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CCR5 receptor antagonists: Discovery and SAR of novel 4-hydroxypiperidine derivatives

Autor: Dave Davey, Karen May, Shou-Fu Lu, Ming Wei, Jih-Lie Tseng, Laura Dunning, Gary Phillips, Robert G. Wei, Bin Ye, Stefan Jaroch, James Onuffer, Binglong Chen, Babu Subramanyam

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 17:1883-1887

The guanylhydrazone of 2-(4-chlorobenzyloxy)-5-bromobenzaldehyde, 1, with an IC50 of 840 nM against the CCR5 receptor was identified using high-throughput screening. Optimization efforts led to the discovery of a novel piperidine series of CCR5 antag

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3b3d586f76f46efc9c15cd8d44fe75b6
https://doi.org/10.1016/j.bmcl.2007.01.050

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CCR5 receptor antagonists: Discovery and SAR study of guanylhydrazone derivatives

Autor: Dave Davey, Arnaiz Damian O, Shou-Fu Lu, Laura Dunning, Yuo-Ling Chou, James Onuffer, Robert G. Wei, Gary Phillips, Wheeseong Lee, Bin Ye

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 17:231-234

High throughput screening (HTS) led to the identification of the guanylhydrazone of 2-(4-chlorobenzyloxy)-5-bromobenzaldehyde as a CCR5 receptor antagonist. Initial modifications of the guanylhydrazone series indicated that substitution of the benzyl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4925686f9f66976b3a1592c816c6e8c0
https://doi.org/10.1016/j.bmcl.2006.09.052

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Oxidative polycyclization with rhenium(VII) oxides: application of the stereoselectivity rules in the total synthesis of rollidecins C and D

Autor: Ehud Keinan, Lawrence J. D'Souza, Shou-Fu Lu, Subhash C. Sinha, Santosh C. Sinha

Publikováno v: Tetrahedron. 57:5255-5262

Rollidecin C, 1, and rollidecin D, 2, two adjacent bis-THF Annonaceous acetogenins, were synthesized from the partially functionalized ‘naked’ carbon skeletons 14 and 15, respectively. The retrosynthetic route to the target compounds was guided b

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::cbf253936666764c32d3268212a97a96
https://doi.org/10.1016/s0040-4020(01)00381-7

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Syntheses of (R)- and (S)-2- and 6-Fluoronorepinephrine and (R)- and (S)-2- and 6-Fluoroepinephrine: Effect of Stereochemistry on Fluorine-Induced Adrenergic Selectivities

Autor: Klaus Wilhelm Laue, O. Oshunleti, William L. Padgett, Kenneth L. Kirk, Günter Haufe, John W. Daly, Shou-fu Lu, Brian Herbert

Publikováno v: Journal of Medicinal Chemistry. 43:1611-1619

Several routes to the enantiomers of fluoronorepinephrines (1) and fluoroepinephrines (2) were explored. A catalytic enantioselective oxazaborolidine reduction and a chiral (salen)Ti(IV) catalyzed asymmetric synthesis of silyl cyanohydrins proved eff

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::af5da3505949bcf528370ac79352522d
https://doi.org/10.1021/jm990599h

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An efficient synthesis and biological activities of 19-nor-17β-hydroxy-17α-trifluoromethyl-Δ4-estren-3-one and its analogs

Autor: Shou-Fu Lu, Zhong-Qi Wang, Chuan-Jun Yang, Lin Chao

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 5:1899-1902

19-Nor-17 β -hydroxy-17 α -trifluoromethyl- Δ 4 -estren-3-one 6 and its analogs 7 and 8 have been synthesized in total yields of 82%, 54% and 27%, respectively, using Me 3 SiCF 3 as a trifluoromethylating agent. The three compounds showed high aff

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::4772b755b9eef4594e8108b299d91983
https://doi.org/10.1016/0960-894x(95)00320-s

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