- Enantiomeric substituents determine the chirality of luminescent conjugated polythiophenes
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Chiral isomers of 3-substituted polythiophenes with amino acid functiontionalized side chains are compared. The polymers show pH-dependent absorption, emission, and circular dichroism spectra in buffered aqueous solution. At pH equal to pi of the amino ac
- Nilsson, K. Peter R.,Olsson, Johan D. M.,Konradsson, Peter,Inganaes, Olle
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- Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors
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Selective inhibition of KDAC isoforms while maintaining potency remains a challenge. Using the largazole macrocyclic depsipeptide structure as a starting point for developing new KDACIs with increased selectivity, a combination of four different simplified largazole analogue (SLA) scaffolds with diverse zinc-binding groups (for a total of 60 compounds) were designed, synthesized, and evaluated against class I KDACs 1, 3, and 8, and class II KDAC6. Experimental evidence as well as molecular docking poses converged to establish the cyclic tetrapeptides (CTPs) as the primary determinant of both potency and selectivity by influencing the correct alignment of the zinc-binding group in the KDAC active site, providing a further basis for developing new KDACIs of higher isoform selectivity and potency.
- Reddy, Damodara N.,Ballante, Flavio,Chuang, Timothy,Pirolli, Adele,Marrocco, Biagina,Marshall, Garland R.
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supporting information
p. 1613 - 1633
(2016/03/05)
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- ISOFORM-SELECTIVE LYSINE DEACETYLASE INHIBITORS
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Isoform-selective lysine deacetylase inhibitors are described. Inhibitors of the lysine deacetylase enzyme are useful as antitumor drugs and for treating addiction, asthma, cardio-vascular disease, immunosuppression, neurodegenerative diseases, sepsis, sickle-cell disease, uveal melanoma and termination of viral latency, particularly HIV-1 latency.
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Paragraph 0141-0143
(2016/11/21)
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- Thiophene derivatives, water soluble conductive polymer and an aqueous solution thereof, and manufacturing method thereof
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PROBLEM TO BE SOLVED: To provide a novel water-soluble thiophene derivative used as a conductive material, and novel water-soluble polythiophenes used as conductive materials.SOLUTION: The thiophene derivative is represented by formula (1) or an ammonium
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Paragraph 0137
(2017/04/27)
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- Modular Access to Substituted Azocanes via a Rhodium-Catalyzed Cycloaddition-Fragmentation Strategy
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A short entry to substituted azocanes by a Rh-catalyzed cycloaddition-fragmentation process is described. Specifically, exposure of diverse N-cyclopropylacrylamides to phosphine-ligated cationic Rh(I) catalyst systems under a CO atmosphere enables the directed generation of rhodacyclopentanone intermediates. Subsequent insertion of the alkene component is followed by fragmentation to give the heterocyclic target. Stereochemical studies show, for the first time, that alkene insertion into rhodacyclopentanones can be reversible.
- Shaw, Megan H.,Croft, Rosemary A.,Whittingham, William G.,Bower, John F.
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supporting information
p. 8054 - 8057
(2015/07/15)
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- New and efficient synthetic approaches for the regioisomeric and iminium impurities of clopidogrel bisulfate
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New and concise synthetic routes have been devised for the regioisomeric and iminium impurities of clopidogrel bisulfate. The synthesis features utilization of commercially available starting materials and simple reactions.
- Aalla, Sampath,Gilla, Goverdhan,Anumula, Raghupathi Reddy,Charagondla, Kavitha,Vummenthala, Prabhakar Reddy,Padi, Pratap Reddy
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p. 1523 - 1526
(2013/02/23)
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- Synthesis of two novel cysteine-functionalized thiophenes
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The synthetic approach to methyl N-(tert-butoxycarbonyl)-S-(3-thienyl)-L- cysteinate (1) and methyl N-(tert-butoxycarbonyl)-S-[2-(3-thienyl)ethyl]-L- cysteinate (2) through tosylate intermediates is reported and discussed. These compounds, which combine the properties of the cysteine side-chain with those of the thiophene ring represent both potential bioactive molecules and interesting synthons for the development of new materials.
- Cagnoli, Rita,Lanzi, Massimiliano,Mucci, Adele,Parenti, Francesca,Schenetti, Luisa
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p. 267 - 271
(2007/10/03)
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- Triflic anhydride-promoted cyclization of sulfides: A convenient synthesis of fused sulfur heterocycles
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A new approach to the synthesis of annulated sulfur heterocycles based on triflic anhydride-promoted cyclization of the hetaryl(aryl) containing alkyl sulfides was elaborated. Smooth demethylation of initially formed cyclic sulfonium salts by treatment with triethylamine afforded a number of five-, six- and seven-membered fused sulfur heterocycles. Unexpected ring opening took place in the reaction of diethylamine with 5-membered sulfonium salts.
- Shevchenko, Nikolay E.,Nenajdenko, Valentine G.,Balenkova, Elizabeth S.
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p. 1191 - 1200
(2007/10/03)
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- New 1-(heterocyclylalkyl)-4-(propionanilido)-4-piperidinyl methyl ester and methylene methyl ether analgesics
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A series of new 1-(heterocyclyalkyl)-4-(propionanilido)-4-piperidinyl methyl esters and methylene methyl ethers have been synthesized and pharmacologically evaluated. In the mouse hot-plate test, the majority of compounds exhibited an analgesia (ED50 1 mg/kg) superior to that of morphine. These studies revealed a pharmacological accommodation for many more structurally diverse and far bulkier aromatic ring systems than the corresponding components of the arylethyl groups of the prototypic methyl ester (carfentanil, 2) and methylene methyl ether (sufentanil, 3 and alfentanil, 4) 4-propionanilido analgesics. Compound 9A (methyl 1-[2-(1H-pyrazol-1-yl)-ethyl]-4-[(1-oxopropyl) phenylamino]-4-piperidinecarboxylate), which exhibited appreciable μ-opioid receptor affinity, was a more potent and short-acting analgesic, than alfentanil with less respiratory depression in the rat. On the other hand, the phthalimides 57A and 57B, which exhibited negligible affinity for opioid receptors associated with the mediation of nociceptive transmission (i.e., μ-, κ-, and δ-subtypes), displayed analgesic efficacy in all antinociception tests. In addition, while 57B, compared to clinical opioids, showed a superior recovery of motor coordination after regaining of righting reflex from full anesthetic doses in the rat rotorod test, 57A showed significantly less depression of cardiovascular function at supraanalgesic doses in the isoflurane-anesthetized rat.
- Bagley,Thomas,Rudo,Spencer,Doorley,Ossipov,Jerussi,Benvenga,Spaulding
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p. 827 - 841
(2007/10/02)
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- Lewis-acid Promoted Aromatic Cyclization of &α-Chlorosulfides: Synthesis of Ethyl Isothiochroman-1-carboxylate and Related Compounds
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A variety of ethyl isothiochroman-1-carboxylates and related compounds were synthesized by treatment of 2-chloro-2-acetates with stannic chloride in methylene chloride.The same procedure was applied to the synthesis of ethyl 4-chloro-4-methyltetrahydrothiopyran-2-carboxylate.Some isothiochroman-1-carboxylic acids were prepared and evaluated for antiinflammatory activity.Among the compounds tested, 7-phenoxyisothiochroman-1-carboxylic acid showed weak activity.
- Ishibashi, Hiroyuki,Okada, Motofumi,Iida, Kyoko,Ikeda, Masazumi
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p. 1527 - 1529
(2007/10/02)
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