69159-50-8

Usage

Uses

Used in Pharmaceutical Industry:
1-(Dibenzosuberyl)piperazine is used as a potential antipsychotic agent for its ability to interact with receptors in the central nervous system, offering a new approach to managing psychotic disorders.
1-(Dibenzosuberyl)piperazine is used as a potential antidepressant agent due to its role in modulating serotonin and dopamine neurotransmission, which are crucial for mood regulation.
Used in Pain Management:
1-(Dibenzosuberyl)piperazine is used as a potential analgesic for its potential to interact with opioid receptors, providing a novel avenue for pain relief.
Used in Neurotransmission Modulation:
1-(Dibenzosuberyl)piperazine is used as a modulator of neurotransmission for its influence on serotonin and dopamine levels, which are vital for various neurological functions and mental health conditions.
Used in Anti-inflammatory Applications:
1-(Dibenzosuberyl)piperazine is used as an anti-inflammatory agent for its potential to reduce inflammation, which can be beneficial in treating various inflammatory conditions.
Used in Oncology:
1-(Dibenzosuberyl)piperazine is used as a potential anti-cancer agent for its potential to target and inhibit cancer cell growth, offering a new therapeutic option for cancer treatment.

InChI:InChI=1/C19H22N2/c1-3-7-17-15(5-1)9-10-16-6-2-4-8-18(16)19(17)21-13-11-20-12-14-21/h1-8,19-20H,9-14H2

Upstream product

• 110-85-0 piperazine 
• 1210-33-9 5-chlorodibenzosuberane 
• 121942-85-6 1-(ethoxycarbonyl)-4-(10,11-dihydro-5H-dibenzocycloheptene-5-yl)piperazine 
• 1210-34-0 dibenzosuberol 
• 108-20-3 di-isopropyl ether 
• 1210-35-1 10,11-Dihydro-5H-dibenzo[a,d]cyclohepten-5-one 

Downstream Products

• 129716-45-6 MS 073 

Relevant academic research and scientific papers

Reversed isoniazids: Design, synthesis and evaluation against Mycobacterium tuberculosis

Novel reversed isoniazid (RINH) agents were synthesized by covalently linking isoniazid with various efflux pump inhibitor (EPI) cores and their structural motifs. These RINH agents were then evaluated for anti-mycobacterial activity against sensitive, isoniazid mono-resistant and MDR clinical isolates of M. tuberculosis and a selected number of compounds were also tested ex vivo for intracellular activity as well as in the ethidium bromide (EB) assay for efflux pump inhibition efficacy. The potency of some compounds against various strains of M. tuberculosis (4a–c, 7 and 8; H37Rv-MIC99 ≤1.25 μM, R5401-MIC99 ≤2.5 μM, X_61-MIC99 ≤5 μM) demonstrated the potential of the reversed anti-TB agent strategy towards the development of novel anti-mycobacterial agents to address the rapidly growing issue of resistance. Further, macrophage activity with >90% inhibition by 1a–c and 3b (MIC90 ≤13.42 μM) and inhibition of EB efflux demonstrated by these compounds are encouraging.

The second aryl piperazine compounds and their pharmaceutical use (by machine translation)

The invention relates to the general formula I indicated by the two aryl piperazine compound, solvate, stereoisomer or a pharmaceutically acceptable salt thereof, pharmaceutical compositions containing them, and the compounds for the preparation for preventing or treating post-surgical pain, migraine, visceral pain, neuropathic pain such as the pain and analgesics such as by analgesic drug addiction and tolerance caused by the use of disease. (by machine translation)

Piperazinyl-substituted pyridylalkane, alkene and alkine carboxamides

The invention relates to new piperazinyl-substituted pyridylalkane, alkene, and alkine acid amides substituted with saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group according to the general formula (I) as well as methods for the production of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.

Heterocyclic compounds

The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula wherein X, Y, Z, R1, R2 and m are as defined in the detailed part of the present description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation, as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.

