Month: April 2022

Quality Control of cis-Dichlorobis(pyridine)platinum(II). The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: cis-Dichlorobis(pyridine)platinum(II), is researched, Molecular C10H10Cl2N2Pt, CAS is 15227-42-6, about Antitumor activity of Group VIII transition metal complexes. I. Platinum(II) complexes. Author is Cleare, Michael J.; Hoeschele, James D..

A wide variety of Pt(II) complexes were studied for antitumor activity against Sarcoma 180 in female mice. In general only neutral complexes exhibited activity, whereas charged species were inactive and relatively nontoxic. A series of complexes of the type cis-[PtA2X2] (where A2 is either 2 monodentate or 1 bidentate amine ligand and X2 is either 2 monodentate or 1 bidentate anionic ligand) were studied with A and B being systematically varied. At least 10 potentially active antitumor drugs were identified, including cis-dichlorbis(methylamine)platinum(2+) [15273-32-2], diamminepropanedioatoplatinum(2+) [38780-43-7], and (1,2-ethanediammine-N,N’)(2-methylpropanedioato)platinum(2+) [41575-97-7]. The trans isomers were inactive in comparison with active cis complexes, so the presence of cis-reactive ligands seems to be a necessary parameter for antitumor activity. Complexes with highly reactive ligands such as cis-[Pt(NH3)2 (H2O)2](NO3)2 were highly toxic. Pd(II) complexes analogous to the active Pt(II) compounds were themselves inactive.

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Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 1-Bromoundecane, is researched, Molecular C11H23Br, CAS is 693-67-4, about Structure-inherent near-infrared bilayer nanovesicles for use as photoacoustic image-guided chemo-thermotherapy.Quality Control of 1-Bromoundecane.

Image-guided therapy, combined with imaging and therapeutic action, forms an attractive system because it can induce outstanding effects at focused locations. However, the conventional liposomes-based system cannot figure in therapeutic or imaging roles themselves, thereby causing the disadvantage of their biol. unavailability as a theragnosis tool. Herein, the structure-inherent near-IR bilayer nanovesicles are fabricated with amphiphilic heptamethine cyanine dye, PEG conjugated heptamethine cyanine dye, and gemcitabine (NEPCG) is developed for the novel photoacoustic image-guided chemo-thermotherapy system. The organic structure-inherent near-IR bilayer nanovesicles are self-assembled and exhibit a liposome-like bilayer structure. Furthermore, NEPCG showed the high photoacoustic signal (PA) due to the specific accumulation in the tumor site. Delivered NEPCG than displayed concurrent chemotherapy and photothermal therapy (PTT) effects against cancer, triggered by PA imaging with minimal side effects. In vitro and in vivo experiments show that NEPCG can be used as outstanding contrast agents and completely obliterate the tumor without reoccurrence under laser irradiation Therefore, this work presents the potential for the realization of unprecedented structure-inherent near-IR bilayer nanovesicles as highly accurate and effective theragnostic tools in clin. fields.

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Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: cis-Dichlorobis(pyridine)platinum(II)(SMILESS: [Cl-][Pt+2]([N]1=CC=CC=C1)([Cl-])[N]2=CC=CC=C2,cas:15227-42-6) is researched.Application of 693-67-4. The article 《Antitumor and antimitogenic properties of cis-dichloro(dipyridine)platinum(II)》 in relation to this compound, is published in Cancer Research. Let’s take a look at the latest research on this compound (cas:15227-42-6).

cis-Dichloro(dipyridine)platinum(II) (I) showed less potent antitumor and antimitogenic activity than previously studied cis-[Pt(NH3)2Cl2] (Rosenberg, B.; Van Camp, L., 1970). However in preliminary experiments, I was also less toxic to mice than the inorganic complex. I inhibited the growth of Escherichia coli. I increased the survival time of mice bearing Ehrlich ascites tumor; in vitro, I also inhibited protein and nucleic acid synthesis by tumors. I inhibited DNA synthesis in phytohemagglutinin-stimulated cultures of human lymphocytes.

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Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 1-Bromoundecane( cas:693-67-4 ) is researched.Application of 693-67-4.Anschuber, Martin; Pollice, Robert; Schnuerch, Michael published the article 《Rhodium-catalyzed direct alkylation of benzylic amines using alkyl bromides》 about this compound( cas:693-67-4 ) in Monatshefte fuer Chemie. Keywords: benzylmethylamino pyridine alkyl bromide rhodium catalyzed alkylation; Catalysis; C–H activation; C–H functionalization; Directing group. Let’s learn more about this compound (cas:693-67-4).

The development and substrate scope evaluation of a direct alkylation protocol of the C(sp3)-H bond of benzylic amines using alkyl bromides was reported. This pyridine-directed method was initiated by elimination of the alkyl bromide to a terminal olefin, which was then the true alkylating agent.

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Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Owen, W. John; Meyer, Kevin G.; Slanec, Thomas J.; Wang, Nick X.; Meyer, Stacy T.; Niyaz, Noormohamed M.; Rogers, Richard B.; Bravo-Altamirano, Karla; Herrick, Jessica L.; Yao, Chenglin published the article 《Synthesis and biological activity of analogs of the antifungal antibiotic UK-2A. I. Impact of picolinamide ring replacement》. Keywords: Leptosphaeria nodorum; Puccinia triticina; Qi-site; UK-2A; Zymoseptoria tritici; antifungal activity; cytochrome c reductase; picolinic acid SAR.They researched the compound: Picolinamide( cas:1452-77-3 ).Recommanded Product: 1452-77-3. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:1452-77-3) here.

BACKGROUND : The antifungal antibiotic UK-2A strongly inhibits mitochondrial electron transport at the Qi site of the cytochrome bc1 complex. Previous reports have described semi-synthetic modifications of UK-2A to explore the structure-activity relationship (SAR), but efforts to replace the picolinic acid moiety have been limited. RESULTS : Nineteen UK-2A analogs were prepared and evaluated for Qi site (cytochrome c reductase) inhibition and antifungal activity. While the majority are weaker Qi site inhibitors than UK-2A (IC50, 3.8 nM), compounds 2, 5, 13 and 16 are slightly more active (IC50, 3.3, 2.02, 2.89 and 1.55 nM, resp.). Compared to UK-2A, compounds 13 and 16 also inhibit growth of Zymoseptoria tritici and Leptosphaeria nodorum more strongly, while 2 and 13 provide stronger control of Z. tritici and Puccinia triticina in glasshouse tests. The relative activities of compounds 1-19 are rationalized based on a homol. model constructed for the Z. tritici Qi binding site. Phys. properties of compounds 1-19 influence translation of intrinsic activity to antifungal growth inhibition and in planta disease control. CONCLUSIONS : The 3-hydroxy-4-methoxy picolinic acid moiety of UK-2A can be replaced by a variety of o-hydroxy-substituted arylcarboxylic acids that retain strong activity against Z. tritici and other agriculturally relevant fungi. © 2018 Society of Chem. Industry

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Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 1-Bromoundecane( cas:693-67-4 ) is researched.Name: 1-Bromoundecane.Su, Yingyu; Chen, Guoshun; Cai, Yu; Gao, Bolan; Zhi, Xijun; Chang, Fengjiang published the article 《Effects of Broussonetia papyrifera-fermented feed on the growth performfermentedance and muscle quality of Hu sheep》 about this compound( cas:693-67-4 ) in Canadian Journal of Animal Science. Keywords: Broussonetia papyrifera fermentation feed muscle quality Hu sheep. Let’s learn more about this compound (cas:693-67-4).

