68944-97-8

Upstream product

• 92-54-6 4-phenyl-1-piperazine 
• 371-40-4 4-fluoroaniline 
• 100-00-5 4-chlorobenzonitrile 
• 350-46-9 4-Fluoronitrobenzene 
• 14960-95-3 1-(4-nitro-phenyl)-4-phenyl-piperazine 

Downstream Products

• 87602-41-3 [4-(4-Phenyl-piperazin-1-yl)-phenyl]-(2,6,8-trimethyl-quinolin-4-yl)-amine 
• 87602-43-5 (6-Methoxy-2-methyl-quinolin-4-yl)-[4-(4-phenyl-piperazin-1-yl)-phenyl]-amine 
• 87602-45-7 (8-Methoxy-2-methyl-quinolin-4-yl)-[4-(4-phenyl-piperazin-1-yl)-phenyl]-amine 
• 78932-93-1 [1-(4-Methoxy-phenyl)-meth-(E)-ylidene]-[4-(4-phenyl-piperazin-1-yl)-phenyl]-amine 
• 73518-41-9 2-{[4-(4-phenyl-piperazin-1-yl)-phenylimino]-methyl}-phenol 
• 1128086-00-9 [4-(4-phenyl-piperazin-1-yl)-phenyl]-carbamic acid ethyl ester 
• 1128086-05-4 N-[4-(4-phenylpiperazin-1-yl)phenyl]acetamide 
• 78933-05-8 (4-Benzyloxy-benzyl)-[4-(4-phenyl-piperazin-1-yl)-phenyl]-amine 
• 78933-03-6 (2-Methoxy-benzyl)-[4-(4-phenyl-piperazin-1-yl)-phenyl]-amine 
• 78933-04-7 2-{[4-(4-Phenyl-piperazin-1-yl)-phenylamino]-methyl}-phenol 
• 78933-02-5 (4-Methoxy-benzyl)-[4-(4-phenyl-piperazin-1-yl)-phenyl]-amine 
• 748777-38-0 N-[4-(4-phenyl-piperazin-1-yl)-phenyl]-3-{2-[4-(4-phenyl-piperazin-1-yl)-phenylcarbamoyl]-ethyldisulfanyl}-propionamide 
• 1027594-32-6 1-(4-isocyanato-phenyl)-4-phenyl-piperazine 
• 78932-95-3 [1-(4-Benzyloxy-phenyl)-meth-(E)-ylidene]-[4-(4-phenyl-piperazin-1-yl)-phenyl]-amine 

Relevant academic research and scientific papers

RADIOLABELED COMPOUNDS

The present invention relates to radiolabeled compounds of formula (I) wherein either A, B, R1, R2, is labeled with a radionuclide selected from 3H, 11C and 18F and its use for imaging alpha synuclein and/or Abeta deposits in mammals.

Development of a potent and selective FLT3 kinase inhibitor by systematic expansion of a non-selective fragment-screening hit

A non-selective inhibitor (1) of FMS-like tyrosine kinase-3 (FLT3) was identified by fragment screening and systematically modified to afford a potent and selective inhibitor 26. We confirmed that 26 inhibited the growth of FLT-3-activated human acute myeloid leukemia cell line MV4-11. Our design strategy enabled rapid development of a novel type of FLT3 inhibitor from the hit fragment in the absence of target-structural information.

Design and synthesis of some new 1-phenyl-3/4-[4-(aryl/heteroaryl/alkyl-piperazine1-yl)-phenyl-ureas as potent anticonvulsant and antidepressant agents

A series of 1-phenyl-3/4-[4-(aryl/heteroaryl/alkyl-piperazine1-yl)-phenyl-urea derivatives (29–42) were designed, synthesized and evaluated for their anticonvulsant activity by using maximal electroshock (MES), subcutaneous pentylenetetrazole (scPTZ) seizure tests. The acute neurotoxicity was checked by rotarod assay. Most of the test compounds were found effective in both seizure tests. Compound 30 (1-{4-[4-(4-chloro-phenyl)-piperazin-1-yl]-phenyl}-3-phenyl-urea) exhibited marked anticonvulsant activity in MES as well as scPTZ tests. The phase II anticonvulsant quantification study of compound 30 indicates the ED50value of 28.5?mg/kg against MES induced seizures. In addition, this compound also showed considerable protection against pilocarpine induced status epilepticus in rats. Seizures induced by 3-mercaptopropionic acid model and thiosemicarbazide were significantly attenuated by compound 30, which suggested its broad spectrum of anticonvulsant activity. Interestingly, compound 30 displayed better antidepressant activity than standard drug fluoxetine. Moreover, compound 30 appeared as a non-toxic chemical entity in sub-acute toxicity studies.

Hydroxybenzenesulfonic compd. diaminopolysiloxane, polymer, oriented film composition, an alignment film and a liquid crystal display element

A phenylenediamine compound is shown by a formula 1, Ar being shown as a formula 2, wherein * represents the position where a group shown by the formula 2 is bonded with two -NH2 of the formula 1; R1s are independent to each other and are hydrogen atoms o

Design, synthesis and pharmacological evaluation of N-[4-(4-(alkyl/aryl/heteroaryl)-piperazin-1-yl)-phenyl]-carbamic acid ethyl ester derivatives as novel anticonvulsant agents

