582-80-9

Usage

Uses

Used in Pharmaceutical Industry:
4-(Benzoylamino)benzoic acid is used as a synthetic intermediate for the development of 8-substituted benzamido-phenylxanthine derivatives. These derivatives act as monoamine oxidase-B (MAO-B) inhibitors, which are crucial in the treatment of various neurodegenerative disorders, such as Parkinson's disease. By inhibiting MAO-B, these derivatives help in reducing the breakdown of dopamine, thereby improving the symptoms and overall quality of life for patients suffering from these conditions.

InChI:InChI=1/C14H11NO3/c16-13(10-4-2-1-3-5-10)15-12-8-6-11(7-9-12)14(17)18/h1-9H,(H,15,16)(H,17,18)

Upstream product

• 91-22-5 quinoline 
• 98-88-4 benzoyl chloride 
• 150-13-0 4-amino-benzoic acid 
• 582-78-5 N-(4-methylphenyl)benzamide 
• 65-85-0 benzoic acid 
• 64-19-7 acetic acid 
• 2797-52-6 mono-O-benzoyl maleic hydrazide 
• 848417-68-5 3,6-dibenzoyloxy-1,2-pyridazine 
• 6427-66-3 4-azidobenzoic acid 
• 59501-97-2 potassium benzeneselenocarboxylate 
• 94-09-7 p-aminoethylbenzoate 
• 611-73-4 Benzoylformic acid 
• 619-45-4 4-methoxycarbonyl aniline 
• 736-40-3 N-benzoylbenzocaine 

Downstream Products

• 102468-18-8 4-benzoylamino-benzoic acid-(4-nitro-phenacyl ester) 
• 150-13-0 4-amino-benzoic acid 
• 116247-31-5 N-{4-[5-(4-Chloro-7-trifluoromethyl-quinolin-3-yl)-[1,3,4]oxadiazol-2-yl]-phenyl}-benzamide 
• 847250-53-7 C₂₈H₂₀N₂O₅ 
• 19989-69-6 2-phenyl-1,3-benzothiazole-6-carboxylic acid 
• 1264702-23-9 N-{4-[N'-(pyridine-4-carbonyl)hydrazinocarbonyl]phenyl}benzamide 
• 1258550-43-4 4-benzamido-N-(3-nitro-4-(2-(phenylthio)ethylamino)phenylsulfonyl)benzamide 
• 1360606-65-0 C₂₀H₁₇N₅O₃ 
• 1360606-69-4 C₂₁H₁₉N₅O₃ 
• 694485-33-1 N-{4-[4-(4-methoxyphenyl)tetrahydro-2H-pyran-4-ylmethyl]carbamoylphenyl}benzamide 
• 137976-39-7 4-benzoylaminobenzoyl chloride 
• 101734-46-7 3-(4-benzoylamino-phenyl)-3-oxo-propionic acid ethyl ester 
• 935660-75-6 N-[4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)phenyl]benzamide 
• 93-98-1 N-phenyl benzoyl amide 

Relevant academic research and scientific papers

Design, synthesis, and biological activity evaluation of 2-(benzo[b]thiophen-2-yl)-4-phenyl-4,5-dihydrooxazole derivatives as broad-spectrum antifungal agents

To discover antifungal compounds with broad-spectrum and stable metabolism, a series of 2-(benzo[b]thiophen-2-yl)-4-phenyl-4,5-dihydrooxazole derivatives was designed and synthesized. Compounds A30-A34 exhibited excellent broad-spectrum antifungal activity against Candida albicans with MIC values in the range of 0.03–0.5 μg/mL, and against Cryptococcus neoformans and Aspergillus fumigatus with MIC values in the range of 0.25–2 μg/mL. In addition, compounds A31 and A33 showed high metabolic stability in human liver microsomes in vitro, with the half-life of 80.5 min and 69.4 min, respectively. Moreover, compounds A31 and A33 showed weak or almost no inhibitory effect on the CYP3A4 and CYP2D6. The pharmacokinetic evaluation in SD rats showed that compound A31 had suitable pharmacokinetic properties and was worthy of further study.

