Category: 87179-40-6

Chan, Kin-Fai published the artcileEfficient Synthesis of Amine-Linked 2,4,6-Trisubstituted Pyrimidines as a New Class of Bacterial FtsZ Inhibitors, Quality Control of 87179-40-6, the publication is ACS Omega (2017), 2(10), 7281-7292, database is CAplus and MEDLINE.

We have recently identified a new class of FtsZ-interacting compounds that possess a 2,4,6-trisubstituted pyrimidine-quinuclidine scaffold with moderate antibacterial activity. Employing this scaffold as a mol. template, a compound library of amine-linked 2,4,6-trisubstituted pyrimidines with ninety-nine candidates was successfully established by employing an efficient convergent synthesis designed to explore its structure activity relationship. The results of min. inhibitory concentration (MIC) assay against S. aureus strains and cytotoxicity assay against mouse L929 cell line identified those compounds with potent anti-staphylococcal properties (MIC ranges from 3 to 8 μg/mL) and some extent of cytotoxicity against normal cell (IC₅₀ ranges from 6 to 27 μM). Importantly, three compounds also exhibited potent antibacterial activities against nine clin. isolated MRSA strains. One of the compounds, I, exhibited low spontaneous frequency of resistance, low toxicity against G. mellonella larvae as well as the ability to rescue G. mellonella larvae (20% survival rate at dosage of 100 mg/Kg) infected with LD of MRSA ATCC 43300 strain. Biol. characterization of compound I by saturation transfer difference NMR, light scattering assay and GTPase hydrolysis assay with purified S. aureus FtsZ protein verified that it interacted with the FtsZ protein. Such property of FtsZ inhibitor was further confirmed by observations of iconic filamentous cell phenotype and mislocalization of the Z-ring formation of B. subtilis. Taken together, these 2,4,6-trisubstituted pyrimidine derivatives represent a novel scaffold of S. aureus FtsZ inhibitors.

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 C13H18N2, Quality Control of 87179-40-6.

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

Srikanth Reddy, T. published the artcileSemi-synthesis and bio-evaluation of polybrominated diphenyl ethers from the sponge Dysidea herbacea, Recommanded Product: (E)-1-Cinnamylpiperazine, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(14), 4900-4906, database is CAplus and MEDLINE.

The sponge Dysidea herbacea was collected from the Mandapam Coast, Tamilnadu, India. Isolated gram quantities of hydroxylated polybrominated di-Ph ether (HO-PBDE) and semi-synthesized a series of new PBDEs derivatives and tested them for antibacterial and cytotoxic activities.

Bioorganic & Medicinal Chemistry 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 C22H21N3O3S, Recommanded Product: (E)-1-Cinnamylpiperazine.

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

Onida, Killian published the artcileDirect Synthesis of Carbamoyl Fluorides by CO₂ Deoxyfluorination, Category: piperazines, the publication is Angewandte Chemie, International Edition (2019), 58(36), 12545-12548, database is CAplus and MEDLINE.

Herein, a new concept for the direct synthesis of carbamoyl fluoride derivatives is disclosed. The developed method makes use of CO₂ as an inexpensive and abundant C₁ source; a variety of amines were successfully converted in the presence of a deoxyfluorinating reagent. The corresponding products were often obtained in excellent yields under mild reaction conditions (1 atm and room temperature). The reaction was easily scaled up, demonstrating the efficiency of the developed process.

Angewandte Chemie, International Edition 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

Laskowska, Anna K. published the artcileOpioid Tripeptides Hybridized with trans-1-Cinnamylpiperazine as Proliferation Inhibitors of Pancreatic Cancer Cells in Two- and Three-Dimensional in vitro Models, Application In Synthesis of 87179-40-6, the publication is ChemMedChem (2017), 12(19), 1637-1644, database is CAplus and MEDLINE.

According to the World Health Organization, the mortality rate among patients with pancreatic cancer will increase in the upcoming years. Gemcitabine is the first choice for treatment of pancreatic malignancy, but increasing resistance to this drug is decreasing its overall efficacy. Studies on new therapies that target metabolic pathways, growth factor inhibitors, and tumor stroma or tumor stem cells are currently underway in many research groups. Herein the authors report the bioactive properties (cytotoxicity and hemolytic activity) of synthetic peptidomimetics containing an opioid tripeptide fragment (Tyr-R¹-R²-; where R¹ is D-Ala or D-Thr, and R² is Phe or Trp) hybridized with trans-1-cinnamylpiperazine. These compounds are stable in plasma up to 96 h and exhibit low hemotoxicity and good inhibitory effects on cancer cell growth in two- and three-dimensional in vitro models of pancreatic cancer.

ChemMedChem 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

Venkatachalam, T. K. published the artcileSynthesis and characterization of oxazolopyridine and benzoxazole derivatives, Formula: C13H18N2, the publication is Letters in Organic Chemistry (2010), 7(7), 519-527, database is CAplus.

