- Design and synthesis of azaindole heterocycle decorated new scaffold in fluorometric sensing of F? and H2PO4?
-
7-Azaindole has been used in designing new molecular structure 1 on enediyne spacer for its application in anion sensing. New structure 1 has been established as efficient fluorescent sensor of H2PO4? and F? ion
- Ghosh, Kumaresh,Ali, Sk. Sarfaraj,Joardar, Soumen
-
p. 3558 - 3565
(2020/08/06)
-
- Heat Versus Basic Conditions: Intramolecular Dehydro-Diels-Alder Reaction of 1-Indolyl-1,6-heptadiynes for the Selective Synthesis of Substituted Carbazoles
-
The intramolecular dehydro-Diels-Alder reaction of 1-indolyl-1,6-heptadiynes proceeds smoothly under rather mild heating conditions to give substituted carbazoles in moderate to good yields. The reaction of 7-aryl-1-indolyl-1,6-heptadiynes under heating gives the corresponding carbazoles chemoselectively in high yields, whereas the reaction under basic conditions gives naphthalenes as major products.
- Kudoh, Takayuki,Fujisawa, Syo,Kitamura, Megumi,Sakakura, Akira
-
p. 2189 - 2193
(2017/09/26)
-
- ANTI-BACTERIAL PYRUVATE KINASE MODULATOR COMPOUNDS, COMPOSITIONS, USES AND METHODS
-
Compounds of general formula I that are capable of inhibiting bacterial pyruvate kinase and/or bacterial growth. The compounds may find use as antibacterial agents in therapeutic and/or non- therapeutic contexts.
- -
-
-
- Discovery and optimization of a new class of pyruvate kinase inhibitors as potential therapeutics for the treatment of methicillin-resistant Staphylococcus aureus infections
-
A novel series of bis-indoles derived from naturally occurring marine alkaloid 4 were synthesized and evaluated as inhibitors of methicillin-resistant Staphylococcus aureus (MRSA) pyruvate kinase (PK). PK is not only critical for bacterial survival which
- Kumar, Nag S.,Dullaghan, Edie M.,Finlay, B. Brett,Gong, Huansheng,Reiner, Neil E.,Jon Paul Selvam,Thorson, Lisa M.,Campbell, Sara,Vitko, Nicholas,Richardson, Anthony R.,Zoraghi, Roya,Young, Robert N.
-
p. 1708 - 1725
(2014/03/21)
-
- Azaindole-1,2,3-triazole conjugate as selective fluorometric sensor for dihydrogenphosphate
-
A new receptor 1 has been designed and synthesized. The open cavity of 1 selectively recognizes H2PO4- over a series of other anions in CH3CN containing 0.01% DMSO by exhibiting a ratiometric change in emission.
- Ghosh, Kumaresh,Kar, Debasis,Joardar, Soumen,Sahu, Debashis,Ganguly, Bishwajit
-
p. 16144 - 16151
(2013/09/12)
-
- A convenient iodination of indoles and derivatives
-
We report a direct iodination of indole and derivative compounds with iodine monochloride (ICl) in the presence of Celite. This procedure has now been extended to the iodination of substituted indoles, azaindoles and pyrroles. The scope of this procedure
- Hamri, Salha,Rodríguez, Jose,Basset, Joan,Guillaumet, Gérald,Dolors Pujol
-
supporting information; experimental part
p. 6269 - 6275
(2012/08/28)
-
- The synthesis of 2- and 3-aryl indoles and 1,3,4,5-tetrahydropyrano[4,3-b]indoles and their antibacterial and antifungal activity
-
A series of 2- and 3-aryl substituted indoles and two 1,3,4,5-tetrahydropyrano[4,3-b]indoles were synthesized from indole and 5-methoxyindole. The 2-aryl indoles were synthesized from the 1-(phenylsulfonyl)indole derivatives using magnesiation followed by iodination. The 2-iodinated compounds were then subjected to Suzuki-Miyaura reactions. In addition, the 3-aryl indoles were made from the corresponding 3-bromoindoles using Suzuki-Miyaura reactions. The 1,3,4,5-tetrahydropyrano[4,3-b]indoles were also synthesized from 1-(phenylsulfonyl)indole by magnesiation followed by treatment with allylbromide. The product was then converted into [2-allyl-1-(phenylsulfonyl)-1H-indol-3-yl]methanol which upon exposure to Hg(OAc)2 and NaBH4 afforded tetrahydropyrano[4,3-b]indoles. A number of the 2- and 3-aryl indoles displayed noteworthy antimicrobial activity, with compound 13a displaying the most significant activity (3.9 μg/mL) against the Gram-positive micro-organism Bacillus cereus.
- Leboho, Tlabo C.,Michael, Joseph P.,van Otterlo, Willem A.L.,van Vuuren, Sandy F.,de Koning, Charles B.