Aminobenzoic acid derivatives as antioxidants and cholinesterase inhibitors; synthesis, biological evaluation and molecular docking studies

Cholinesterase namely, acetyl- and butyrylcholinesterase (AChE and BChE, respectively), has been recognized as a primary class of enzyme that hydrolyzes the acetylcholine (ACh) neurotransmitter in synaptic junctions. Diminished levels of the neurotransmitter in synaptic junction lead to Alzheimerís disease (AD). Inhibition of cholinesterase is thus, an attractive strategy for AD treatment. The study includes the synthesis and characterization of a series of 2-, 3- and 4-aminobenzoic acid derivatives (1a?5c), their biological screening against cholinesterase enzyme and molecular docking study to demonstrate putative binding modes. Antioxidant potential of the synthesized series was also determined. The cholinesterase enzyme inhibition assay showed that compound 5b has the highest inhibition potential against acetylcholinesterase with an IC50 value of 1.66 ± 0.03 μM while in case of butyrylcholinesterase, compound 2c has the highest inhibitory potential with an IC50 value of 2.67 ± 0.05 μM. Molecular docking studies supports the results of enzyme inhibition potential with binding energy value ?G = -9.54 Kcal mol-1 for compound 5b in case for acetylcholinesterase while for butyrylcholinesterase, ?G = -5.53 Kcal mol-1 was obtained for compound 2c. The synthesized series of compounds also shows mild to moderate antioxidant potential. The benzoyl- containing compounds shows better antioxidant activity as compared to other derivatives of the synthesized series. Based on the molecular docking studies and enzyme inhibition potential, the synthesized series of compounds can be regarded as potent cholinesterase inhibitors and can be used for designing and synthesizing more potent drugs for Alzheimerís disease and neurodegenerative diseases.

Substituted pyridoimidazole derivative and preparation thereof, and applications of substituted pyridoimidazole derivative in medicines

The present invention discloses a substituted pyridoimidazole derivative and preparation thereof, and applications of the substituted pyridoimidazole derivative in medicines, and particularly relates to a new derivative represented by a general formula (I) and a pharmaceutically acceptable salt thereof or a pharmaceutical composition containing the new derivative, and a preparation method of the new derivative. The present invention further discloses applications of the derivative and the pharmaceutically acceptable salt thereof or the pharmaceutical composition containing the new derivative in Bruton tyrosine kinase inhibitors and in preparation of drugs for treatment and/or prevention of tumors, inflammations, and other diseases, wherein each substituent in the general formula (I) is defined in the specification. The formula (I) is defined in the specification.

With substituted pyrazine and imidazole derivatives, their preparation and their use in medicine (by machine translation)

The invention discloses a substituted pyrazine and imidazole derivatives, their preparation and their use in medicine. Specifically, the invention relates to a compound of general formula (I) indicated by the new derivative and its pharmaceutically acceptable salt or pharmaceutical composition containing the same, and its preparation method. The invention also discloses the derivative and its pharmaceutically acceptable salt or pharmaceutical composition containing the same in the Bruton tyrosine kinase inhibitors, and in preparing and treating and/or preventing tumor diseases such as inflammation of the application of the medicament. Wherein the general formula (I) of each substituent as defined in the specification. (by machine translation)

Derivative with imidazopyridine, preparation method and application in medicine thereof

The invention discloses a derivative with imidazopyridine, a preparation method and application in medicine thereof. Concretely speaking, the invention relates to a novel derivative, medicinal salt of the derivative or pharmaceutical compositions containing the derivative, and the preparation method of the derivative showed in general formula (I). The invention also discloses application of the derivative, medicinal salt of the derivative or pharmaceutical compositions containing the derivative in Bruton tyrosine kinase inhibitor, preparing the medicine for treating or preventing tumor and inflammation diseases. Substituent groups in general formula (I) are identical to definitions in the specification (the structure is shown in the description).

