4385-75-5

Usage

Uses

Used in Pharmaceutical Industry:
4-Pyridin-3-yl-benzoic acid is used as a building block in the synthesis of pharmaceuticals for its diverse reactivity and potential biological activity. It plays a crucial role in the development of new drugs, contributing to the advancement of medicinal chemistry.
Used in Agrochemical Industry:
In the agrochemical sector, 4-Pyridin-3-yl-benzoic acid is utilized as a key component in the synthesis of agrochemicals, such as pesticides and herbicides. Its unique structure and properties make it a valuable asset in the development of effective and environmentally friendly agricultural products.
Used in Organic Synthesis:
4-Pyridin-3-yl-benzoic acid is employed as a versatile intermediate in organic synthesis, enabling the creation of a wide range of organic compounds. Its reactivity and structural features facilitate the synthesis of complex organic molecules, contributing to the advancement of organic chemistry.
Used in Material Science:
In the field of material science, 4-Pyridin-3-yl-benzoic acid is used for its unique structure and properties, which can be leveraged to develop new materials with specific characteristics. Its potential applications include the creation of novel polymers, coatings, and other materials with tailored properties for various industries.

Upstream product

• 626-55-1 3-Bromopyridine 
• 14047-29-1 4-carboxyphenylboronic acid 
• 87199-17-5 4-formylphenylboronic acid, 
• 4385-71-1 4-(pyridin-3-yl)benzoic acid ethyl ester 
• 90395-47-4 methyl 4-(3-pyridinyl)benzoate 
• 65520-08-3 3-bromopyridine hydrochloride 
• 586-76-5 4-Bromobenzoic acid 
• 619-42-1 4-methoxycarbonylphenyl bromide 
• 1692-25-7 3-pyridylboronic acid 
• 25487-66-5 3-Carboxyphenylboronic acid 
• 127406-55-7 4-(pyridin-3-yl)benzaldehyde 
• 5720-05-8 4-methylphenylboronic acid 
• 106-38-7 para-bromotoluene 

Downstream Products

• 193152-98-6 (2R,3R)-2-(3-Cyano-benzyl)-3-(4-pyridin-3-yl-benzoylamino)-butyric acid methyl ester 
• 328125-43-5 4-(1-oxido-3-pyridinyl)benzoic acid 
• 90395-47-4 methyl 4-(3-pyridinyl)benzoate 
• 340040-62-2 3-(3-Cyanophenyl)-2-[1-(4-pyridin-3-ylbenzoyl)-pyrrolidin-2-yl]propionic acid methyl ester 

Relevant academic research and scientific papers

Design, synthesis and stepwise optimization of nitrile-based inhibitors of cathepsins B and L

Human cathepsin B (CatB) is an important biological target in cancer therapy. In this work, we performed a knowledge-based design approach and the synthesis of a new set of 19 peptide-like nitrile-based cathepsin inhibitors. Reported compounds were assayed against a panel of human cysteine proteases: CatB, CatL, CatK, and CatS. Three compounds (7h, 7i, and 7j) displayed nanomolar inhibition of CatB and selectivity over CatK and CatL. The selectivity was achieved by using the combination of a para biphenyl ring at P3, halogenated phenylalanine in P2 and Thr-O-Bz group at P1. Likewise, compounds 7i and 7j showed selective CatB inhibition among the panel of enzymes studied. We have also described a successful example of bioisosteric replacement of the amide bond for a sulfonamide one [7e → 6b], where we observed an increase in affinity and selectivity for CatB while lowering the compound lipophilicity (ilogP). Our knowledge-based design approach and the respective structure–activity relationships provide insights into the specific ligand-target interactions for therapeutically relevant cathepsins.

