Heterocyclic Building Blocks-Thiazolidine

Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 1273-73-0, is researched, SMILESS is Br[C-]12[Fe+2]3456789([C-]%10C6=C7C8=C9%10)C1=C3C4=C25, Molecular C10BrFeJournal, Journal of Organometallic Chemistry called Synthesis, X-ray structure and chemical properties of 17α-ferrocenylestradiol, Author is Vichard, Dominique; Gruselle, Michel; Jaouen, Gerard; Nefedova, Marina N.; Mamedyarova, Irina A.; Sokolov, Viatcheslav I.; Vaissermann, Jacqueline, the main research direction is ferrocenylestradiol crystal structure reaction; estradiol ferrocenyl crystal structure reaction.Name: Bromoferrocene.

The X-ray structure of 17α-ferrocenylestradiol shows that the ferrocenyl group is at the α-position of the steroid, below the plane of the D ring. From acidic medium it is possible to obtain and isolate the derivative with a carbenium ion in 17-α position. This ion is transformed by various nucleophiles into the C(16)-C(17)-unsaturated derivative With NaBH4 in acidic medium the reduction leads to a mixture of 17α- and 17β-ferrocenylestrol with a predominance of the β product, owing to a more favorable entrance of hydride in the α position. The oxidized derivative 17α-ferrociniumylestradiol tetrafluoroborate was prepared and its properties are described.

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Electric Literature of C9H13NO2. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: Ethyl 3,5-Dimethyl-2-pyrrolecarboxylate, is researched, Molecular C9H13NO2, CAS is 2199-44-2, about 5-Unsubstituted 2-pyrrolecarboxaldehydes for porphyrin synthesis and the cyanovinyl protecting group. Author is Paine, John B. III; Dolphin, David.

(Cyanovinyl)pyrroles I (R = Me, R1 = Et, octyl; R = Et, R1 = Me) derived from the Knoevenagel condensation of benzyl 5-formyl-2-pyrrolecarboxylates with NCCH2CO2Me were employed in a facile sequence of 4 steps to produce, regioselectively, 2-pyrrolecarboxaldehydes II, important intermediates for porphyrin synthesis. Each step proceeded in 90-95% yield, making II available smoothly from benzyl 5-methyl-2-pyrrolecarboxylates in 7 steps, with an overall yield of 66-72%.

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The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: Bromoferrocene(SMILESS: Br[C-]12[Fe+2]3456789([C-]%10C6=C7C8=C9%10)C1=C3C4=C25,cas:1273-73-0) is researched.SDS of cas: 38006-08-5. The article 《Electron-transfer properties of a nonheme manganese(IV)-oxo complex acting as a stronger one-electron oxidant than the iron(IV)-oxo analogue》 in relation to this compound, is published in Chemical Communications (Cambridge, United Kingdom). Let’s take a look at the latest research on this compound (cas:1273-73-0).

Electron-transfer properties of a nonheme Mn(iv)-oxo complex, [(Bn-TPEN)MnIV(O)]2+, reveals that Mn(iv)-oxo complex acts as a stronger 1-electron oxidant than the Fe(iv)-oxo analog. As a result, an electron transfer process in N-dealkylation was detected by a transient radical cation intermediate, para-Me-DMA√+, in the oxidation of para-Me-DMA by [(Bn-TPEN)MnIV(O)]2+.

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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 83237-15-4, Name is 3-(3,5-Di-tert-butyl-1-hydroxy-4-oxocyclohexa-2,5-dien-1-yl)propanoic acid, molecular formula is C17H26O4. In an article, author is de Oliveira Filho, Gevanio Bezerra,once mentioned of 83237-15-4, COA of Formula: C17H26O4.

