63002-49-3

Basic information

• Product Name: 3-CHLORO-N''-(CHLOROACETYL)BENZOHYDRAZIDE
• Synonyms: 3-chloro-N'-(2-chloroacetyl)benzohydrazide
• CAS NO: 63002-49-3
• Molecular Formula: C₉H₈Cl₂N₂O₂
• Molecular Weight: 247.08
• Mol File: 63002-49-3.mol
• Article Data: 3

Chemical Properties

• Appearance: /
• CAS DataBase Reference: 3-CHLORO-N''-(CHLOROACETYL)BENZOHYDRAZIDE(CAS DataBase Reference)
• NIST Chemistry Reference: 3-CHLORO-N''-(CHLOROACETYL)BENZOHYDRAZIDE(63002-49-3)
• EPA Substance Registry System: 3-CHLORO-N''-(CHLOROACETYL)BENZOHYDRAZIDE(63002-49-3)

Safety Data

• Hazardous Substances Data: 63002-49-3(Hazardous Substances Data)

Upstream product

• 1128-76-3 3-chloro-benzoic acid ethyl ester 
• 79-04-9 chloroacetyl chloride 
• 1673-47-8 3-chlorobenzhydrazide 
• 535-80-8 3-chlorobenzoate 

Downstream Products

• 33575-82-5 2-(chloromethyl)-5-(3-chlorophenyl)-1,3,4-oxadiazole 

Relevant articles and documents

Synthesis and biological evaluation of honokiol derivatives bearing 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)oxazol-2(3h)-ones as potential viral entry inhibitors against sars-cov-2

The 2019 coronavirus disease (COVID-19) caused by SARS-CoV-2 virus infection has posed a serious danger to global health and the economy. However, SARS-CoV-2 medications that are specific and effective are still being developed. Honokiol is a bioactive component from Magnoliae officinalis Cortex with damp-drying effect. To develop new potent antiviral molecules, a series of novel honokiol analogues were synthesized by introducing various 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)oxazol-2(3H)-ones to its molecule. In a SARS-CoV-2 pseudovirus model, all honokiol derivatives were examined for their antiviral entry activities. As a result, 6a and 6p demonstrated antiviral entry effect with IC50 values of 29.23 and 9.82 μM, respectively. However, the parental honokiol had a very weak antiviral activity with an IC50 value more than 50 μM. A biolayer interfero-metry (BLI) binding assay and molecular docking study revealed that 6p binds to human ACE2 protein with higher binding affinity and lower binding energy than the parental honokiol. A competitive ELISA assay confirmed the inhibitory effect of 6p on SARS-CoV-2 spike RBD’s binding with ACE2. Importantly, 6a and 6p (TC50 > 100 μM) also had higher biological safety for host cells than honokiol (TC50 of 48.23 μM). This research may contribute to the discovery of potential viral entrance inhibitors for the SARS-CoV-2 virus, although 6p’s antiviral efficacy needs to be validated on SARS-CoV-2 viral strains in a biosafety level 3 facility.

Design, synthesis, and biological evaluation of novel dual FFA1 (GPR40)/PPARδ agonists as potential anti-diabetic agents

The free fatty acid receptor 1 (FFA1) and peroxisome proliferator-activated receptor δ (PPARδ) were considered as potential anti-diabetic targets, and the dual FFA1/PPARδ agonists might provide synergistic effect in insulin secretion and sensibility. Herein, we further develop dual agonists by screening 7 series of heterocycles, resulting in the discovery of compound 19 with considerable oral pharmacokinetic profile. Compound 19 exhibited a balanced potency between FFA1 and PPARδ, and high selectivity over PPARα and PPARγ. Moreover, compound 19 exerted improved glucose-lowering effects and insulin sensitivity in a dose-dependent manner, which might be attributed to its dual effects to simultaneously regulate insulin secretion and resistance. Our results extended the existing chemical space, and provided a potent tool compound 19.