Derivative having imidazopyrazines, preparation method and application thereof of derivative on medicine

The invention discloses a derivative having imidazopyrazines, a preparation method and an application thereof of the derivative on medicine. Concretely speaking, the invention relates to a novel derivative shown in a general formula (I) and its medicinal salt or a pharmaceutical composition containing the derivative, and its preparation method. The invention also discloses the derivative or its medicinal salt or an application of the pharmaceutical composition containing the derivative in a Bruton tyrosine kinase inhibitor, and in preparation of medicines for treating and/or preventing diseases such as tumour and inflammation. The substituent in the formula (I) has same definition in the specification.

Catalyst-Free Singlet Oxygen-Promoted Decarboxylative Amidation of α-Keto Acids with Free Amines

A novel catalyst-free decarboxylative amidation of α-keto acids with amines under mild conditions has been developed. Advantages of the new protocol include avoidance of metal catalysts and high levels of functional group tolerance. In addition, the reaction can be scaled up and shows high chemoselectivity. Preliminary mechanistic studies suggest that singlet oxygen, generated from oxygen under irradiation, is the key promoter for this catalyst-free transformation.

Thermoplastic polymer composition

The invention provides a compound conforming to the structure of Formula (C) The invention also provides a thermoplastic polymer composition comprising a polyolefin polymer and a compound conforming to the structure of Formula (C) as a nucleating agent.

2-(HETERO)ARYL-BENZIMIDAZOLE AND IMIDAZOPYRIDINE DERIVATIVES AS INHIBITORS OF ASPARAGIME EMETHYL TRANSFERASE

Substituted benzimidazole and 3H-imidazo[4,5-b]pyridines or formula I: where X and Y respectively are selected from: (i) N and N; and (ii) N and CR4; A2 is selected from:, a C5 heteroarylene group, containing 2 or 3 ring heteroatoms, where the bonds to L1 and the core are β to one another; L1 is selected from: (i)A1-O-CH2-A2; (ii)A1-CH2-O-A2; (iii)A1-C(=O)-NH-A2; (iv)A1-CH(OH)-A2; (v)A1-CH2-NH-C(=O)-A2; (vi) A1-S-CH2-A2; (vii)A1- CH2-S-A2; (viii)A1-CH2-A2; and (ix)A1-CH(CH3)-O-A2; A1 is phenyl, optionally substituted by F or CF3; their use as pharmaceuticals, and in particular, in treating cancer and hemoglobinopathies.

Substituent effects on energetics of peptide-carboxylate hydrogen bonds as studied by 1H NMR spectroscopy: Implications for enzyme catalysis

Substituent effects in N-H···O hydrogen bonds were estimated by comparing the acidities of two series of model compounds: N-benzoylanthranilic acids (A) and 4-benzoylamidobenzoic acids (B). Intramolecular N-H···O hydrogen bonds were found to be present in the A series of compounds, while B acids were used as control models. The respective pKa values for A and B acids were determined experimentally in DMSO solution using proton NMR spectroscopy. With X = H, the pKa for A and B acids were observed to be 7.6 and 11.6, respectively, a difference of 4.0 units (ΔpKa). However, with X = p-NO 2, the ΔpKa value between A and B acids increased to 4.7 units: the pKa values for A and B acids were determined as 6.7 and 11.4, respectively. The ΔpKa values between A and B acids as a function of the X substituents were studied in 10 other examples. The effects of X substituents in A acids could be predicted on the basis of the observed linear Hammett correlations, and the sensitivity of each substituent effect was found to be comparable to those observed for the ionization of substituted benzoic acids (ρ = 1.04 for A acids, and ρ = 1.00 for benzoic acids).