- Zn- And Cu-catalyzed coupling of tertiary alkyl bromides and oxalates to forge challenging C?O, C?S, and C?N bonds
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We describe here the facile construction of sterically hindered tertiary alkyl ethers and thioethers via the Zn(OTf)2catalyzed coupling of alcohols/phenols with unactivated tertiary alkyl bromides and the Cu(OTf)2-catalyzed thiolation of unactivated tertiary alkyl oxalates with thiols. The present protocol represents one of the most effective unactivated tertiary C(sp3)? heteroatom bond-forming conditions via readily accessible Lewis acid catalysis that is surprisingly less developed.
- Gong, Yuxin,Zhu, Zhaodong,Qian, Qun,Tong, Weiqi,Gong, Hegui
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supporting information
p. 1005 - 1010
(2021/02/01)
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- Single Peptide Backbone Surrogate Mutations to Regulate Angiotensin GPCR Subtype Selectivity
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Mutating the side-chains of amino acids in a peptide ligand, with unnatural amino acids, aiming to mitigate its short half-life is an established approach. However, it is hypothesized that mutating specific backbone peptide bonds with bioisosters can be exploited not only to enhance the proteolytic stability of parent peptides, but also to tune its receptor subtype selectivity. Towards this end, four [Y]6-Angiotensin II analogues are synthesized where amide bonds have been replaced by 1,4-disubstituted 1,2,3-triazole isosteres in four different backbone locations. All the analogues possessed enhanced stability in human plasma in comparison with the parent peptide, whereas only two of them achieved enhanced AT2R/AT1R subtype selectivity. This diversification has been studied through 2D NMR spectroscopy and unveiled a putative more structured microenvironment for the two selective ligands accompanied with increased number of NOE cross-peaks. The most potent analogue, compound 2, has been explored regarding its neurotrophic potential and resulted in an enhanced neurite growth with respect to the established agent C21.
- Vrettos, Eirinaios I.,Valverde, Ibai E.,Mascarin, Alba,Pallier, Patrick N.,Cerofolini, Linda,Fragai, Marco,Parigi, Giacomo,Hirmiz, Baydaa,Bekas, Nick,Grob, Nathalie M.,Stylos, Evgenios Κ.,Shaye, Hamidreza,Del Borgo, Mark,Aguilar, Marie-Isabel,Magnani, Francesca,Syed, Nelofer,Crook, Timothy,Waqif, Emal,Ghazaly, Essam,Cherezov, Vadim,Widdop, Robert E.,Luchinat, Claudio,Michael-Titus, Adina T.,Mindt, Thomas L.,Tzakos, Andreas G.
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supporting information
p. 10690 - 10694
(2020/07/25)
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- NEW TRICYCLIC ANGIOTENSIN II AGONISTS
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There is provided compounds of formula (I) wherein the dotted line, X1, X2, X3, A, Y1, Y2, Y3, Y4, Z1, Z2, R2 and R3 have meanings giv
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Page/Page column 32
(2008/06/13)
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- NEW BICYCLIC ANGIOTENSIN II AGONISTS
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There is provided a compound of formula (I) wherein R1a, R1b, X, Y1, Y2, Y3, Y4, Z1, Z2, R2 and R3 have meanings given in the description, and ph
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Page/Page column 36
(2008/06/13)
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- NEW TRICYCLIC ANGIOTENSIN II AGONISTS
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There is provided compounds of Formula (I), wherein A, X1, X2, X3, X4, Y1, Y2, Y3, Y4, Z1, Z2, R4 and R5 have meanings given in the description, and pharmaceuticalfy-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.
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Page/Page column 35
(2008/06/13)
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- NEW BICYCLIC ANGIOTENSIN II AGONISTS
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There is provided compounds of formula (I), wherein R1a, R1b, n, Y1, Y2, Y3, Y4, Z1, Z2, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.
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- NEW TRICYCLIC ANGIOTENSIN II AGONISTS
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There is provided compounds of formula (I), wherein the dotted line, X1, X2, X3, A, Y1, Y2, Y3, Y4, Z1, Z2, R2 and R3 have meanings gi
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- NEW TRICYCLIC ANGIOTENSIN II AGONISTS
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There is provided compounds of formula (I), wherein the dotted lines, XI, X2, X3, X4, A, YI, Y2, Y3, Y4, ZI, Z2, R2 and R3
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- BICYCLIC COMPOUNDS USEFUL AS ANGIOTENSIN II AGONISTS
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There is provided compounds of formula I, wherein R1a, R1b, X, Y1, Y2, Y3, Y4, Z 1, Z2, R2 and R3 have meanings given in the description, and pha
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- Sulfonamides useful as carbonic anhydrase inhibitors
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Sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.
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- Thiophene sulfonamides useful as carbonic anhydrase inhibitors
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Thiophene sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.
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