Category: 87179-40-6

Malinka, W. published the artcileSynthesis of some N-substituted 3,4-pyrroledicarboximides as potential CNS depressive agents, Related Products of piperazines, the publication is Pharmazie (2000), 55(1), 9-16, database is CAplus and MEDLINE.

Several novel N-substituted 3,4-pyrroledicarboximides were prepared and eleven representatives were examined in a series of in vivo CNS tests. A few of these compounds displayed a similar profile of biol. selectivity to that of 3,4-pyrroledicarboximides described previously; their structure-activity relationships are discussed.

Pharmazie published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Related Products of piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Malinka, W. published the artcileSynthesis and preliminary screening of derivatives of 2-(4-arylpiperazin- 1-ylalkyl)-3-oxoisothiazolo[5,4-b]pyridines as CNS and antimycobacterial agents, Application In Synthesis of 87179-40-6, the publication is Pharmazie (2000), 55(6), 416-425, database is CAplus and MEDLINE.

Isothiazolopyridines, e.g. I (X = S, SO₂; X¹ = CO, CH₂CH₂, CH₂CH₂CH₂; R = H, 3-Cl, 3-CF₃, 2-MeO), were prepared that possess a side chain at the isothiazole ring typical, among others, for trazodone or NAN-195. Representatives of these novel isothiazolopyridines were examined for acute toxicity and in several commonly used CNS tests in mice and for arterial blood pressure in rats. Three of the five compounds tested showed significant analgesic activity. The most active compound, I (X = S; X¹ = CH₂CH₂; R = 3-Cl) exhibited analgesic action in the writhing test in a dose 1/1280 of LD₅₀ (LD₅₀ = 1135.5 mg/kg) after administration i.p. to mice. Addnl., the compounds described here and related isothiazolopyridines obtained previously were evaluated against Mycobacterium tuberculosis H₃₇Rv at 12.5 μg/mL in in vitro assays. Seven of the nineteen compounds tested showed 100% inhibition of that mycobacterium.

Pharmazie published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Application In Synthesis of 87179-40-6.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Hattori, Kazuyuki published the artcilePd/C(en)-catalyzed chemoselective hydrogenation with retention of the N-Cbz protective group and its scope and limitations, Application In Synthesis of 87179-40-6, the publication is Tetrahedron (2000), 56(43), 8433-8441, database is CAplus.

A chemoselective method for the hydrogenation of acetylene, olefin, azide, nitro and benzyl ester functionalities with retention of the aliphatic N-Cbz group was established. The chemoselectivity was accomplished by using a combination of 5% Pd/C-ethylenediamine [5% Pd/C(en)] and THF (or 1,4-dioxane) as a solvent, and the scope and limitations of this methodol. were investigated. These results reinforce the utility of N-Cbz protective groups in synthetic chem., especially in peptide synthesis.

Tetrahedron published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Application In Synthesis of 87179-40-6.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Kurokawa, Mikio published the artcileSynthesis and biological activity of 11-[4-(cinnamyl)-1-piperazinyl]-6,11-dihydrodibenz[b,e]oxepin derivatives, potential agents for the treatment of cerebrovascular disorders, Category: piperazines, the publication is Chemical & Pharmaceutical Bulletin (1991), 39(10), 2564-73, database is CAplus and MEDLINE.

A series of 11-[4-(cinnamyl)-1-piperazinyl]-6,11-dihydrodibenz[b,e]oxepins and related compounds were synthesized and evaluated for their protective activities against complete ischemia, normobaric hypoxia, lipid peroxidation and convulsion. Structure-activity relationship studies of this series led to the finding of (E)-1-(3-fluoro-6,11-dihydrodibenz[b,e]oxepin-11-yl)-4-(3-phenyl-2-propenyl)piperazine dimaleate (I), AJ-3941, with the most appropriate property for combined pharmacol. activities. I also shows an inhibitory effect against cerebral edema as well when orally given to rats.

