24225-89-6

Upstream product

• 140-28-3 N,N'-Dibenzylethylenediamine 
• 100-52-7 benzaldehyde 
• 104-71-2 N,N'-bis(benzyliden)ethylendiamine 
• 72351-59-8 ethyl 1,4-dibenzylpiperazin-2-carboxylate 
• 94437-04-4 1,4-dibenzyl-2-hydroxypiperazine 

Downstream Products

• 70403-22-4 4-(1,4-dibenzyl-piperazin-2-ylmethyl)-morpholine 
• 70403-11-1 2-(1,4-dibenzyl-2-piperazinyl)acetonitrile 
• 111760-25-9 2-dimethylaminomethyl-1,4-bis(phenylmethyl)piperazine 
• 124257-73-4 6-(acetylamino)-1,4-dibenzylhexahydro-1H-1,4-diazepine 
• 124257-72-3 2-<(acetylamino)methyl>-1,4-dibenzylpiperazine 
• 162510-50-1 ethyl (1,4-dibenzylpiperazin-2-yl)acetate 
• 116163-33-8 2-aminomethyl-1,4-di-phenylmethyl piperazine 
• 129295-48-3 1,4-dibenzyl-1,4-diazepan-6-amine 
• 141944-72-1 1-benzyl-2-(cyanomethyl)piperazine 
• 141944-77-6 1-ethyl-6-fluoro-7-<3-(cyanomethyl)-4-benzyl-1-piperazinyl>-1,4-dihydro-4-oxo-3-quinolinecaboxylic acid 
• 70403-32-6 4-piperazin-2-ylmethyl-morpholine 
• 769159-55-9 1,4-dibenzyl-2-[1,2,4]triazol-1-ylmethylpiperazine 
• 2465-79-4 2-(piperazin-2-yl)acetonitrile 
• 368441-98-9 methyl piperazin-2-ylacetate 

Relevant academic research and scientific papers

Design, synthesis and evaluation against Mycobacterium tuberculosis of azole piperazine derivatives as dicyclotyrosine (cYY) mimics

Three series of azole piperazine derivatives that mimic dicyclotyrosine (cYY), the natural substrate of the essential Mycobacterium tuberculosis cytochrome P450 CYP121A1, were prepared and evaluated for binding affinity and inhibitory activity (MIC) against M. tuberculosis. Series A replaces one phenol group of cYY with a C3-imidazole moiety, series B includes a keto group on the hydrocarbon chain preceding the series A imidazole, whilst series C explores replacing the keto group of the piperidone ring of cYY with a CH2-imidazole or CH2-triazole moiety to enhance binding interaction with the heme of CYP121A1. The series displayed moderate to weak type II binding affinity for CYP121A1, with the exception of series B 10a, which displayed mixed type I binding. Of the three series, series C imidazole derivatives showed the best, although modest, inhibitory activity against M. tuberculosis (17d MIC = 12.5 μg/mL, 17a 50 μg/mL). Crystal structures were determined for CYP121A1 bound to series A compounds 6a and 6b that show the imidazole groups positioned directly above the haem iron with binding between the haem iron and imidazole nitrogen of both compounds at a distance of 2.2 ?. A model generated from a 1.5 ? crystal structure of CYP121A1 in complex with compound 10a showed different binding modes in agreement with the heterogeneous binding observed. Although the crystal structures of 6a and 6b would indicate binding with CYP121A1, the binding assays themselves did not allow confirmation of CYP121A1 as the target.

AZAQUINAZOLINE INHIBITORS OF ATYPICAL PROTEIN KINASE C

The present invention provides a compound of formula (I) or a salt thereof, wherein R7, R8, R9, G, and X are as defined herein. A compound of formula (I) and its salts have a PKC inhibitory activity, and may be used to treat proliferative disorders.

DIBENZO[B,F][1,4]OXAZAPINE COMPOUNDS

The present invention relates to 11-(piperazin-l-yl)dibenzo[b,f][l,4]oxazapine compounds of the formula I (I) where the variables are as defined herein, their salts and pharmaceutically acceptable compositions thereof. Methods of preparing these compounds are also described. These compounds may be used in the treatment of disorders such as schizophrenia, treatment resistant schizophrenia, bipolar disorder, psychotic depression, treatment resistant depression, schizophrenia-associated depression, treatment resistant OCD, autism, senile psychosis, psychotic dementia, L-DOPA induced psychosis, psychogenic polydipsia, psychotic symptoms of neurological disorders, sleep disorders.

2-PHENOXY- AND 2-PHENYLSULFOMAMIDE DERIVATIVES WITH CCR3 ANTAGONISTIC ACTIVITY FOR THE TREATMENT OF ASTHMA AND OTHER INFLAMMATORY OR IMMUNOLOGICAL DISORDERS

The present invention relates to a benzenesulfonamide derivative of formula (I), which is useful as an active ingredient of pharmaceutical preparations. The benzenesulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) ant

Design and synthesis of imidazoline derivatives active on glucose homeostasis in a rat model of type ii diabetes. 2. Syntheses and biological activities of 1,4-dialkyl-, 1,4-dibenzyl, and 1-benzyl-4-alkyl-2-(4',5'- dihydro-1'H-imidazol-2'-yl)piperazines and isosteric analogues of imidazoline

Piperazine derivatives have been identified as new antidiabetic compounds. Structure-activity relationship studies in a series of 1-benzyl- 4-alkyl-2-(4',5'-dihydro-1'H-imidazol-2'-yl)piperazines resulted in the identification of 1-methyl-4-(2',4'-dichlorobenzyl)-2-(4',5'-dihydro-1'H- imidazol-2'-yl)piperazine, PMS 812 (S-21663), as a highly potent antidiabetic agent on a rat model of diabetes, mediated by an important increase of insulin secretion independently of α2 adrenoceptor blockage. These studies were extended to find additional compounds in these series with improved properties. In such a way, substitution of both piperazine N atoms was first optimized by using various alkyl, branched or not, and benzyl groups. Second, some modifications of the imidazoline ring and its replacement by isosteric heterocycles were carried out, proceeding from PMS 812, to evaluate their influence on the antidiabetic activity. The importance of the distance between the imidazoline ring and the piperazine skeleton was studied third. Finally, the influence of the N-benzyl moiety was also analyzed compared to a direct N-phenyl substitution. The pharmacological evaluation was performed in vivo using glucose tolerance tests on a rat model of type II diabetes. The most active compounds were 1,4-diisopropyl-2-(4',5'-dihydro-1'H-imidazol-2'- yl)piperazine (41a), PMS 847 (S-22068), and 1,4-diisobutyl-2-(4',5'-dihydro- 1'H-imidazol-2'-yl)piperazine (41b), PMS 889 (S-22575), which strongly improved glucose tolerance without any side event or hypoglycemic effect. More particularly, PMS 847 proved to be as potent after po (100 μmol/kg) as after ip administration and appears as a good candidate for clinical investigations.

Substituted piperazines for treatment of non-insulin dependent diabetes

A compound selected from those of formula (I): STR1 in which A represents STR2 X represents N-R 4 or oxygen, and R 1, R 2, R 3, R 4, R 5, n and m are as defined in the description, useful in improving glucose tolerance in the treatment of non-insulin-dependent diabetes.

7-(substituted)piperazinyl-1-ethyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids

7-(substituted)piperazinyl-1-ethyl-6-fluoro-4-oxo-3-quinolinecarboxylic acids, the pharmacologically acceptable salts thereof, compositions containing them, processes and intermediates for producing them, and methods of using them to treat bacterial infections in warm-blooded animals.

1-tertiary-alkyl-substituted naphthyridine carboxylic acid antibacterial agents

There are disclosed new naphthyridine- and quinoline-carboxylic acids having a 1-tertiary-alkyl substituent, compositions containing them, and their use in treating bacterial infections in warm-blooded animals. Also disclosed are novel amines and intermediates used in the preparation of the naphthyridine- and quinoline-carboxylic acids.

Synthesis and Structure-Activity Relationships of 5-Substituted 6,8-Difluoroquinolones, Including Sparfloxacin, a New Quinolone Antibacterial Agent with Improved Potency

A series of 5,7-disubstituted 1-cyclopropyl-6,8-difluoro-4(1H)-oxoquinoline-3-carboxylic acids (10-36) were prepared; the C-5 substituent in these compounds comprised halo, hydroxy, mercapto, and amino groups and the C-7 functional group included variously substituted piperazines.In vitro antibacterial screening results indicated that the amino group was optimal among the C-5 substituents.A combination of the C-5 amino group and the C-7 3,5-dimethylpiperazinyl appendage in this series conferred the best overall antibacterial property with lack of adverse drug interactions.Compound 36k was superior to ciprofloxacin in both in vitro and in vivo potency and hence was selected as a promising candidate for an improved therapeutic agent.