Structure-based drug optimization and biological evaluation of tetrahydroquinolin derivatives as selective and potent CBP bromodomain inhibitors

CBP bromodomain could recognize acetylated lysine and function as transcription coactivator to regulate transcription and downstream gene expression. Furthermore, CBP has been shown to be related to many human malignancies including acute myeloid leukemia. Herein, we identified DC-CPin734 as a potent CBP bromodomain inhibitor with a TR-FRET IC50 value of 19.5 ± 1.1 nM and over 400-fold of selectivity against BRD4 bromodomains through structure based rational drug design guided iterative chemical modification endeavoring to discover optimal tail-substituted tetrahydroquinolin derivatives. Moreover, DC-CPin734 showed potent inhibitory activity to AML cell line MV4-11 with an IC50 value of 0.55 ± 0.04 μM, and its cellular on-target effects were further evidenced by c-Myc downregulation results. In summary, DC-CPin734 showing good potency, selectivity and anti AML activity could serve as a potent and selective in vitro and in vivo probe of CBP bromodomain and a promising lead compound for future drug development.

Cadmium-based metal organic framework material as well as preparation method and application thereof

The invention discloses a cadmium-based metal organic framework material as well as a preparation method and an application thereof. The preparation method of the cadmium-based metal organic frameworkmaterial comprises steps as follows: 1) synthesis of li

Synthesis and biological evaluation of novel aromatic-heterocyclic biphenyls as potent anti-leukemia agents

As a continuation to our previous research, twenty-eight aromatic-heterocyclic biphenyls were designed and synthesized as novel Bcr-Abl inhibitors. The title compounds were investigated for their antiproliferative activities against wild K562 cells and Imatinib-resistant K562 cells (K562R). The results indicated that most of them exhibited potent Bcr-Abl inhibition and moderate antiproliferative potency against K562 cells. Furthermore, three compounds 3, 7 and 21 displayed moderate antiproliferative activities against K562R cells. Molecular docking indicated that 3 bound more tightly with Bcr-AblT315I compared to Bcr-AblWT. The higher affinity was consistent with its relatively promising K562R cell growth inhibition. These aromatic-heterocyclic biphenyls could be considered as novel lead compound for optimized as Bcr-AblT315I inhibitors. They provide a good starting point for the further development of novel anti-leukemia agents capable of dealing with clinical acquired resistance against Imatinib.

PYRROLIDINE OR THIAZOLIDINE CARBOXYLIC ACID DERIVATIVES, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN TREATING METABOLIC DISORDERSAS AS AGONISTS OF G- PROTEIN COUPLED RECEPTOR 43 (GPR43)

The present invention is directed to novel compounds of formula (I) and their use in treating and/or preventing metabolic diseases.

HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES

The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases

BENZOXAZOLE CARBOXAMIDE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)

A compound having the structure set forth in Formula (I) or Formula (II): wherein the variables Y, R1, R2, R3, and R4 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.

Structural modifications of salicylates: Inhibitors of human CD81-receptor HCV-E2 interaction

Starting point of the present paper was the result of a virtual screening using the open conformation of the large extracellular loop (LEL) of the CD81-receptor (crystal structure: PDB-ID: 1G8Q). After benzyl salicylate had been experimentally validated to be a moderate inhibitor of the CD81-LEL-HCV-E2 interaction, further optimization was performed and heterocyclic-substituted benzyl salicylate derivatives were synthesized. The compounds were tested for their ability to inhibit the interaction of a fluorescence-labeled antibody to CD81-LEL using HUH7.5 cells. No compound showed an increase concerning the inhibition of the protein-protein interaction compared to benzyl salicylate.

Biarylcarboxybenzamide derivatives as potent vanilloid receptor (VR1) antagonistic ligands

Seventeen biarylcarboxybenzamide derivatives were prepared for the study of their agonistic/antagonistic activities to the vanilloid receptor (VR1) in rat DRG neurons. The replacement of the piperazine moiety of the lead compound 1 with phenyl ring showed quite enhanced antagonistic activity. Among the prepared derivatives, N-(4-tert-butylphenyl)-4-pyridine-2-yl-benzamide (2, IC 50 = 31 nM) and N-(4-tert-butylphenyl)-4-(3-methylpyridine-2-yl) benzamide (3g, IC50 = 31 nM), showed 5-fold higher antagonistic activity than 1 in 45Ca2+-influx assay.

HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES

The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases