- 8-Hydroxyquinolin-2(1H)-one analogues as potential β2-agonists: Design, synthesis and activity study
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β2-Agonists that bind to plasmalemmal β2-adrenoceptors causing cAMP accumulation are widely used as bronchodilators in chronic respiratory diseases. Here, we designed and synthesized a group of 8-hydroxyquinolin-2(1H)-one analogues and studied their β2-agonistic activities with a cellular cAMP assay. Compounds B05 and C08 were identified as potent (EC50 2-agonists among the compounds tested. They behaved as partial β2-agonists in non-overexpressed HEK293 cells, and possessed rapid smooth muscle relaxant actions and long duration of action in isolated guinea pig tracheal strip preparations. In summary, B05 and C08 are β2-agonists with potential applicability in chronic respiratory diseases.
- Xing, Gang,Zhi, Zhengxing,Yi, Ce,Zou, Jitian,Jing, Xuefeng,Yiu-Ho Woo, Anthony,Lin, Bin,Pan, Li,Zhang, Yuyang,Cheng, Maosheng
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- METHOD FOR SYNTHESIZING D3 DOPAMINE RECEPTOR AGONISTS
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An improved method for synthesizing a compound according to formula (I) by reaction of a compound of formula (II) with a sulfinamide according to formula (III). The resultant compound is then reduced and hydrolyzed, and optionally alkylated or arylated to
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Page/Page column 22-24
(2020/05/28)
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- Functional Characterization of a Novel Series of Biased Signaling Dopamine D3 Receptor Agonists
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Dopamine receptors play an integral role in controlling brain physiology. Importantly, subtype selective agonists and antagonists of dopamine receptors with biased signaling properties have been successful in treating psychiatric disorders with a low inci
- Xu, Wei,Wang, Xiaozhao,Tocker, Aaron M.,Huang, Peng,Reith, Maarten E. A.,Liu-Chen, Lee-Yuan,Smith, Amos B.,Kortagere, Sandhya
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p. 486 - 500
(2017/03/20)
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- Switchable asymmetric bio-epoxidation of α,β-unsaturated ketones
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Efficient asymmetric bio-epoxidation of electron-deficient α,β-unsaturated ketones was realized via a tandem reduction-epoxidation-dehydrogenation cascade, which proceeds in a switchable manner to afford either chiral epoxy ketones or allylic epoxy alcoho
- Liu, Yu-Chang,Wu, Zhong-Liu
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supporting information
p. 1158 - 1161
(2016/01/15)
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- Chemoselective conjugate reduction of α,β-unsaturated ketones catalyzed by rhodium amido complexes in aqueous media
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Although a notable feature of Noyori's Ru-TsDPEN complex is that the transfer hydrogenation reaction is highly chemoselective for the C-O functional group and tolerant of alkenes, our early report indicated that the chemoselectivity could be switched from C-O to C-C bonds in the transfer hydrogenation of activated α,β-unsaturated ketones. Now we have found that a variety of α,β-unsaturated ketones, even without other electron-withdrawing functional groups, could be reduced on the alkenic double bonds with high selectivities employing amido-rhodium hydride complex in aqueous media, and up to 100% chemoselectivity has been achieved. It is notable that the chemoselectivity was improved significantly on going from organic solvent to water. Moreover, a 1,4-addition mechanism has been proposed on the basis of the corresponding experimental details and computational analysis.
- Li, Xuefeng,Li, Liangchun,Tang, Yuanfu,Zhong, Ling,Cun, Linfeng,Zhu, Jin,Liao, Jian,Deng, Jingen
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experimental part
p. 2981 - 2988
(2010/07/05)
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- A domino annulation reaction under Willgerodt-Kindler conditions
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(Chemical Equation Presented) Butanone side chains at arenes and hetarenes, efficiently introduced by a Heck-type reaction, are transformed to annulated thieno[3,2-b]thiophenes in a domino redox process under Willgerodt-Kindler conditions. A nucleophilic aromatic substitution with an intermediary thioenolate is a reasonable key step of this process.
- Kadzimirsz, Daniel,Kramer, Daniel,Sripanom, Lertnarong,Oppel, Iris M.,Rodziewicz, Pawel,Doltsinis, Nikos L.,Dyker, Gerald
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p. 4644 - 4649
(2008/09/21)
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- Triketoacid inhibitors of HIV-integrase: A new chemotype useful for probing the integrase pharmacophore
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Integrase is one of three enzymes expressed by HIV and represents a validated target for therapy. This study reports on the discovery of a new triketoacid-based chemotype that selectively inhibits the strand transfer reaction of HIV-integrase. SAR studies showed that the template binds to integrase in a manner similar to the diketoacid-based inhibitors. Moreover, comparison of the new chemotype to two different diketoacid templates led us to propose two aryl-binding domains in the inhibitor binding site. This information was used to design a new diketoacid template with improved activity against the enzyme.
- Walker, Michael A.,Johnson, Timothy,Ma, Zhuping,Banville, Jacques,Remillard, Roger,Kim, Oak,Zhang, Yunhui,Staab, Andrew,Wong, Henry,Torri, Albert,Samanta, Himadri,Lin, Zeyu,Deminie, Carol,Terry, Brian,Krystal, Mark,Meanwell, Nicholas
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p. 2920 - 2924
(2007/10/03)
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- HIV integrase inhibitors
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The present invention relates to the inhibition of HIV integrase, and to the treatment of AIDS or ARC by administering compounds of the following formula, or a tautomer of said compound, or a pharmaceutically acceptable salt, solvate or prodrug of said compound or of a tautomer thereof. wherein R1 is phenyl, wherein said phenyl is substituted from 1-3 times with R2, or R1 naphthyl, and wherein said naphthyl is optionally substituted from 1-3 times with R2; each R2 is independently selected from halo, C1-C3 alkyl, C1-C2 alkoxy, C1-C3 haloalkyl, and phenyl-(CH2)mOn—; m is 0 or 1; n is 0 or 1; and Z is methylene or —C(O)—, provided that when Z is —C(O)— said substituted phenyl is not ortho-chloro phenyl.
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- Cyclic Amidines Part 27. An Unambiguous Synthesis of 5,10,14c-Triazabenzo naphthanthracene by a Palladium Catalysed Cyclodehalogenation
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An unambiguous route to the title triazabenzonaphthanthracene (5) is reported via a palladium-catalyzed cyclodehalogenation of the 6-chloro-7-(2-chlorobenzylidene)-benzanthracene (10) avoiding high temperature reactions and the possibility of skeletal rea
- Upton, Christopher
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p. 951 - 965
(2007/10/02)
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