Chagas disease is one of the most significant health problems in the American continent. benznidazole (BDZ) and nifurtimox (NFX) are the only drugs approved for treatment and exhibit strong side effects and ineffectiveness in the chronic stage, besides different susceptibility among T. cruzi DTUs (Discrete Typing Units). Therefore, new drugs to treat this disease are necessary. Thiazole compounds have been described as potent trypanocidal agents. Here we report the structural planning, synthesis and anti-T cruzi evaluation of a new series of 1,3-thiazoles (7-28), which were designed by placing this heterocycle instead of thiazolidin-4-one ring. The synthesis was conducted in an ultrasonic bath with 2-propanol as solvent at room temperature. By varying substituents attached to the phenyl and thiazole rings, substituents were observed to retain, enhance or greatly increase their anti-T. cruzi activity. In some cases, methyl at position 5 of the thiazole (compounds 9, 12 and 23) increased trypanocidal property. The exchange of phenyl for pyridinyl heterocycle resulted in increased activity, giving rise to the most potent compound against the trypomasigote form (14, IC50trypo = 0.37 mu M). Importantly, these new thiazoles were toxic for trypomastigotes without affecting macrophages and cardiomyoblast viability. The compounds were also evaluated against cruzain, and five of the most active compounds against trypomastigotes (7, 9, 12, 16 and 23) inhibited more than 70% of enzymatic activity at 10 mu M, among which compound 7 had an IC50 in the submicromolar range, suggesting a possible mechanism of action. In addition, examination of T. cruzi cell death showed that compound 14 induces apoptosis. We also examined the activity against intracellular parasites, revealing that compound 14 inhibited T cruzi infection with potency similar to benznidazole. The antiparasitic effect of 14 and benznidazole in combination was also investigated against trypomastigotes and revealed that they have synergistic effects, showing a promising profile for drug combination. Finally, in mice acutely-infected with T cruzi, 14 treatment significanty reduced the blood parasitaemia and had a protective effect on mortality. In conclusion, we report the identification of compounds (7), (12), (15), (23) and (26) with similar trypanocidal activity of benznidazole; compounds (9) and (21) as trypanocidal agents equipotent with BDZ, and compound 14 with potency 28 times better than the reference drug without affecting macrophages and cardiomyoblast viability. Mechanistically, the compounds inhibit cruzain, and 14 induces T. cruzi cell death by an apoptotic process, being considered a good starting point for the development of new anti-Chagas drug candidates. (C) 2017 Elsevier Masson SAS. All rights reserved.

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Application of 85-42-7, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 85-42-7, Name is Hexahydroisobenzofuran-1,3-dione, SMILES is O=C1OC(C2CCCCC21)=O, belongs to thiazolidine compound. In a article, author is Mirakmahaleh, Maedeh Saeedi, introduce new discover of the category.

A library of pyran-2H-one-3-ylmethylidene and chromene-2H-one-3-ylmethylidene derivatives of the titled heterocyclic framework was synthesized from 3-acyl-4-hydroxypyran/chromene-2H-one via sequential reaction with thiosemicarbazide and dialkyl acetylenedicarboxylates. The syntheses were carried out under efficient catalysis of a new binary ionic liquid mixture [l-prolinium chloride][1-methylimidazolium-3-sulfonate] in one pot and solvent-free conditions. Calculations based on density functional theory displayed that the barrier energy for interconversion of the two possible diastereomeric isomers of each product is less than the thermal energy of molecules at room temperature, as only one product can be resolved from a given reaction mixture. This seems to be the case for the previously reported hydrazonothiazolidines. The binary ionic liquid mixture melts at near room temperature and can be considered as a solution of HCl in 1:1 mixture of two zwitterionic species. It proved to be more efficient than its constituents in catalyzing the above synthesis in one-pot operation. Some of the synthesized products have shown pronounced antibacterial activities. The ionic liquid is virtually stable in air and moisture, as can be retrieved several times without appreciable decrease in its catalytic activity. Graphic abstract

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Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 593-85-1, Name is guanidinecarbonate, molecular formula is C3H12N6O3. In an article, author is Brahmbhatt, Harshad,once mentioned of 593-85-1, COA of Formula: C3H12N6O3.