-
scheme or table
p. 4948 - 4951
(2009/12/24)
-
- Fluorous synthesis of yuehchukene by α-lithiation of perfluoroalkyl-tagged 1-(arylsulfonyl)indole with mesityllithium
-
Lithiation chemistry has not been well explored in fluorous synthesis because of the lack of appropriate base-resistant fluorous tags; we recently developed a perfluoroalkylated arylsulfonyl tag for the protection of the indole ring nitrogen atom. Mesityl
- Naka, Hiroshi,Akagi, Yusuke,Yamada, Kyoko,Imahori, Tatsushi,Kasahara, Takahiro,Kondo, Yoshinori
-
p. 4635 - 4637
(2008/03/12)
-
- A convenient synthesis of 2-nitroindoles
-
The reaction of 2-iodo- and 2-bromoindoles with silver nitrite in aqueous acetone affords the corresponding 2-nitroindoles in modest to good yields.
- Roy, Sujata,Gribble, Gordon W.
-
p. 1325 - 1328
(2007/10/03)
-
- Benzannulation reactions of Fischer carbene complexes for the synthesis of indolocarbazoles
-
The synthesis of indolocarbazoles was achieved via photochemical and thermal annulation reactions of chromium Fischer carbene complexes. This methodology allows for facile incorporation of hydrogen bonding functionality which complements the pharmacophore contained within bioactive indolocarbazole natural products.
- Merlic, Craig A.,You, Ying,McInnes, Daniel M.,Zechman, Andrea L.,Miller, Michael M.,Deng, Qiaolin
-
p. 5199 - 5212
(2007/10/03)
-
- Intermolecular reactions of indol-2-yl radicals: A new route to 2-substituted indoles
-
The generation of indol-2yl radicals and their addition to a variety of radical accepters to prepare 2-substituted indoles is presented.
- Fiumana, Andrea,Jones, Keith
-
p. 1761 - 1762
(2007/10/03)
-
- Biphenylsulfonamide endothelin antagonists: Structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2'-amino-N-(3,4- dimethyl-5-isoxazolyl)-4'-(2-methylpropyl)[1,1'-biphenyl]-2-sulfonamide (BMS- 187308)
-
Substitution at the ortho position of N-(3,4-dimethyl-5-isoxazolyl) benzenesulfonamide led to the identification of the biphenylsulfonamides as a novel series of endothelin-A (ETA) selective antagonists. Appropriate substitutions on the pendant phenyl ring led to improved binding as well as functional activity. A hydrophobic group such as isobutyl or isopropoxyl was found to be optimal at the 4'-position. Introduction of an amino group at the 2'-position also led to improved analogues. Combination of the optimal 4'- isobutyl substituent with the 2'-amino function afforded an analogue (20, BMS-187308) with improved ET(A) binding affinity and functional activity. Compound 20 also has good oral activity in inhibiting the pressor effect caused by an ET-1 infusion in rats. Doses of 10 and 30 μmol/kg iv 20 attenuated the pressor responses due to the administration of exogenous ET-1 to conscious monkeys, indicating that the compound inhibits the in vivo activity of endothelin-1 in nonhuman primates.
- Murugesan, Natesan,Gu, Zhengxiang,Stein, Philip D.,Bisaha, Sharon,Spergel, Steve,Girotra, Ravi,Lee, Ving G.,Lloyd, John,Misra, Raj N.,Schmidt, Joan,Mathur, Arvind,Stratton, Leslie,Kelly, Yolanda F.,Bird, Eileen,Waldron, Tom,Liu, Eddie C.-K.,Zhang, Rongan,Lee, Helen,Serafino, Randy,Abboa-Offei, Benoni,Mathers, Parker,Giancarli, Mary,Seymour, Andrea Ann,Webb, Maria L.,Moreland, Suzanne,Barrish, Joel C.,Hunt, John T.
-
p. 5198 - 5218
(2007/10/03)
-
- Synthesis of indolocarbazoles via sequential palladium catalyzed cross- coupling and benzannulation reactions
-
Differentially substituted indolocarbazoles are readily prepared via a synthetic route employing two palladium catalyzed reactions. First, biindoles are prepared from a palladium catalyzed cross coupling reaction. Second, a new palladium catalyzed benzannulation reaction employing biindolyl iodides and alkynes provides indolocarbazoles.
- Merlic, Craig A.,McInnes, Daniel M.
-
p. 7661 - 7664
(2007/10/03)
-
- Magnesiation of indoles with magnesium amide bases
-
1-Substituted indole derivatives are deprotonated with Hauser bases (R2NMgBr) or magnesium diamide [(R2N)2-Mg] to give magnesioindoles which are then reacted with electrophiles.
- Kondo, Yoshinori,Yoshida, Akihiro,Sakamoto, Takao
-
p. 2331 - 2332
(2007/10/03)
-
- Synthesis of Alkyl-Substituted N-Protected Indoles via Acylation and Reductive Deoxygenation
-
The synthesis of 2-, 3-, and 5-alkyl-1-(phenylsulfonyl)indoles involving Friedel-Crafts acylation followed by reductive deoxygenation is described.The application of this acylation-deoxygenation sequence to 3-acyl-1-(phenylsulfonyl)indoles bearing potenti
- Ketcha, Daniel M.,Lieurance, Brett A.,Homan, Dominic F. J.,Gribble, Gordin W.
-
p. 4350 - 4356
(2007/10/02)
-