A series of alkyl/aryl/heteroaryl piperazine derivatives (37-54) were designed and synthesized as potential anticonvulsant agents. The target compounds are endowed with satisfactory physicochemical as well as pharmacokinetic properties. The synthesized compounds were screened for their in vivo anticonvulsant activity in maximal electroshock (MES) and subcutaneous pentylenetetrazole (sc-PTZ) seizure tests. Further, neurotoxicity evaluation was carried out using rotarod method. Structure activity relationship studies showed that compounds possessing aromatic group at the piperazine ring displayed potent anticonvulsant activity. Majority of the compounds showed anti-MES activity whereas compounds 39, 41, 42, 43, 44, 50, 52, and 53 exhibited anticonvulsant activity in both seizure tests. All the compounds except 42, 46, 47, and 50 did not show neurotoxicity. The most active derivative, 45 demonstrated potent anticonvulsant activity in MES test at the dose of 30 mg/kg (0.5 h) and 100 mg/kg (4 h) and also delivered excellent protection in sc-PTZ test (100 mg/kg) at both time intervals. Therefore, compound 45 was further assessed in PTZ-kindling model of epilepsy which is widely used model for studying epileptogenesis. This compound was effective in delaying onset of PTZ-evoked seizures at the dose of 5 mg/kg in kindled animals and significantly reduced oxidative stress better than standard drug phenobarbital (PB). In result, compound 45 emerged as a most potent and safer anticonvulsant lead molecule.

Design, synthesis, 3D pharmacophore, QSAR, and docking studies of carboxylic acid derivatives as Histone Deacetylase inhibitors and cytotoxic agents

In this study, five series of (E)-6-(4-substituted phenyl)-4-oxohex-5-enoic acids IIb-f (E), (E)-3-(4-(substituted)-phenyl)acrylic acids IIIa-g (E), 4-(4-(substituted)phenylamino)-4-oxobutanoic acids VIa,b,e, 5-(4-(substituted)phenylamino)-5-oxopentanoic acids VIIa,f and 2-[(4-(substituted)phenyl) carbamoyl]benzoic acids VIIIa,e were designed and synthesized. Selected compounds were screened in vitro for their cytotoxic effect on 60 human NCI tumor cell lines. Compound IIf (E) displayed significant inhibitory activity against NCI Non-Small Cell Lung A549/ATCC Cancer cell line (68% inhibition) and NCI-H460 Cancer cell line (66% inhibition). Moreover, the final compounds were evaluated in vitro for their cytotoxic activity on HepG2 Cancer cell line in which histone deacetylase (HDAC) is overexpressed. Compounds IIc (E), IIf (E), IIIb (E), and IIIg (E) exhibited the highest cytotoxic activity against HepG2 human cancer cell lines with IC50ranging from 2.27 to 10.71 μM. In addition, selected compounds were tested on histone deacetylase isoforms (HDAC1-11). Molecular docking simulation was also carried out for HDLP enzyme to investigate their HDAC binding affinity. In addition, generation of 3D-pharmacophore model and quantitative structure activity relationship (QSAR) models were combined to explore the structural requirements controlling the observed cytotoxic properties.

1,4-Diarylpiperazines and analogs as anti-tubercular agents: Synthesis and biological evaluation

Despite progress in modern chemotherapy to combat tuberculosis, the causative pathogen Mycobacterium tuberculosis (M.tb.) is far from eradicated. Bacillary resistance to anti-mycobacterial agents, bacillary persistence and human immunodeficiency virus (HIV) co-infection hamper current drug treatment to completely cure the infection, generating a constant demand for novel drug candidates to tackle these problems. A small library of novel heterocyclic compounds was screened in a rapid luminometric in vitro assay against the laboratory M.tb. strain H37Rv. A group of amidines was found to have the highest potency and was further evaluated for acute toxicity against C3A hepatocytes. Next, the most promising compounds were evaluated for activity against a multi-drug resistant clinical isolate. The group of amidines was also tested for their ability to kill intracellular M.tb. residing in mouse J774A.1 macrophages. Finally, we report on a correlation between the structural differences of the compounds and their anti-mycobacterial activity.

Synthesis and pharmacological evaluation of new arylpiperazines N-{4-[4-(aryl) piperazine-1-yl]-phenyl}-amine derivatives: Putative role of 5-HT1A receptors

In an attempt to design novel 5-HT1A agonists/partial agonists, based on an arylpiperazine nucleus, a series of N-{4-[4-(aryl)piperazine-1-yl]-phenyl}-amine derivatives were synthesized and biologically tested. The anxiolytic effect of the comp

Benzodiazepines as potent and selective bradykinin B1 antagonists

Antagonism of the bradykinin B1 receptor was demonstrated to be a potential treatment for chronic pain and inflammation. Novel benzodiazepines were designed that display subnanomolar affinity for the bradykinin B1 receptor (Ki = 0.59 nM) and high selectivity against the bradykinin B2 receptor (Ki > 10 nM). In vivo efficacy, comparable to morphine, was demonstrated for lead compounds in a rodent hyperalgesia model.

Compounds Acting on CVS : Part I - Synthesis of 1-(p-Substituted-benzylaminophenyl)-4-arylpiperazines

1-(p-Nitrophenyl)-4-arylpiperazines (II), prepared by the reaction of various arylpiperazines with p-chloronitrobenzene, on reduction with Raney nickel give the corresponding 1-(p-aminophenyl)-4-arylpiperazines (III) which are converted into 1-(p-arylideneaminophenyl)-4-arylpiperazines (IV) by condensation with appropriate araldehydes.Reduction of IV with Pd/C im DMF furnishes the title compounds.Some of these compounds have been found to possess marked cardiovascular activity.Compound IVk exhibits maximum hypotensive activity (38.2 percent) and blocks the carotid occlu-sion response without affecting noradrenaline response indicating a neural (central/peripheral) origin for the hypotensive action.