40340-73-6

Usage

Uses

Used in Pharmaceutical Industry:
1-(2-CHLOROACETYL)-4-METHYL-PIPERAZINE HCL is used as a reagent for the preparation of 2-substituted benzimidazoles for their potential anthelmintic properties. These benzimidazoles can be further developed and utilized as drugs to combat parasitic worm infections.
Used in Chemical Synthesis:
1-(2-CHLOROACETYL)-4-METHYL-PIPERAZINE HCL is used as a key intermediate in the synthesis of various organic compounds, particularly those with potential applications in the pharmaceutical, agrochemical, and materials science industries. Its unique chemical structure allows for the creation of a wide range of derivatives with diverse properties and functionalities.

InChI:InChI=1/C7H13ClN2O/c1-9-2-4-10(5-3-9)7(11)6-8/h2-6H2,1H3

Upstream product

• 109-01-3 1-methyl-piperazine 
• 79-04-9 chloroacetyl chloride 

Downstream Products

• 94012-35-8 1-(piperazin-1-ylacetyl)-4-methylpiperazine 
• 1352948-70-9 2-(4-methylpiperazin-1-yl)-2-oxoethyl 3-((4-oxo-8-(3-(2-oxo-2,3-dihydro-1H-benzo[d]imidazol-1-yl)propyl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-3-yl)methyl)benzoat 
• 1352948-71-0 tert-butyl 3-(3-((2-(4-methylpiperazin-1-yl)-2-oxoethoxy)carbonyl)benzyl)-4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]decane-8-carboxylate 

Relevant academic research and scientific papers

Design, synthesis and evaluation of piperazine clubbed 1,2,4-triazine derivatives as potent anticonvulsant agents

The new series of N-(5,6-diphenyl-1,2,4-triazin-3-yl)-2-(4-substituted piperazin-1-yl) acetamide (RP1–5) and 2-((5,6-diphenyl-1,2,4-triazin-3-yl)thio)-1-(4- substituted piperazin-1-yl)-ethan-1-one (RP6–10) derivatives were designed and synthesised by clubbing substituted 5,6-diphenyl-1,2,4-triazine with different substituted piperazines. The synthesized compounds were tested for anticonvulsant activity and various biochemical toxicity parameters. Among the series, two compounds (2-(4-benzylpiperazin-1-yl)-N-(5,6-diphenyl-1,2,4-triazin-3-yl)acetamide (RP4), and 2?chloro-1-(4-substituted piperazin-1-yl)ethan-1-one (RP5) were found to demonstrate the most potent anticonvulsant activity in both MES and scPTZ convulsion mice models. The most active compound RP5 was effective at median doses (ED50) of 14.82 mg/kg in MES and 14.61 mg/kg in scPTZ model. The median toxic dose (TD50) was > 600 which provided the compound RP5 with high protective index of 40.48 in the MES test and 41.06 in scPTZ test. Further, both the compounds were also found to possess significant antidepressant activity. The compounds did not show any adverse effect in various parameters such as grip-strength test (skeletal muscular strength), actophotometer, and rotarod test (locomotor) as compared to the control groups. In biochemical estimation, RP4 and RP5 were found nontoxic and showed no sign of any pathological changes in blood chemistry, liver, and nephrology of the kidney. The GABA level estimation in the whole brain of mice was performed to predict the mechanistic study of the selected compounds.

Synthesis, anticancer evaluation and molecular docking studies of new benzimidazole- 1,3,4-oxadiazole derivatives as human topoisomerase types I poison

In this study, some benzimidazole-oxadiazole derivatives were synthesised and tested for their in vitro anticancer activities on five cancer cell lines, including HeLa, MCF7, A549, HepG2 and C6. Their structures were elucidated by IR, 1H-NMR,

Design and synthesis of C-19 isosteviol derivatives as potent and highly selective antiproliferative agents

Six series of novel isosteviol derivatives; modified in the C-19 position; were synthesized; and their antiproliferative activity was evaluated against three human cancer cell lines (HCT-116; BEL-7402; HepG2) and the human L02 normal cell line in vitro. M

A quinazoline derivative and its preparation method and application (by machine translation)

The invention discloses a 4 - (4 '- substituted phenyl) amino - 6, 7 - dimethoxy quinazoline derivatives; the quinazoline derivatives of the formula II synthesis method for compound 4 - (4' - hydroxy phenyl) amino - 6, 7 - dimethoxy quinazoline, type III compounds and alkaline reagent to dissolve in the solvent, stirring at room temperature the reaction 15h - 24h; after the reaction cooling and filtering to obtain the crude product, obtained after the refining of crude yellow solid powder; quinazoline derivatives of the present invention human cervical carcinoma cells, human liver cancer cells, human lung cancer cells, human breast cancer cells with human colon cancer cells has better inhibition activity, can be used as a lead compound in the treatment of cancer, its preparation method is simple and feasible, is easy to operate. (by machine translation)