Chemical & Pharmaceutical Bulletin published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Category: piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Guerrera, F. published the artcileSynthesis of 1-alkyl-3-dialkylaminoalkylamino[1]benzothieno[2,3-b]pyrazin-2(1H)-ones and their ability to antagonize KCl-induced contractions, HPLC of Formula: 87179-40-6, the publication is European Journal of Medicinal Chemistry (1996), 31(7-8), 607-613, database is CAplus.

A series of 1-alkyl-3-dialkylaminoalkylamino[1]benzothieno[2,3-b]pyrazin-2(1H)-ones was prepared Some of these compounds showed appreciable inhibition towards KCl-induced contractions in isolated rat aortic rings. Although this activity appears at higher concentrations than with caroverine, used as reference standard, this new tricyclic system could be considered as a nucleus with potential calcium antagonistic activity.

European Journal of Medicinal Chemistry published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, HPLC of Formula: 87179-40-6.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Dyatkin, Alexey B. published the artcileThe solid phase synthesis of complex propargylamines using the combination of Sonogashira and Mannich reactions, Quality Control of 87179-40-6, the publication is Tetrahedron Letters (1998), 39(22), 3647-3650, database is CAplus.

The Sonogashira alkynylation reaction of resin-bound iodobenzoic acids, e.g. 4-IC₆H₄CO₂H, with Me₃SiCCH followed by TBAF desilylation provided polymer-supported aryl acetylenes, e.g. 4-(HCC)C₆H₄CO₂H. Treatment of the latter with aldehydes, e.g. R¹CHO [R¹ = 4-MeC₆H₄, 3-FC₆H₄, 3-(PhO)C₆H₄, 1-naphthyl, 4-PhC₆H₄] and secondary amines, e.g. piperazines I (R² = trans-PhCH:CHCH₂, 2,3-Me₂C₆H₃, 2-FC₆H₄, cyclohexyl, Ph) in dioxane in the presence of CuCl catalyst results in the generation of resin-bound propargylamines . The final products, e.g. II, were cleaved from the resin and obtained in excellent yields and purity. This method provides a straightforward synthesis of diverse libraries of complex propargylamines.

Tetrahedron Letters published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Quality Control of 87179-40-6.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Malinka, Wieslaw published the artcileDerivatives of pyrrolo[3,4-d]pyridazinone, a new class of analgesic agents, Recommanded Product: (E)-1-Cinnamylpiperazine, the publication is European Journal of Medicinal Chemistry (2011), 46(10), 4992-4999, database is CAplus and MEDLINE.

A series of N2-{2-[4-aryl(benzyl)-1-piperazinyl(piperidinyl)]ethyl}pyrrolo[3,4-d]pyridazinones, e.g. I (R = Ph, 2-FC₆H₄, 3-F₃CC₆H₄, 2-Me-5-ClC₆H₄, PhCH₂), and related derivatives, II (R¹ = H, R² = H, MeO; R¹ = CH₂OH, R² = MeO), were synthesized as potential analgesic agents. The structures of the new compounds were elucidated by micro, spectral and X-ray anal. Analgesic activity of the compounds was investigated in the phenylbenzoquinone induced writhing’ and hot plate’ test in mice and at radioligand binding assay. At writhing’ test all compounds, without exception, were more active than acetylsalicylic acid (ASA) with ED₅₀ values ranging from 0.04 to 11 mg/kg (i.p.) (ED₅₀ for ASA – 39.15 mg/kg). Analgesic effect at the hot plate’ test was observed for three compounds I (R = 2-FC₆H₄, 3-F₃CC₆H₄, 2-Me-5-ClC₆H₄) at the dose 3-5 times higher then that of morphine (ED₅₀-3.39 mg/kg). At radioligand binding assay of I (R = 2-FC₆H₄, 3-F₃CC₆H₄, 2-Me-5-ClC₆H₄) only compound I (R = 2-Me-5-ClC₆H₄) exhibited affinity for the μ-opioid receptors similar to that of Tramadol. The acute toxicity of the pyrrolopyridazinones were also studied and non toxic effect was observed at the 2000 mg/kg ( 1420 mg/kg) i.p. dose level for compound II (R¹ = H, R² = H). On the basis of the available pharmacol. data S-A relationship is discussed. The preferred conformational characteristic of the pyrrolopyridazinones was also described.

