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Usage

Uses

Used in Pharmaceutical Industry:
4-PIPERAZIN-1-YLMETHYL-BENZOIC ACID METHYL ESTER is used as a key intermediate in the synthesis of various drugs and pharmaceuticals for its ability to contribute to the development of medications with diverse therapeutic applications.
Used in Medicinal Chemistry:
4-PIPERAZIN-1-YLMYL-BENZOIC ACID METHYL ESTER is utilized as a building block in the production of other organic compounds, playing a significant role in the creation of new chemical entities with potential medicinal uses.
Used in the Development of Antipsychotic Agents:
4-PIPERAZIN-1-YLMETHYL-BENZOIC ACID METHYL ESTER is employed as a precursor in the development of antipsychotic medications, leveraging its biological activity to manage psychiatric disorders.
Used in Antihistaminic Formulations:
4-PIPERAZIN-1-YLMETHYL-BENZOIC ACID METHYL ESTER is used in the formulation of antihistamine drugs, capitalizing on its antihistaminic properties to treat conditions like allergies and histamine-mediated symptoms.
Used in Anxiolytic Medications:
4-PIPERAZIN-1-YLMETHYL-BENZOIC ACID METHYL ESTER is applied in the development of anxiolytic drugs, helping to alleviate anxiety and stress-related disorders by targeting relevant biological pathways.

InChI:InChI=1/C13H18N2O2/c1-17-13(16)12-4-2-11(3-5-12)10-15-8-6-14-7-9-15/h2-5,14H,6-10H2,1H3

Upstream product

• 110-85-0 piperazine 
• 2417-72-3 Methyl 4-(bromomethyl)benzoate 
• 1571-08-0 methyl 4-formylbenzoate 
• 34040-64-7 p-methyloxycarbonylbenzyl chloride 
• 619-66-9 4-Carboxybenzaldehyde 
• 844891-11-8 tert-butyl 4-[(4-methoxycarbonylphenyl)methyl]piperazine-1-carboxylate 
• 142-64-3 piperazine dihydrochloride 
• 142-63-2 piperazine hexahydrate 

Downstream Products

• 895519-97-8 4-((4-ethylpiperazin-1-yl)methyl)benzoic acid 
• 208754-40-9 4-((4-propylpiperazin-1-yl)methyl)benzoic acid 
• 415951-48-3 C₁₅H₂₂N₂O₂ 
• 86620-80-6 Methyl 4-[1-(2-hydroxypropyl)-piperazin-4-ylmethyl]-benzoate 

Relevant academic research and scientific papers

Synthesis, biological evaluation, and molecular docking of ((4-([1,2,4]triazolo[4,3-b][1,2,4,5]tetrazin-6-yl) piperazin-1-yl)methyl) benzohydrazide derivatives

A series of ((4-([1,2,4]triazolo[4,3-b][1,2,4,5] methyl) benzo-hydrazide derivatives was designed, synthesized, and evaluated for their inhibition activities against five tumor cells and c-Met kinase in vitro. These compounds were fully characterized by

LPAR1 Inhibitor. Medical application and preparation method thereof

LPAR1 Inhibitor, medical application and preparation method thereof, and the structural general formula I of the inhibitor is as follows. In-flight RX Alkyl groups selected from H, C1 - C6, COOCH3 , CF3 , NO2 ,

ROR [gamma]t inhibitor, preparation method and application thereof

The invention relates to the technical field of medicines, in particular to an ROR [gamma]t inhibitor, a preparation method and application thereof. The invention also relates to a pharmaceutical composition containing the compound, a method for preparing the pharmaceutical composition, and application of the compound or the pharmaceutical composition in treatment or prevention of ROR [gamma]t-mediated cancers, inflammations or autoimmune diseases of mammals, especially human beings.

Rational modifications, synthesis and biological evaluation of new potential antivirals for RSV designed to target the M2-1 protein

Respiratory syncytial virus (RSV) is the main cause of lower respiratory tract diseases in infants and young children, with potentially serious and fatal consequences associated with severe infections. Despite extensive research efforts invested in the identification of therapeutic measures, no vaccine is currently available, while treatment options are limited to ribavirin and palivizumab, which both present significant limitations. While clinical and pre-clinical candidates mainly target the viral fusion protein, the nucleocapsid protein or the viral polymerase, our focus has been the identification of new antiviral compounds targeting the viral M2-1 protein, thanks to the presence of a zinc-ejecting group in their chemical structure. Starting from an anti-RSV hit we had previously identified with an in silico structure-based approach, we have designed, synthesised and evaluated a new series of dithiocarbamate analogues, with which we have explored the antiviral activity of this scaffold. The findings presented in this work may provide the basis for the identification of a new antiviral lead to treat RSV infections.