Synthesis of piperazinyl-substituted oxazolopyridine and benzoxazole was achieved in three steps starting from aminophenols and carbon disulfide. Condensation of aminophenols with carbon disulfide in ethanol using potassium hydroxide as catalyst gave the required benzoxazolethiols in one step. Treatment of the thiols with piperazine and substituted piperazine derivatives in toluene furnished the title compounds in good yields. We introduced halogen substitution in the pendant arm of the piperazine derivatives for versatile functionalization. We report the synthesis and characterization of these compounds using high resolution NMR techniques.

Letters in 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 C10H14BNO5S, Formula: C13H18N2.

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

Aguilera, Elena published the artcileA nature-inspired design yields a new class of steroids against trypanosomatids, Application In Synthesis of 87179-40-6, the publication is Molecules (2019), 24(20), 3800, database is CAplus and MEDLINE.

Chagas disease and Leishmaniasis are neglected endemic protozoan diseases recognized as public health problems by the World Health Organization. These diseases affect millions of people around the world however, efficient and low-cost treatments are not available. Different steroid mols. with antimicrobial and antiparasitic activity were isolated from diverse organisms (ticks, plants, fungi). These mols. have complex structures that make de novo synthesis extremely difficult. In this work, we designed new and simpler compounds with antiparasitic potential inspired in natural steroids and synthesized a series of nineteen steroidal arylideneketones and thiazolidenehydrazines. We explored their biol. activity against Leishmania infantum, Leishmania amazonensis, and Trypanosoma cruzi in vitro and in vivo. We also assayed their genotoxicity and acute toxicity in vitro and in mice. The best compound, a steroidal thiosemicarbazone compound 8 (ID_1260) was active in vitro (IC₅₀ 200 nM) and in vivo (60% infection reduction at 50 mg/kg) in Leishmania and T. cruzi. It also has low toxicity in vitro and in vivo (LD₅₀ >2000 mg/kg) and no genotoxic effects, being a promising compound for anti-trypanosomatid drug development.

Molecules 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

Byrtus, Hanna published the artcileSynthesis and anticonvulsant activity of new N-Mannich bases derived from 5-cyclopropyl-5-phenyl- and 5-cyclopropyl-5-(4-chlorophenyl)-imidazolidine-2,4-diones, Related Products of piperazines, the publication is Bioorganic & Medicinal Chemistry (2011), 19(20), 6149-6156, database is CAplus and MEDLINE.

Synthesis, physicochem. and anticonvulsant properties of new N-Mannich bases derived from 5-cyclopropyl-5-phenyl- and 5-cyclopropyl-5-(4-chlorophenyl)-imidazolidine-2,4-diones have been described. Initial anticonvulsant screening was performed using i.p. maximal electroshock (MES) and s.c. pentylenetetrazole (scPTZ) seizure tests. The neurotoxicity was determined applying the rotarod test. The in vivo results in mice showed that all compounds were effective especially in the MES screen. The quant. evaluation after oral administration in rats showed that the most active was 5-cyclopropyl-5-phenyl-imidazolidine-2,4-dione (I) with ED₅₀ values of 5.76 mg/kg (MES) and 57.31 mg/kg (scPTZ). This mol. was more potent than phenytoin and ethosuximide which were used as reference antiepileptic drugs. Addnl. compound I with ED₅₀ of 26.06 mg/kg in psychomotor seizure test (6-Hz) in mice showed comparable activity to new generation anticonvulsant – levetiracetam.

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 C13H18N2, Related Products of piperazines.

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

Mazzei, Mauro published the artcileActivity of Mannich bases of 7-hydroxycoumarin against Flaviviridae, Quality Control of 87179-40-6, the publication is Bioorganic & Medicinal Chemistry (2008), 16(5), 2591-2605, database is CAplus and MEDLINE.

Some Mannich bases of 7-hydroxycoumarin (2) and their simple derivatives (3 and 4) were prepared and tested against viruses containing single-stranded, pos.-sense RNA genomes (ssRNA⁺). This study was directed toward Flaviviridae and, in particular, HCV surrogate viruses (BVDV, YFV). The 7-hydroxy derivatives 2 were generally devoid of activity, but when position 7 was propylated, the resulting 7-propyloxy derivatives 3 were in some cases endowed with an interesting activity against BVDV. The formation of 7-benzoyl derivatives 4 gave compounds generally lacking in activity against Flaviviridae, whereas the appearance of activity against RSV has been observed Also some unsym. methylene derivatives 5-7 (namely coumarins bridged to chromones or indoles) were found moderately active in antiviral tests. Derivatives 3 were submitted to a mol. modeling study using DNA polymerase of HCV as a target. The good correlation between calculated mol. modeling IC₅₀ and exptl. EC₅₀ indicates that DNA polymerase is potentially involved in the inhibition of surrogate HCV viruses.

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 C13H18N2, Quality Control of 87179-40-6.

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

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