This study aims to determine the effect of adding different proportions of Broussonetia papyrifera (BP)-fermented feed on Hu sheep. A total of 40 male Hu sheep (weighting 20.6 ± 2.20 kg) were collected and then divided into group I, II, III, and IV, with 0%, 5%, 10%, and 15% of BP-fermented feed to based diet, resp. After the trial period of 10 and 50 d, the sheep were slaughtered by conventional methods for the chem. analyses. It showed that adding 10% fermented feed could significantly increase the growth performance of the Hu sheep. Adding the fermented feed can improve the protein level, main flavor amino acid content, and fatty acid in the muscle. Based on the headspace solid-phase microextraction and gas chromatog. – mass spectrometry methods, a total of 125, 120, 119, and 117 kinds of volatile compounds were identified in group I, II, III, and IV, among which the relative content of the acid compound, ester compound, ketone compound, and aldehydes in group II, III, and IV were higher than that in control group, resp. Addition of BP-fermented feed could significantly improve growth performance and meat quality of Hu sheep.

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Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: Picolinamide, is researched, Molecular C6H6N2O, CAS is 1452-77-3, about Synthesis and biological activity of analogs of the antifungal antibiotic UK-2A. I. Impact of picolinamide ring replacement.Formula: C6H6N2O.

BACKGROUND : The antifungal antibiotic UK-2A strongly inhibits mitochondrial electron transport at the Qi site of the cytochrome bc1 complex. Previous reports have described semi-synthetic modifications of UK-2A to explore the structure-activity relationship (SAR), but efforts to replace the picolinic acid moiety have been limited. RESULTS : Nineteen UK-2A analogs were prepared and evaluated for Qi site (cytochrome c reductase) inhibition and antifungal activity. While the majority are weaker Qi site inhibitors than UK-2A (IC50, 3.8 nM), compounds 2, 5, 13 and 16 are slightly more active (IC50, 3.3, 2.02, 2.89 and 1.55 nM, resp.). Compared to UK-2A, compounds 13 and 16 also inhibit growth of Zymoseptoria tritici and Leptosphaeria nodorum more strongly, while 2 and 13 provide stronger control of Z. tritici and Puccinia triticina in glasshouse tests. The relative activities of compounds 1-19 are rationalized based on a homol. model constructed for the Z. tritici Qi binding site. Phys. properties of compounds 1-19 influence translation of intrinsic activity to antifungal growth inhibition and in planta disease control. CONCLUSIONS : The 3-hydroxy-4-methoxy picolinic acid moiety of UK-2A can be replaced by a variety of o-hydroxy-substituted arylcarboxylic acids that retain strong activity against Z. tritici and other agriculturally relevant fungi. © 2018 Society of Chem. Industry

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Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Quality Control of 1-Bromoundecane. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 1-Bromoundecane, is researched, Molecular C11H23Br, CAS is 693-67-4, about Viscosity of liquid bromoalkanes at ambient pressure from 253.15 to 423.15 K: New experimental data and their free volume theory-based interpretation. Author is Ryshkova, Olga S.; Belenkov, Roman N.; Postnikov, Eugene B..

This work reports new exptl. data for the viscosity of 1-bromopenthane (within the temperature range (253.15-298.15) K), 1-bromohexane ((263.15-293.15) K), 1-bromoheptane ((263.15-298.15) K), 1-bromooctane ((253.15-293.15) K), 1-bromononane ((253.15-413.15) K), 1-bromodecane ((253.15-423.15) K), 1-bromoundecane ((283.15-423.15) K), 1-bromododecane ((273.15-293.15) K), and 1-bromohexadecane ((298.15-423.15) K). Considering them in combination with previously known data for these substances, it is shown that the viscosity of this series of 1-bromoalkanes accurately satisfies the Bingham-Coombs model based on the free volume approach. The quant. connection of the excluded volume with the van der Waals volume and the packing fraction is revealed.