Flavonoid derivatives as selective ABCC1 modulators: Synthesis and functional characterization

A series of chromones, bearing substituted amino groups or N-substituted carboxamide moieties in position 2, was synthesized and characterized in cellular assays for modulation of the ABC transporters ABCC1 (MDCKII-MRP1 cells), ABCB1 (Kb-V1 cells) and ABCG2 (MCF-7/Topo cells). The most potent ABCC1 modulators identified among these flavonoid-type compounds were comparable to the reference compound reversan regarding potency, but superior in terms of selectivity concerning ABCB1 and ABCG2 (2-[4-(Benzo[c][1,2,5]oxadiazol-5-ylmethyl)piperazin-1-yl]-5,7-dimethoxy-4H-chromen-4-one (51): ABCC1, IC50 11.3-1/4M; inactive at ABCB1 and ABCG2). Compound 51 was as effective as reversan in reverting ABCC1-mediated resistance to cytostatics in MDCKII-MRP1 cells and proved to be stable in mouse plasma and cell culture medium. Modulators, such as compound 51, are of potential value as pharmacological tools for the investigation of the (patho)physiological role of ABCC1.

Benzamide capped peptidomimetics as non-ATP competitive inhibitors of CDK2 using the REPLACE strategy

Inhibition of cyclin dependent kinase 2 (CDK2) in complex with cyclin A in G1/S phase of the cell cycle has been shown to promote selective apoptosis of cancer cells through the E2F1 pathway. An alternative approach to catalytic inhibition is to target the substrate recruitment site also known as the cyclin binding groove (CBG) to generate selective non-ATP competitive inhibitors. The REPLACE strategy has been applied to identify fragment alternatives and substituted benzoic acid derivatives were evaluated as a promising scaffold to present appropriate functionality to mimic key peptide determinants. Fragment Ligated Inhibitory Peptides (FLIPs) are described which potently inhibit both CDK2/cyclin A and CDK4/cyclin D1 and have preliminary anti-tumor activity. A structural rationale for binding was obtained through molecular modeling further demonstrating their potential for further development as next generation non ATP competitive CDK inhibitors.

NEW FYN KINASE INHIBITORS

The invention relates to new selective FYN kinase inhibitors of Formula (I), pharmaceutical compositions containing them, and their use for the pharmacological treatment of pain and arthritis, including osteoarthritis and rheumatoid arthritis.

Conjugating a groove-binding motif to an Ir(iii) complex for the enhancement of G-quadruplex probe behavior

In this study, the reported G-quadruplex groove binder benzo[d,e]isoquinoline was linked to a cyclometallated Ir(iii) complex to generate a highly selective DNA probe 1 that retains the favorable photophysical properties of the parent complex. The linked complex 1 showed advantages of both parent complex 2 and groove binder 3. Similar to 3, the conjugated complex 1 exhibits a superior affinity and selectivity for G-quadruplex DNA over other conformations of DNA or proteins, with the fold enhancement ratio obviously improved compared with parent complex 2. The molecular modelling revealed a groove-binding mode between complex 1 and G-quadruplex. Meanwhile 1 also possesses the prominent advantages of transition metal complex probes such as a large Stokes shift and long lifetime phosphorescence, which could be recognized in strong fluorescence media through time-resolved emission spectroscopy (TRES). We then employed 1 to develop a detection assay for AGR2, a potential cancer biomarker, as a "proof-of-principle" demonstration of the application of a linked complex for DNA-based detection in diluted fetal bovine serum. We anticipate that this conjugation method may be further employed in the development of DNA probes and have applications in label-free DNA-based diagnostic platforms.

2-ACYLAMINOTHIAZOLES FOR THE TREATMENT OF CANCER

The present invention relates to inhibitors of the oncogenic protein kinase ALK of formula (I) as herein described and pharmaceutical compositions thereof. The compounds of formula (I) are useful in the preparation of a medicament, in particular for the treatment of cancer.

COMPOSITIONS OF NOVEL OPIOID COMPOUNDS AND METHOD OF USE THEREOF

Diarylmethylpiperazine compounds are described, which are useful as mu and/or delta receptor opioid compounds, without central side effects. Pharmaceutical compositions containing such compounds are variously useful for peripheral or non-centrally mediated indications, including peripherally mediated and neuropathic pain, urogenital tract disorders, overactive bladder, urinary incontinence, sexual disorders, premature ejaculation, cough, lung edema, cardiac disorders, cardioprotection, gastro-intestinal disorders, diarrhea, irritable bowl syndrome, functional distention, immuno-modulation and anti-tumor activity.