Tag: M.W=200-250

Deng, Yongqi published the artcileDiscovery of Novel, Dual Mechanism ERK Inhibitors by Affinity Selection Screening of an Inactive Kinase, COA of Formula: C16H18N2, the publication is Journal of Medicinal Chemistry (2014), 57(21), 8817-8826, database is CAplus and MEDLINE.

An affinity-based mass spectrometry screening technol. was used to identify novel binders to both nonphosphorylated and phosphorylated ERK2. Screening of inactive ERK2 identified a pyrrolidine analog 1 that bound to both nonphosphorylated and phosphorylated ERK2 and inhibited ERK2 kinase activity. Chem. optimization identified compound 4 as a novel, potent, and highly selective ERK1,2 inhibitor which not only demonstrated inhibition of phosphorylation of ERK substrate p90RSK but also demonstrated inhibition of ERK1,2 phosphorylation on the activation loop. X-ray cocrystallog. revealed that upon binding of compound 4 to ERK2, Tyr34 undergoes a rotation (flip) along with a shift in the poly-Gly rich loop to create a new binding pocket into which 4 can bind. This new binding mode represents a novel mechanism by which high affinity ATP-competitive compounds may achieve excellent kinase selectivity.

Journal of Medicinal Chemistry published new progress about 180698-19-5. 180698-19-5 belongs to piperazines, auxiliary class Piperazine,Benzene, name is 1-Biphenyl-4-yl-piperazine, and the molecular formula is C16H18N2, COA of Formula: C16H18N2.

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

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

Yadav, Mangal S. published the artcileSilicon Industry Waste Polymethylhydrosiloxane-Mediated Benzotriazole Ring Cleavage: A Practical and Green Synthesis of Diverse Benzothiazoles, Application of (E)-1-Cinnamylpiperazine, the publication is ACS Omega (2019), 4(4), 6681-6689, database is CAplus and MEDLINE.

A green modification has been introduced to the synthesis of benzothiazoles by using polymethylhydrosiloxane (PMHS) for successive steps of benzotriazole ring cleavage (BtRC) and cyclization; an approach which was previously developed in our lab by use of n-Bu₃SnH. The use of silicone industry byproduct PMHS makes this protocol cost-effective and non-toxic one and thus may be considered for the industrial importance.

ACS Omega 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 C26H41N5O7S, Application of (E)-1-Cinnamylpiperazine.

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

Niewiadomy, Andrzej published the artcileSynthesis and biological activity of novel N,n-cyclic-2,4-dihydroxythiobenzamide derivatives, Name: (E)-1-Cinnamylpiperazine, the publication is Acta Poloniae Pharmaceutica (2015), 72(5), 943-950, database is CAplus.

A series of novel N,N-cyclic-2,4-dihydroxythiobenzamide derivatives is described. Test compounds were formed by the reaction of the com. available reagents with sulfinylbis[(2,4- dihydroxyphenyl)methanethione] (STB). The chem. structures were confirmed by IR, 1H NMR, 13CNMR, EI-MS, and elemental anal. For the estimation of potential activity in vitro, the MIC values against strains of Candida were determined Antifungal properties of selected compounds under in vitro conditions against five phytopathogenic fungi were estimated Furthermore, the antiproliferative activity against the HCV29T cancer cell lines has been studied. These compounds exhibited antiproliferative activity in the range of 33.98 n 10.51 μg/mL.

Acta Poloniae Pharmaceutica 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, Name: (E)-1-Cinnamylpiperazine.

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

Beiginejad, Hadi published the artcileDependence of mechanisms to thermodynamics in the electrochemical study of different electrophiles in the presence of some sulfur nucleophiles, COA of Formula: C12H16N2O2, the publication is Monatshefte fuer Chemie, database is CAplus.

Abstract: Electrochem. study of different electrophiles in the presence of p-toluenesulfinic acid and 2-mercaptobenzothiazole as sulfur nucleophiles was investigated. Mechanistic study of the electrochem. reactions indicates that the electrochem. oxidation of some species in the presence of the sulfur groups has different mechanisms, but some other species in the presence of both sulfur nucleophiles have the same mechanism. To explain the reason for this difference, the computational study was used. Thermodn. investigation shows that when ΔG_tot of the electrochem. oxidation of products are less than that of initial species, the electrochem. produced species can be oxidized during controlled-potential coulometry. The results of this work indicate that the computational study can be used to justify the reaction mechanisms. Cyclic voltammetry, linear sweep voltammetry, and controlled-potential coulometry were used to obtain the exptl. results. Also, by the use of BP86 level of theory and 6-31 + G(d,p) basis set, the theor. data were obtained.

Monatshefte fuer Chemie published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, COA of Formula: C12H16N2O2.

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

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

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

Fujimoto, Teppei published the artcilePhenoFluorMix: Practical Chemoselective Deoxyfluorination of Phenols, Synthetic Route of 67914-60-7, the publication is Organic Letters (2015), 17(3), 544-547, database is CAplus and MEDLINE.

A practical deoxyfluorination with novel deoxyfluorinating reagent PhenoFluorMix, a mixture of N,N’-1,3-bis(2,6-diisopropylphenyl)chloroimidazolium chloride and CsF, is presented. PhenoFluorMix overcomes the challenges associated with hydrolysis of PhenoFluor. PhenoFluorMix does not hydrolyze, is readily available on decagram scale, and is storable in air. In this paper, we demonstrate the practicality of the reagent and exhibit the deoxyfluorination of a variety of phenols and heterocycles.

Organic Letters published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Synthetic Route of 67914-60-7.

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