- β-Strand Mimicry: Exploring Oligothienylpyridine Foldamers
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Protein–protein interactions (PPIs) are involved in many cellular processes; consequently, the discovery of small molecules as modulators of PPIs has become an important challenge in medicinal chemistry. Structural mimetics of α-helices, β-turns or β-strands could maintain or restore biological functions and should possess biological activity. At this time, the most challenging classes of PPIs are those mediated by β-sheet interactions, which are implicated in a number of diseases. Only a few β-strand mimics have been published to date. This study presents an evaluation of oligothienylpyridyl scaffolds in view of their ability for β-strand mimicry. In this study, theoretical ring twist angle predictions for these scaffolds have been validated by X-ray diffraction and molecular dynamics simulations with NMR constraints. Careful choice of substituent and heavy-atom positions in the foldamer units opens the way to produce reasonably coplanar compounds mimicking β-strand side-chain distribution.
- Jouanne, Marie,Voisin-Chiret, Anne Sophie,Legay, Rémi,Coufourier, Sébastien,Rault, Sylvain,Sopkova-de Oliveira Santos, Jana
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Read Online
- COMPOUND ACTING AS ANTIBIOTICS
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The present invention provides a novel antibiotic compound represented by the following formula (I), a pharmaceutically acceptable salt thereof, an ester thereof, a prodrug thereof, a solvate thereof, or a deuterated analog thereof, or a stereoisomer thereof. The compound of the present invention exhibits excellent antibacterial activity, especially against Gram bacteria. wherein each group is defined as in the description.
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Paragraph 0431-0433
(2020/12/22)
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- Regioselective oxidative Pd-catalysed coupling of alkylboronic acids with pyridin-2-yl-substituted heterocycles
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A total of 19 alkylated heterocycles (thiophenes, benzothiophenes, pyrroles, furans) were prepared (36-99% yield) from the respective pyridin-2-yl-substituted precursors employing alkylboronic acids as the C-H alkylating reagents in an oxidative (Ag2
- Wippich, Julian,Schnapperelle, Ingo,Bach, Thorsten
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supporting information
p. 3166 - 3168
(2015/06/11)
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- 6-11 Bicyclic ketolide derivatives
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The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
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- 6-11 bicyclic ketolide derivatives
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The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
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- 6-11 BICYCLIC KETOLIDE DERIVATIVES
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The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: (I) which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the afor
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Page/Page column 121-122
(2010/02/12)
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- 6-11 BICYCLIC KETOLIDE DRIVATIVES
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The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: Formule (I) which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising
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Page/Page column 127-128
(2010/02/12)
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- 6-11 Bicyclic ketolide derivatives
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The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
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- 6-11 BICYCLIC KETOLIDE DERIVATIVES
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The present invention discloses compounds of formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforem
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Page/Page column 128
(2010/02/07)
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- Process for the preparation of 6-O-propargyl erythromycin derivatives
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Disclosed herein is a process for the preparation of erythromycin derivatives, or pharmaceutically acceptable salts thereof, which contain an optionally substituted propargyl group at the 6-O-position.
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- Coupling of Organotin Reagents with Aryl, Acyl and Heteroaryl Halides Part Two: Synthesis of Thienylpyridine Derivatives
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Coupling of organotin reagent Bu3SnAr (Ar = 2- or 3-pyridyl, or 2- or 3-thienyl) with appropriately halogenated heterocyclic in the presence of PdCl(CH2Ph)(PPh3)2 leads to the corresponding thienylpyridine derivative.Functionality is tolerated on the thiophene centre, but not in the case of the corresponding pyridine analogue.The compounds Bu3SnAr were prepared by a variety of methods, giving good yield of the tri-n-butylstannylated heterocycle.Other derivatives are prepared by direct reaction with the thienylpyridine nucleus.Examples of homo-coupling of the both organotin compounds and the aryl halide are also reported.
- Sosabowski, Michael H.,Powell, Paul
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p. 201 - 219
(2007/10/03)
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- Pyridine-Substituted Hydroxythiophenes. V. Preparation of 5-(2-, 3- and 4-pyridyl)-2-hydroxythiophenes
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5-(2-, 3- and 4-Pyridyl)-2-t-butoxythiophenes have been prepared in very good yields by Pd(O) catalyzed cross-coupling of the three isomeric bromopyridines with 5-trimethylstannyl-2-t-butoxythiophene derived from 2-bromothiophene via 2-t-butoxythiophene.Dealkylation of 5-(2-, 3- and 4-pyridyl)-2-t-butoxythiophenes with boron trifluoride etherate in dichloromethane at room temperature led to predominant formation of rearranged products, 5-(2- and 3-pyridyl)-3-t-butyl-3-thiolene-2-ones, together with a small amount of 5-(2- and 3-pyridyl)-2-hydroxythiophenes as a mixture of two tautomeric keto forms in the case of the 2-pyridyl and the 3-pyridyl isomers, and exclusive formation of rearranged product in the case of the 4-pyridyl isomer.However, dealkylation of 2-methoxy-5-(2-, 3- and 4-pyridyl)thiophenes, prepared similarly to the 5-(2-, 3- and 4-pyridyl)-2-t-butoxythiophenes, with boron tribromide under the same reaction conditions as above resulted exclusively in the tautomeric mixture of 5-(2- and 3-pyridyl)-3-thiolene-2-ones and 5-(2- and 3-pyridyl)-4-thiolene-2-ones in the case of the 2-pyridyl and 3-pyridyl isomers.In case of the 4-pyridyl isomer polymerization took place.
- Zhang, Yihua,Hoernfeldt, Anna-Britta,Gronowitz, Salo
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p. 771 - 778
(2007/10/03)
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- A CONVENIENT SYNTHESIS OF FIVE-MEMBERED HETEROARYL -SUBSTITUTED PYRIDINES
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Five-membered heteroarylpyridines (3) or (4) such as furylpyridines, thienylpyridines, imidazolylpyridines and pyrrolylpyridines were obtained regioselectively in appreciable yields (40-67percent) by reaction of heteroaryllithium salts with N-ethoxycarbonylpyridinium chloride (1) followed by oxygen oxidation.
- Shiao, Min- Jen,Shih, Li- Hua,Chia, Win- Long,Chau, Tay- Yuan
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p. 2111 - 2118
(2007/10/02)
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- Thienotriazolodiazepines as platelet-activating factor antagonists. Steric limitations for the substituent in position 2
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The preparations of thienotriazolodiazepines bearing a substituted ethynyl group at the 2-position, and the corresponding cis-olefins and fully saturated analogues are described. The compounds were evaluated as potential antagonists of platelet-activating
- Walser,Flynn,Mason,Crowley,Maresca,O'Donnell
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p. 1440 - 1446
(2007/10/02)
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- SYNTHESIS OF 2-(2-THIENYL)PYRIDINE AND SOME OF ITS DERIVATIVES
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2-(2-Thienyl)pyridine was obtained with a high yield from 2-thiophenecarbonitrile and acetylene at elevated pressure and temperature in the presence of η5-dicyclopentadienylcobalt (cobaltocene).The bromination, chlorination, nitration, carboxylation, and acetylation of 2-(2-thienyl)pyridine were studied.Oximation of 2-(5-acetyl-2-thienyl)pyridine in water-alcohol solution gave a mixture of 2-(5-methylcarbamoyl-2-thienyl)pyridine and syn-2-pyridine.
- Ivanov, A. P.,Levin, D. Z.,Promonenkov, V. K.,Mortikov, E. S.
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p. 570 - 575
(2007/10/02)
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