Amino acid derivative having anti-CCK activity

A compound represented by the formula (1): STR1 wherein, m is an integer of 1 to 3; n is an integer 0 or 1; A represents CH or N atom, and forms together with the N atom bonded to the carbonyl group a piperidine ring or a piperazine ring; R1 independently represents a straight or branched chain alkyl group having 1 to 4 carbon atoms; a cycloalkyl group having 3 to 8 carbon atoms; a phenyl group, unsubstituted or substituted with a halogen atom or with an alkoxy group having 1 to 4 carbon atoms; or a pyridyl group; or two R1, together with the group >CH-- to which they bind, form a dibenzo cycloheptenyl group or a fluorenyl group; R2 represents a phenyl group substituted with a carboxyl or substituted carboxyl group; a pyridyl group substituted with a carboxyl or substituted carboxyl group, a pyrazyl group substituted with a carboxyl or substituted carboxyl group, an oxazolyl substituted with a carboxyl or substituted carboxyl group, a triazolyl substituted with one or two carboxyl or substituted carboxyl groups, or a phosphonopyridyl group; and R3 represents an indolyl group unsubstituted or substituted with a substituent selected from the group consisting of a halogen atom, a hydroxy group, an alkoxy group having 1 to 4 carbon atoms and methoxycarbonyl ethyl group and the pharmaceutically acceptable salts thereof.

Structure-activity relationship of newly synthesized quinoline derivatives for reversal of multidrug resistance in cancer

The effect of 24 newly synthesized quinoline derivatives on tumor cell multidrug resistance (MDR) was examined in vitro. At low concentrations, these compounds enhanced the accumulation of [3H]vincristine in K562/ADM cells and reversed tumor cell MDR. The results of the structure-activity relationship analysis indicate that in highly active compounds the two aryl rings in the hydrophobic moiety deviate from a common plane, so they are capable of interacting with hydrogen bond donors of P-170 glycoprotein (P- gp) via π-hydrogen-π interactions. Other major structural features which influence the MDR-reversing activities of these compounds are a quinoline nitrogen atom and a basic nitrogen atom in piperazine. Furthermore, in highly active compounds, the distance between the hydrophobic moiety and the basic nitrogen atom (an atom connected to 2-hydroxypropoxyquinoline) must be at least 5 A?. Several compounds were found to reverse vincristine resistance in K562/ADM cells in vitro, and compound 16 (MS-209) was selected for clinical studies.

Bis-benzo or benzopyrido cyclohepta piperidene, piperidylidene and piperazine compounds, compositions and methods of use

Bis-benzo or benzopyrido piperidene, piperidylidene and piperazine compounds of the formula: STR1 and pharmaceutically acceptable salts thereof are disclosed, wherein Z represents --(C(Ra)2)m --Y--(C(Ra)2)n -- or STR2 The compounds of Formula I possess anti-allergic and anti-inflammatory activity. Methods for preparing and using the compounds are also described.

Bis-benzo, cyclohepta piperidylidene, piperidine and piperazine compounds, compositions and methods of use

Bis-benzo cyclohepta piperidine, piperidylidene and piperazine compounds of the general formula, STR1 and pharmaceutically acceptable salts thereof are disclosed, which possess anti-allergic and/or anti-inflammatory activity. Methods for preparing and using the compounds are also described.

Quinoline derivative fumarates

Compounds having an activity to stimulate the carcinostatic effect of carcinostatic agents, which can be expressed by the following general formula (1): STR1 in which A is STR2 (in which R1, R2 and R3 are each independent

New Triazine Derivatives as Potent Modulators of Multidrug Resistance

A series of 70 triazine derivatives have been synthesized and tested for their capacity to modulate multidrug resistance (MDR) in DC-3F/AD and KB-A1 tumor cells in vitro, in comparison with verapamil (VRP), a calcium channel antagonist currently used in therapy as an antihypertensive drug, which also shows MDR modulating activity.Among the 12 selected compounds, 16 (S9788) showed high MDR reversing properties in vitro (300- and 6-fold VRP at 5μM in DC-3F/AD and KB-A1 cells, respectively) and induced a strong accumulation of adriamycin.The relationship between the increase of ADR accumulation and the fold reversal induced by these compounds and their lack of effects on the sensitive DC-3F cells suggest that they act mainly by inhibiting the P-glycoprotein (Pgp) catalyzed efflux of cytotoxic agents, as already described for a majority of MDR modulators.In vivo, in association with the antitumor drug vincristine (0.25 mg/kg), 16 (100 mg/kg) increased the T/C by 39percent in mice bearing the resistant tumor cell line P388/VCR.According to these interesting properties, 16 was selected for a clinical development because it is more bioavailable than 34, even though it was less active.