Ultrasound assisted-synthesis and biological evaluation of piperazinylprop-1-en-2-yloxy-2h-chromen-2-ones as cytotoxic agents

Background: The molecular hybridization concept was used to develop novel coupled derivatives with the hope of synergistic cytotoxic activity. A novel class of 12 derivatives, containing coupled 7-oxycoumarin, piperazine, and heteryl/aryl propenone moieties namely, 4-methyl-7-(3-(4-methylpiperazin-1-yl)-3-oxo-1-substituted phenyl/heteryl prop-1-en-2-yloxy)-2h-chromen-2-ones were synthesized by an ultrasound-assisted, eco-friendly protocol. Methods: All the designed hybrids were evaluated for their in vitro cytotoxic activity against a panel of three human cancer cell lines viz MCF-7 (human breast cancer cell line), HeLa (human cervical cancer cell line), NCI-H226 (non-small cell lung cancer cell line). Most of the compounds exhibited promising cytotoxicity; some compounds have shown GI50 values similar to that of the standard drug, Adriamycin. Compounds 4d, 4b, and 4a were found to be the most promising cytotoxic derivatives in this study. Results: Molecular docking study was performed to support the effective binding of compounds at the active site of the enzyme and to know the binding mode of synthesized compounds for inhibition of topoisomarase II. Further, the compounds docking results against topoisomerase-II were in good agreement with the observed GI50 values. Conclusion: A computational study was performed for prediction of ADME properties and it was observed that the compounds exhibited good % absorption; all the tested compounds 4(a-l) followed the criteria for an orally active drug and, therefore, these compounds can have a good potential for eventual development as oral agents.

Containing substituted piperazinyl such Thienopyridine tenuifoliae derivatives and process for their preparation and use

The invention belongs to the technical field of anti-platelet aggregation drugs and provides substituent piperazinyl-containing thienopyridine ester derivatives. The molecular formula of the derivatives are as shown in the specification, wherein n1 can be

Design, Synthesis, and Biological Evaluation of Scutellarein Derivatives Based on Scutellarin Metabolic Mechanism in Vivo

Three series of scutellarein derivatives have been designed and synthesized based on metabolic mechanism of scutellarin (1) in vivo. Their thrombin inhibition activities were tested through the analyzation of prothrombin time (PT), activated partial thromboplastin time (APTT), thrombin time (TT), and fibrinogen (FIB). The antioxidant activities of these target products were assessed by 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) assay and the ability to protect PC12 cells against H2O2-induced cytotoxicity, and their solubilities were evaluated by ultraviolet (UV) spectrophotometer. The results showed that the two isopropyl groups substituted derivative (18c) demonstrated stronger anticoagulant activity, better water solubility, and good antioxidant activity compared with scutellarein (2), which warrants further development of 18c as a promising agent for ischemic cerebrovascular disease treatment. Three series of scutellarein derivatives have been designed and synthesized based on metabolic mechanism of scutellarin (1) in vivo. The results of the biological evaluation showed that the two isopropyl groups substituted derivative (18c) demonstrated stronger anticoagulant activity, better water solubility, and good antioxidant activity compared with scutellarein (2), which warrants further development of 18c as a promising agent for ischemic cerebrovascular disease treatment.

SUBSTITUTED BENZOXAZINE AND RELATED COMPOUNDS

The present invention relates to compounds including but not limited to of any one of formulas Ia, Ib, IIa, IIb, IIIa, IIIb, and IV to VI, VIIa, VIIb, VIIIa, VIIIb and VIIIc as described herein and their tautomers and/or pharmaceutically acceptable salts, compositions, and methods of uses thereof.

New 2-benzylsulfanyl-nicotinic acid based 1,3,4-oxadiazoles: Their synthesis and biological evaluation

A novel series of 5-(2-benzylsulfanyl-pyridin-3-yl)-2-(substituted)- sulfanyl-1,3,4-oxadiazoles 6a-j were synthesized from key intermediate 5-(2-benzylsulfanyl-pyridin-3-yl)-3H-[1,3,4]oxadiazole-2-thione 5. Nucleophilic substitution reactions with differe

D2 ANTAGONISTS, METHODS OF SYNTHESIS AND METHODS OF USE

Provided are D2 or D3 antagonist compounds and pharmaceutical compositions of formula I and pharmaceutically acceptable salts thereof, or isomers thereof, wherein R1, R2 and R3 are as defined herein. The invention further comprises methods for making the compounds of the invention and methods for the treatment of conditions mediated by the dopamine D2 or D3 receptor from the compounds of the invention.