Background: Rhodanine is known for its potential and important role in the medicinal chemistry since its derivatives exhibit a wide range of pharmacological activities such as antibacterial, antifungal, antidiabetic, antitubercular, anti-HIV, antiparasitic, antioxidant, anticancer, antiproliferative and anthelmintic agents. Objectives: Since N-substituted rhodanine synthons are rarely commercially available, it is desirable to develop a straightforward synthetic approach for the synthesis of these key building blocks. The objective was to synthesize a series of rhodanine derivatives and to investigate their antimicrobial and antioxidant activity. Also, in order to obtain an insight into their structure-activity relationship, QSAR studies on the antioxidant activity were performed. Methods: H-1 and C-13 FTNMR spectra were recorded on Bruker Avance 600 MHz NMR Spectrometer, mass analysis was carried out on ESI+ mode by LC-MS/MS API 2000. 2,2-Diphenyl-1-picrylhydrazyl radical scavenging activity (% DPPH) was determined in dimethylsulfoxide (DMSO) as a solvent. The antibacterial activity was assessed against Bacillus subtilis, Staphylococcus aureus (Gram positive) and Escherichia coli, Pseudomonas aeruginosa (Gram negative) bacteria in terms of the minimum inhibitory concentrations (MICs) by a modified broth microdilution method. Results: A series of N-substituted-2-sulfanylidene-1,3-thiazolidin-4-ones were synthesized and characterized by H-1 NMR, C-13 NMR, FTIR, GC MS, LCMS/ MS and C,H,N,S elemental analysis. Most of the synthesized compounds showed moderate to excellent antibacterial activity (MIC values from 125 mu g/ml to 15.62 mu g/mL) and DPPH scavenging activity (from 3.60% to 94.40%). Compound 2-thioxo-3-(4-(trifluoromethyl)-phenyl)thiazolidin-4-one showed the most potent activity against Escherichia coli (3.125 mu g/mL), equivalent to antibiotic Amikacin sulphate and against Staphylococcus aureus (0.097 mu g/ml), 100 times superior then antibiotic Amikacin sulphate. It has also shown a potent antioxidant activity (95% DPPH scavenging). Two best QSAR models, obtained by GETAWAY descriptor R7p(+), Balabans molecular connectivity topological index and Narumi harmonic topological index (HNar), suggest that the enhanced antioxidant activity is related to the presence of pairs of atoms higher polarizability at the topological distance 7, substituted benzene ring and longer saturated aliphatic chain in N-substituents. Conclusion: A series of novel N-substituted-2-thioxothiazolidin-4-one derivatives were designed, synthesized, characterized and evaluated for their antibacterial and antioxidant activity in vitro. Majority of the compounds showed excellent antibacterial activity compared to ampicillin and few of them have an excellent activity as compared to Chloramphenicol standard antibacterial drug. The QSAR study has clarified the importance of presenting a pairs of atoms higher polarizability, such as Cl and S at the specific distance, as well as the substituted benzene ring and a long saturated aliphatic chain in N-substituents for the enhanced antioxidant activity of 2-sulfanylidene-1,3thiazolidin-4-one derivatives.

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Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. 2421-28-5, Name is Benzophenone-3,3′,4,4′-tetracarboxylic dianhydride, molecular formula is C17H6O7, belongs to thiazolidine compound, is a common compound. In a patnet, author is Ying, Jun, once mentioned the new application about 2421-28-5, Application In Synthesis of Benzophenone-3,3′,4,4′-tetracarboxylic dianhydride.

A tBuOK-mediated carbonylative cyclization of propargylic amines with elemental sulfur has been developed. With benzene-1,3,5-triyl triformate (TFBen) as a convenient CO surrogate, various substituted 1,3-thiazolidin-2-ones were produced in good to excellent yields.