European Journal of Medicinal Chemistry published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Recommanded Product: (E)-1-Cinnamylpiperazine.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Kamal, Ahmed published the artcileBase-free monosulfonylation of amines using tosyl or mesyl chloride in water, HPLC of Formula: 87179-40-6, the publication is Tetrahedron Letters (2008), 49(2), 348-353, database is CAplus.

A mild and efficient procedure was developed for the monosulfonylation of various amines using mesyl or tosyl chlorides in water at room temperature to afford the corresponding sulfonamides in high yields.

Tetrahedron Letters published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, HPLC of Formula: 87179-40-6.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Szkaradek, Natalia published the artcileSynthesis and preliminary evaluation of pharmacological properties of some piperazine derivatives of xanthone, Category: piperazines, the publication is Bioorganic & Medicinal Chemistry (2013), 21(2), 514-522, database is CAplus and MEDLINE.

A series of 9 piperazine derivatives of xanthone were synthesized and evaluated for cardiovascular activity. The following pharmacol. experiments were conducted: the binding affinity for adrenoceptors, the influence on the normal ECG, the effect on the arterial blood pressure and prophylactic antiarrhythmic activity in adrenaline induced model of arrhythmia (rats, iv). Three compounds revealed nanomolar affinity for α₁-adrenoceptor which was correlated with the strongest cardiovascular (antiarrhythmic and hypotensive) activity in animals’ models. The most promising compound was 4-(3-(4-(2-methoxyphenyl)piperazine-1-yl)propoxy)-9H-xanthen-9-one hydrochloride (12) which revealed antiarrhythmic activity with ED₅₀ value of 0.69 mg/kg in adrenaline induced arrhythmia (rats, iv). Other synthesized xanthone derivatives, i.e., (R,S)-4-(2-hydroxy-3-(4-(2-methoxyphenyl)piperazine-1-yl)propoxy)-9H-xanthen-9-one hydrochloride (10) and (R,S)-4-(2-acetoxy-3-(4-(2-methoxyphenyl)piperazine-1-yl)propoxy)-9H-xanthen-9-one hydrochloride (11) also acted as potential antiarrhythmics in adrenaline induced model of arrhythmia in rats after i.v. injection (ED₅₀ = 0.88 mg/kg and 0.89 mg/kg, resp.). These values were lower than values obtained for reference drugs such as propranolol and urapidil, but not carvedilol. Results were quite promising and suggested that in the group of xanthone derivatives new potential antiarrhythmics and hypotensives might be found.

Bioorganic & Medicinal Chemistry published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C17H16O2, Category: piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Kumar, Dhananjay published the artcileSynthesis of 2-N/S/C-Substituted Benzothiazoles via Intramolecular Cyclative Cleavage of Benzotriazole Ring, Quality Control of 87179-40-6, the publication is Journal of Organic Chemistry (2014), 79(1), 251-266, database is CAplus and MEDLINE.

The synthesis of numerous 2-N/S/C-substituted benzothiazoles was achieved from substituted thiocarbonylbenzotriazoles via free-radical intramol. cyclative cleavage of the benzotriazole ring in the presence of (TMS)₃SiH and AIBN under mild conditions. The developed methodol. demonstrates significant compatibility under microwave conditions and is important as it avoids the use of toxic metals for radical cyclization.

Journal of Organic Chemistry published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Quality Control of 87179-40-6.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics