inhibition of Cdc7. Early lead isoquinoline 1 suffered from modest cell potency (cellular IC50 = 0.71 μM measuring pMCM2), low selectivity against structurally related kinases, and high IV clearance in rats (CL = 18 L/h/kg). Extensive optimization resulted in azaindole 26 (Cdc7 IC50 = 1.1 nM, pMCM2 IC50 = 32 nM) that demonstrated robust lowering of pMCM2 in a mouse pharmacodynamic (PD) model when dosed orally. Modifications to improve the pharmacokinetic profile of this series were guided by trapping experiments with glutathione in rat hepatocytes.

GSK-3BETAINHIBITOR

For the purpose of providing a GSK-3β inhibitor containing an oxadiazole compound or a salt thereof or a prodrug thereof useful as an agent for the prophylaxis or treatment of a GSK-3β-related pathology or disease, the present invention provides a GSK-3β inhibitor containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.

Design, synthesis and structure-activity relationships of 1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3β

Glycogen synthase kinase-3β (GSK-3β) is implicated in abnormal hyperphosphorylation of tau protein and its inhibitors are expected to be a promising therapeutic agents for the treatment of Alzheimer's disease. Here we report design, synthesis and structure-activity relationships of a novel series of oxadiazole derivatives as GSK-3β inhibitors. Among these inhibitors, compound 20x showed highly selective and potent GSK-3β inhibitory activity in vitro and its binding mode was determined by obtaining the X-ray co-crystal structure of 20x and GSK-3β.

Discovery and SAR of hydrazide antagonists of the pituitary adenylate cyclase-activating polypeptide (PACAP) receptor type 1 (PAC1-R)

Potent small molecule antagonists for the PAC1-R have been discovered. Previously known antagonists for the PAC1-R were slightly truncated peptide ligands. The hydrazides reported here are the first small molecule antagonists ever reported for this class B GPCR.