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Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Application of 693-67-4. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 1-Bromoundecane, is researched, Molecular C11H23Br, CAS is 693-67-4, about Effect of n-alkyl substitution on Cu(II)-selective chemosensing of rhodamine B derivatives.

Rhodamine B hydrazide-based mol. probes (1-10) were synthesized by derivatization with n-alkyl chains of different lengths at the hydrazide amino end. These probes exhibited selective absorption (A∼557) and fluorescence (I∼580) ‘off-on’ signal transduction along with a colorless → magenta color transition in the presence of Cu(II) ions among all the competitive metal ions investigated. The effective coordination of these probes to Cu(II) ions under the investigated environment forming [Cu·L]2+ (L = 1-5) and [Cu·L2]2+ (L = 6-10) complexes led to their spiro-ring opening, which in turn was expressed through signatory spectral peaks of ring-opened rhodamine. All these probes exhibited Cu(II) selectivity in signalling despite structural modifications to the core receptor unit through variation of the nature of the alkyl substituents. However, the sensitivity of the signalling and kinetics of the spiro-ring opening varied and could be correlated with the number of carbon atoms present in the n-alkyl substituents. Structural elucidation with X-ray diffraction and X-ray photoemission spectroscopic analyses provided further insight into the structure-function correlation in their Cu(II) complexes. These probes with Cu(II) coordination showed selectivity in signalling, high complexation affinity (log Ka = 4.8-8.8), high sensitivity (LOD = 4.1-80 nM), fast response time (rate = 0.0017-0.0159 s-1) and reversibility with counter anions, which ascertained their potential utility as chemosensors for Cu(II) ion detection.

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Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: Picolinamide( cas:1452-77-3 ) is researched.SDS of cas: 1452-77-3.Owen, W. John; Meyer, Kevin G.; Slanec, Thomas J.; Wang, Nick X.; Meyer, Stacy T.; Niyaz, Noormohamed M.; Rogers, Richard B.; Bravo-Altamirano, Karla; Herrick, Jessica L.; Yao, Chenglin published the article 《Synthesis and biological activity of analogs of the antifungal antibiotic UK-2A. I. Impact of picolinamide ring replacement》 about this compound( cas:1452-77-3 ) in Pest Management Science. Keywords: Leptosphaeria nodorum; Puccinia triticina; Qi-site; UK-2A; Zymoseptoria tritici; antifungal activity; cytochrome c reductase; picolinic acid SAR. Let’s learn more about this compound (cas:1452-77-3).

BACKGROUND : The antifungal antibiotic UK-2A strongly inhibits mitochondrial electron transport at the Qi site of the cytochrome bc1 complex. Previous reports have described semi-synthetic modifications of UK-2A to explore the structure-activity relationship (SAR), but efforts to replace the picolinic acid moiety have been limited. RESULTS : Nineteen UK-2A analogs were prepared and evaluated for Qi site (cytochrome c reductase) inhibition and antifungal activity. While the majority are weaker Qi site inhibitors than UK-2A (IC50, 3.8 nM), compounds 2, 5, 13 and 16 are slightly more active (IC50, 3.3, 2.02, 2.89 and 1.55 nM, resp.). Compared to UK-2A, compounds 13 and 16 also inhibit growth of Zymoseptoria tritici and Leptosphaeria nodorum more strongly, while 2 and 13 provide stronger control of Z. tritici and Puccinia triticina in glasshouse tests. The relative activities of compounds 1-19 are rationalized based on a homol. model constructed for the Z. tritici Qi binding site. Phys. properties of compounds 1-19 influence translation of intrinsic activity to antifungal growth inhibition and in planta disease control. CONCLUSIONS : The 3-hydroxy-4-methoxy picolinic acid moiety of UK-2A can be replaced by a variety of o-hydroxy-substituted arylcarboxylic acids that retain strong activity against Z. tritici and other agriculturally relevant fungi. © 2018 Society of Chem. Industry

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Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem