65884-01-7Relevant academic research and scientific papers
Development of novel multipotent compounds modulating endocannabinoid and dopaminergic systems
Grillo, Alessandro,Chemi, Giulia,Brogi, Simone,Brindisi, Margherita,Relitti, Nicola,Fezza, Filomena,Fazio, Domenico,Castelletti, Laura,Perdona, Elisabetta,Wong, Andrea,Lamponi, Stefania,Pecorelli, Alessandra,Benedusi, Mascia,Fantacci, Manuela,Valoti, Massimo,Valacchi, Giuseppe,Micheli, Fabrizio,Novellino, Ettore,Campiani, Giuseppe,Butini, Stefania,Maccarrone, Mauro,Gemma, Sandra
, (2019/09/12)
Polypharmacology approaches may help the discovery of pharmacological tools for the study or the potential treatment of complex and multifactorial diseases as well as for addictions and also smoke cessation. In this frame, following our interest in the de
Iron-catalysed carbene-transfer reactions of diazo acetonitrile
Empel, Claire,Hock, Katharina J.,Koenigs, Rene M.
supporting information, p. 7129 - 7133 (2018/10/24)
A continuous-flow protocol for the synthesis of diazo acetonitrile was developed. It was further applied in iron-catalysed insertion reactions of diazo acetonitrile into N-H and S-H bonds to yield valuable α-substituted acetonitrile, including gram-scale synthesis.
Preparation method for alpha-cyanoamine
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Paragraph 0084; 0045, (2016/10/07)
The invention discloses a preparation method for alpha-cyanoamine. According to the method, the product alpha-cyanoamine is prepared through nucleophilic substitution in a mixed solvent in the presence of an oxidizing agent with an amine compound and cyanoacetic acid as reactants, iodide as a catalyst and sodium acetate as alkali. The catalyst used in the method has high reactivity; reaction conditions are mild; the application scope of a substrate is wide; post-treatment is convenient; the yield of the target product is high; preparation process is simple, green and environment-friendly; and used raw materials are widely available.
Cyanoacetic Acid as a Masked Electrophile: Transition-Metal-Free Cyanomethylation of Amines and Carboxylic Acids
Wang, Hongxiang,Shao, Ying,Zheng, Hao,Wang, Hanghang,Cheng, Jiang,Wan, Xiaobing
supporting information, p. 18333 - 18337 (2015/12/24)
Using cyanoacetic acid as a masked electrophile, a new cyanomethylation reaction of amines and carboxylic acids was developed, producing a variety of α-aminonitriles and cyanomethyl esters with good yields and excellent functionality tolerance. This protocol features simple manipulation, inexpensive reagents, and a wide substrate scope. Iodoacetonitrile was generated in situ from the iodination-decarboxylation of cyanoacetic acid in this transformation.
Synthesis and pharmacological evaluation of [(4-Arylpiperazin-1-yl)-alkyl]- carbamic acid ethyl ester derivatives as potential anxiolytic agents
Khatri, Manisha,Rai, Santosh K.,Ranbhor, Ranjit,Kishore, Krishna,Tiwari, Manisha
experimental part, p. 1143 - 1152 (2012/11/07)
On the basis of our earlier studies, a series of N-{4-[4-(aryl) piperazin-1-yl]-phenyl}-amine derivatives containing terminal carbamoyl fragment with alkyl spacer of different lengths (15-20) were synthesized as ligands, for 5-hydroxytryptamine-1A (5-HT1A
3-IMIDAZOLYL-INDOLES FOR THE TREATMENT OF PROLIFERATIVE DISEASES
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Page/Page column 141, (2008/12/04)
The invention relates to 3-heterocyclyl indolyl compounds capable of inhibiting the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively, said compounds having the formula (I) wherein R1, R2, R3, R4, RA, Y and Y are as defined in the specification. Due to their activity, the compounds are useful in the treatment of various disorders and diseases mediated by the activity of MDM2 and/or MDM4, or variants thereof, such as inflammatory or proliferative diseases or in the protection of cells.
Further structure-activity relationships study of hybrid 7-{[2-(4-phenylpiperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2- ol analogues: identification of a high-affinity D3-preferring agonist with potent in vivo activity with long duration
Biswas, Swati,Zhang, Suhong,Fernandez, Fernando,Ghosh, Balaram,Zhen, Juan,Kuzhikandathil, Eldo,Reith, Maarten E. A.,Dutta, Aloke K.
, p. 101 - 117 (2008/09/20)
This paper describes an extended structure-activity relationships study of aminotetralin-piperazine-based hybrid molecules developed earlier for dopamine D2/D3 receptors. Various analogues as positional isomers have been developed where location of the ph
Synthesis, characterization and in vitro biological studies of novel cyano derivatives of N-alkyl and N-aryl piperazine
Chaudhary, Preeti,Nimesh, Surendra,Yadav, Veena,Verma, Akhilesh Kr.,Kumar, Rupesh
, p. 471 - 476 (2008/02/07)
Cyano derivatives of N-alkyl and N-aryl piperazine have been synthesized and screened for antibacterial and antifungal activities. All the synthesized compounds showed the antibacterial activity against pathogenic strains of Staphylococcus aureus (MTCCB 737), Pseudomonas aeruginosa (MTCCB 741), Streptomyces epidermidis (MTCCB 1824) and Escherichia coli (MTCCB 1652) and antifungal activity against pathogenic strains of Aspergillus fumigatus (ITCC 4517), Aspergillus flavus (ITCC 5192) and Aspergillus niger (ITCC 5405). All compounds showed mild to moderate antimicrobial activity. However, compounds 3c, 4a and 6 showed potent antibacterial activity against pathogenic strains used in the study. Compounds 3a, 3b, 4b, and 4d showed mild to moderate antifungal activity against Aspergillus pathogenic strains. The compounds reported in this study were assessed for there cytotoxicity using MTT colorimetric assay on Hela cells. All the compounds showed cell viability more than the control drug gentamicin, with compound 2 having highest i.e. 95% cell viability.
Microwave assisted, highly efficient solid state N- and S-alkylation
Jaisinghani, Harsha G.,Khadilkar, Bhushan M.
, p. 3693 - 3698 (2007/10/03)
Secondary amines and thiophenols were alkylated with alkyl and benzyl halides rapidly on alumina supported potassium carbonate under solvent-free conditions using microwaves. Equimolar amounts of the secondary amine/thiophenol and alkyl halide were used. The procedure neither required any strong base nor a PTC Aniline was also monobenzylated with benzylchloride. Separation of the products from the reactants was very simple by using a nonpolar solvent for desorption.
4-Bromo-1-methoxy-N-[2-(4-aryl-1-piperazinyl)ethyl]-2- naphthalenecarboxamides: Selective dopamine D3 receptor partial agonists
Glase, Shelly A.,Akunne, Hyacinth C.,Heffner, Thomas G.,Johnson, Stephen J.,Kesten, Suzanne R.,Mackenzie, Robert G.,Manley, Peter J.,Pugsley, Thomas A.,Wright, Jon L.,Wise, Lawrence D.
, p. 1361 - 1366 (2007/10/03)
A series of 4-bromo-1-methoxy-N-[2-(4-aryl-1-piperazinyl)ethyl]-2- naphthalenecarboxamide dopamine (DA) D3 receptor agonists has been identified. These compounds were found to be selective for DA D3 over D2 receptors and were shown to be partial to full agonists as measured by stimulation of mitogenesis in D3-transfected CHO p-5 cells.