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Electric Literature of 6117-80-2, Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. 6117-80-2, Name is (Z)-But-2-ene-1,4-diol, SMILES is OC/C=CCO, belongs to thiazolidine compound. In a article, author is Lu, Min, introduce new discover of the category.

The present study enumerates the discovery and development of novel thiazolidin-4-one-1,3,5-triazine as neuro-protective agent against cerebral ischemia-reperfusion injury in mice. These compounds showed significant inhibition of NF-kappa B transcriptional activity in LPS-stimulated RAW264.7 cells, displaying compound8kas most potent inhibitor among the tested derivative. The compound 8k was further studied in in vivo middle cerebral artery occlusion (MCAO) mice model for neuro-protective action. Results suggest that compound8kcauses attenuation of inflammation (TNF-alpha, IL-beta, and IL-6), oxidative stress (SOD, GSH, and MDA), and apoptosis (Bcl-2, Bax, and cleaved caspase-3) in MCAO mice in concentration-dependent manner. Collectively, our results documented that compound8kpre-treatment protects cerebral I/R. This novel lead scaffold may be helpful for investigation of new neuro-protective agent by inactivation of NF-kappa B.

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Reference of 6117-80-2, Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. 6117-80-2, Name is (Z)-But-2-ene-1,4-diol, SMILES is OC/C=CCO, belongs to thiazolidines compound. In a article, author is Lu, Min, introduce new discover of the category.

The present study enumerates the discovery and development of novel thiazolidin-4-one-1,3,5-triazine as neuro-protective agent against cerebral ischemia-reperfusion injury in mice. These compounds showed significant inhibition of NF-kappa B transcriptional activity in LPS-stimulated RAW264.7 cells, displaying compound8kas most potent inhibitor among the tested derivative. The compound 8k was further studied in in vivo middle cerebral artery occlusion (MCAO) mice model for neuro-protective action. Results suggest that compound8kcauses attenuation of inflammation (TNF-alpha, IL-beta, and IL-6), oxidative stress (SOD, GSH, and MDA), and apoptosis (Bcl-2, Bax, and cleaved caspase-3) in MCAO mice in concentration-dependent manner. Collectively, our results documented that compound8kpre-treatment protects cerebral I/R. This novel lead scaffold may be helpful for investigation of new neuro-protective agent by inactivation of NF-kappa B.

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An article NaOH-Promoted Chemoselective Cascade Cyclization of Cyclopropyl Esters with Unsaturated lmines: Access to Bioactive Cyclopenta[c]pyridine Derivatives WOS:000485089300009 published article about ANTIBACTERIAL ACTIVITY; ORGANOCATALYTIC ACTIVATION; BLIGHT in [Pan, Dingwu; Zan, Ningning; Lv, Ya; Song, Bao-An; Chi, Yonggui Robin; Jin, Zhichao] Guizhou Univ, Lab Breeding Base Green Pesticide & Agr Bioengn, Key Lab Green Pesticide & Agr Bioengn, Guiyang 550025, Guizhou, Peoples R China; [Mou, Chengli] Guizhou Univ Tradit Chinese Med, Guiyang 550025, Guizhou, Peoples R China; [Chi, Yonggui Robin] Nanyang Technol Univ, Sch Phys & Math Sci, Div Chem & Biol Chem, Singapore 637371, Singapore in 2019.0, Cited 42.0. The Name is Chalcone. Through research, I have a further understanding and discovery of 94-41-7. Product Details of 94-41-7

A chemoselective cascade cycloaddition reaction is developed for green and efficient access to cyclopenta-[c]pyridine derivatives. Simple and inexpensive NaOH is used as the sole catalyst for this process. The delta-carbon of cyclopropyl ester is activated as a nucleophiic carbon to initiate highly chemoselective cascade reactions. Cyclopenta-[c]pyridines bearing various substituents are afforded in excellent yields. Preliminary studies on the bioactivities of the afforded products show promising antibacterial activities for potential applications in plant protections.

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