5308-28-1

Usage

Uses

Used in Pharmaceutical Manufacturing:
N-Isobutyl piperazine is used as a raw material for the production of various pharmaceuticals, particularly antiviral and antimicrobial drugs. Its unique chemical structure allows it to be incorporated into the synthesis of these therapeutic agents, enhancing their efficacy and safety.
Used in Corrosion Inhibition:
N-Isobutyl piperazine is employed as a corrosion inhibitor, protecting metal surfaces from degradation and wear. Its chemical properties enable it to form a protective layer on metal surfaces, reducing the rate of corrosion and extending the service life of equipment and structures.
Used in Pesticide Formulations:
N-Isobutyl piperazine is used as a component in some pesticide formulations, enhancing the effectiveness of these products in controlling pests and diseases. Its incorporation into pesticide formulations can improve the stability, solubility, and bioavailability of active ingredients, leading to better pest control outcomes.

InChI:InChI=1/C8H18N2/c1-8(2)7-10-5-3-9-4-6-10/h8-9H,3-7H2,1-2H3

Upstream product

• 110-85-0 piperazine 
• 78-77-3 Isobutyl bromide 
• 629625-93-0 benzyl 4-iso-butylpiperazine-1-carboxylate 
• 1026893-83-3 4-Isobutyl-piperazine-1-carboxylic acid tert-butyl ester 

Downstream Products

• 102535-28-4 3-(4-Isobutyl-piperazine-1-carbonyl)-4-methoxy-benzenesulfonamide 
• 129791-92-0 rifalazil 
• 102590-21-6 1-[2-(2-chloro-benzhydryloxy)-ethyl]-4-isobutyl-piperazine 
• 305379-88-8 1-{5-[4-(3,4-dichloro-phenyl)-1H-imidazol-2-yl]-pyridin-2-yl}-4-isobutyl-piperazine, hydrochloride 
• 4649-58-5 2-(4-isobutyl-piperazin-1-yl)-ethylamine 
• 77777-04-9 8-Benzylthio-2-(N-isobutyl-piperazino)-4-morpholino-pyrimido-[5,4-d]-pyrimidine 
• 1214265-89-0 N-(4-(4-i-butylpiperazin-1-yl)cyclohexyl)acetamide 
• 1257432-85-1 1-(4-fluoro-benzenesulfonyl)-pyrrolidine-2S-carboxylic acid [2-(4-isobutyl-piperazin-1-yl)-6-(4-trifluoromethyl-phenyl)-pyrimidin-4-ylmethyl]-amide 
• 1260242-68-9 C₂₉H₃₃F₆N₇ 
• 1245319-23-6 5-amino-2-(4-fluorophenyl)-7-(4-isobutylpiperazin-1-yl)-oxazolo[5,4-d]pyrimidine 

Relevant academic research and scientific papers

Heteroaromatic acetamide derivative, preparation and applications thereof

The present invention provides a heteroaromatic acetamide derivative, a preparation and applications thereof, wherein the derivative comprises a pharmaceutically acceptable salt and/or a solvate thereof. According to the present invention, the experiment results prove that the heteroaromatic acetamide derivative can specifically bind to transient receptor potential ankyrin 1 (TRPA1) and inhibit orreduce the activity of TRPA1, and can be used for treating diseases mediated by TRPA1; and the inhibitor of the present invention further comprises a pharmaceutical composition of the compound, and amethods for preparing the compounds. The derivative has a general formula defined in the specification.

Discovery of 2-substituted 1H-benzo[d]immidazole-4-carboxamide derivatives as novel poly(ADP-ribose)polymerase-1 inhibitors with in?vivo anti-tumor activity

Novel 1H-benzo[d]immidazole-4-carboxamide derivatives bearing five-membered or six-membered N-heterocyclic moieties at the 2-position were designed and synthesized as PARP-1 inhibitors. Structure-activity relationships were conducted and led to a number of potent PARP-1 inhibitors having IC50 values in the single or double digit nanomolar level. Some potent PARP-1 inhibitors also had similar inhibitory activities against PARP-2. Among all the synthesized compounds, compound 10a and 11e displayed strong potentiation effects on temozolomide (TMZ) in MX-1?cells (PF50?=?7.10, PF50?=?4.17). In?vivo tumor growth inhibition was investigated using compound 10a in combination with TMZ, and it was demonstrated that compound 10a could strongly potentiate the cytotoxicity of TMZ in MX-1 xenograft tumor model. Two co-crystal structures of compounds 11b and 15e complexed with PARP-1 were achieved and demonstrated a unique binding mode of these benzo-imidazole derivatives.

NOVEL PHYSIOLGICALLY ACTIVE SUBSTANCES

The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.

Diaminothiazoles having antiproliferative activity

Disclosed are novel diaminothiazoles that are selective inhibitors of Cdk4. These compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds as well as intermediates useful in the preparation of the compounds.

Pyridinecarboxamide derivatives

Pyridinecarboxamide derivatives of the formula STR1 (wherein n represents an integer of 14-18, and R represents a hydrogen atom or a straight or branched C1 -C4 alkyl group) or physiologically acceptable salts thereof. The compounds have excellent inhibiting activity of cerebral edema, especially ischemic cerebral edema, and inhibiting activity of delayed death of neuronal cells (an inhibiting activity of Ca-influx in neuronal cells). Cerebral edema is a pathologic condition accompanying cerebrovascular disorders, especially the acute stage of cerebrovascular disorders and then the compounds are useful as an agent for inhibiting cerebral edema or a therapeutic agent for cerebrovascular disorders. Moreover, the compounds have no hypotensive action which is considered to be side-effect in treating the acute stage cerebrovascular disorders and hardly show a behavior suppressing action so that they are an excellent therapeutic agent for, in particular, the acute stage cerebrovascular disorders. Moreover, the compounds show a cerebral protective activity (an anti-anoxic activity), an increasing activity of cerebral blood flow, and an inhibiting activity of lipid peroxidation and these activities may lead to the increased utility as a therapeutic agent for cerebrovascular disorders.

N-acylpiperazine derivative, antibacterial drug and anti-ulcer drug

An N-acylpiperazine derivative or a salt thereof in accordance with the present invention is represented by the following formula 1: STR1 wherein R1 represents a lower alkyl, hydroxy lower alkyl, lower acyl, or arylcarbonyloxy lower alkyl group; R2 represents hydrogen atom or a lower alkyl, lower alkoxy, lower alkenyl, amino, or nitro group; R3 and R4, which are identical to or different from each other, represent hydrogen atoms, halogen atoms, or cyano, nitro, lower alkyl, or lower alkoxy groups; and n represents 0 or 1. The N-acylpiperazine derivative has anti-ulcer effect or an antibacterial activity against Helicobacter pyroli to be available for prevention or cure of ulsers.

Alkylenediamine derivative anti-ulcer drug and antibacterial drug

The invention provides a compound which has anti-ulcer effect and antibacterial activity against Helicobacter pyroli. This compound is an alkylenediamine derivative or salt which has a general formula of (1): STR1 wherein each of R4, R5/s

Structure-activity relationships of the quinolone antibacterials against mycobacteria: Effect of structural changes at N-1 and C-7

The re-emergence of tuberculosis infections which are resistant to conventional drug therapy has demonstrated the need for alternative chemotherapy against Mycobacterium tuberculosis. As part of a study to optimize the quinolone antibacterials against M. tuberculosis, we have prepared a series of N-1- and C-7-substituted quinolones to examine specific structure-activity relationships between modifications of the quinolone at these two positions and activity against mycobacteria. The compounds, synthesized by literature procedures, were evaluated for activity against Mycobacterium fortuitum and Mycobacterium smegmatis as well as Gram-negative and Gram-positive bacteria. The activity of the compounds against M. fortuitum was used as a barometer of M. tuberculosis activity. The results demonstrate that (i) the activity against mycobacteria was related more to antibacterial activity than to changes in the lipophilicity of the compounds, (ii) the antimycobacterial activity imparted by the N-1 substituent was in the order tert-butyl ≥ cyclopropyl > 2,4-difluorophenyl > ethyl ? cyclobutyl > isopropyl, and (iii) substitution with either piperazine or pyrrolidine heterocycles at C-7 afforded similar activity against mycobacteria.

Synthesis and biological activity of 3'-hydroxy-5'-aminobenzoxazinorifamycin derivatives

As a part of our studies on the syntheses of benzoxazinorifamycin derivatives, 3'-hydroxy-5'-aminobenzoxazinorifamycin derivatives were synthesized, and tested for their antimicrobial activities. The antimicrobial activities of these compounds against gram-positive and gram-negative bacteria were almost identical to those of rifampicin (RFP) and rifabutain (RFB), however, antimicrobial activities against Mycobacterium tuberculosis were superior to RFP, while being similar to RFB. 3'-Hydroxy-5'-(4-alkyl-1-piperazinyl)benzoxazinorifamycin derivatives also had in vitro potent activities against Mycobacterium avium complex (MAC). Their minimal inhibitory concentration values against MAC were 2-256 times greater than RFP and RFB. Their in vivo efficacies against M. tuberculosis and MAC, after oral administration to mice, were superior to RFP and REB, except for RFB against M. tuberculosis activity in vivo. Although they were absorbed from the gastrointestinal tract, their plasma levels were lower than that of RFP. Among these 5'-(4-alkyl-1-piperazinyl) derivatives, 3'-hydroxy-5'-(4-isobutyl-1-piperazinyl)benzoxazinorifamycin, compound 19 (KRM-1648), was selected as the most promising and its preliminary pharmacokinetic characteristics in mice were investigated. Compound 19 was distributed much more in tissues, especially in spleen and lung, than in plasma and had a long elimination time from tissues.

Ruthenium catalyzed reactions of ethylene glycol with primary amines: steric factors and selectivity control

The selectivity of reactions of ethylene glycol with primary amines in the presence of RuCl2(PPh3)3 at 120 deg C is highly dependent on the steric nature of the amine.Selectivity to di-amination is favored by smaller alkyl groups on the amine while large amines cleanly yield ethanolamines.This contrasts with the results obtained with secondary amines at this temperature, in which ruthenium-triphenylphosphine catalyst systems always favor mono-amination.In the case of sec-butyl amine, where almost equal amounts of mono- and di-aminated product are obtained, the selecti vity can be shifted to mono-amination by the addition of excess triphenylphosphine.The steric effects seen in these reactions are consistent with standard steric parameters availble from the literature.