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Practical Synthesis of 4‐Fluoro‐2‐(methylthio)benzylamine and the Corresponding Sulfone and Sulfonamide

Autor: Michelle S. Kuo, D. S. Perlow, H. Marie Moritz, John S. Wai, Melissa S. Egbertson

Publikováno v: Synthetic Communications. 37:1887-1897

Practical syntheses of 4‐fluoro‐2‐(methylthio)benzylamine 1 and the corresponding 2‐methylsulfonyl analog 2 are reported. The methylthio moiety was introduced regioselectively by two methods. In the first method, metallation of 4‐fluoro‐2

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::cba871bc41c1f6391d993ea9f2c74b05
https://doi.org/10.1080/00397910701319221

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Nonpeptide oxytocin antagonists: Potent, orally bioavailable analogs of L-371,257 containing A 1-R-(pyridyl)ethyl ether terminus

Autor: C. J. Woyden, Roger M. Freidinger, Mark G. Bock, Duane R. Reiss, Joseph M. Pawluczyk, Michelle S. Kuo, Amy G. Quigley, Douglas J. Pettibone, Maribeth T. Guidotti, E V Lis, D. S. Perlow, Peter D. Williams

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 8:3081-3086

Structure-activity studies on the oxytocin antagonist 1 (L-371,257) have identified a new series of high affinity, receptor-selective OT antagonists in which the N-acetyl-4-piperidinyl ether terminus in 1 has been replaced with a 1-(aryl)ethoxy group

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::765c00dce9dedfe799c42f855a73f496
https://doi.org/10.1016/s0960-894x(98)00568-x

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Synthesis of protected lactam-bridged dipeptides

Autor: D S, Perlow, R M, Freidinger

Publikováno v: Methods in molecular medicine. 23

Lactam-bridged dipeptides are useful tools for the introduction of conformational constraint in higher peptides. General methods have been devised for the synthesis of dipeptides having five-, six-, and seven-membered ring constraints (1,2). This cha

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::5234d3cafa210a380753bacec6234643
https://pubmed.ncbi.nlm.nih.gov/21380900

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The selectivity of statine-based inhibitors against various human aspartic proteinases

Autor: R A Jupp, B M Dunn, J W Jacobs, G Vlasuk, K E Arcuri, D F Veber, D S Perlow, L S Payne, J Boger, S de Laszlo, P K Chakravarty, J T Broeke, D G Hangauer, D Ondeyka, W J Greenlee, J Kay

Publikováno v: Biochemical Journal. 265:871-878

The interactions of five human enzymes (renin, pepsin, gastricsin, cathepsin D and cathepsin E) and the aspartic proteinase from Endothia parasitica with several series of synthetic inhibitors were examined. All of the inhibitors contained the dipept

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::62a4f9d0bd5c538f6a6fe0780add6d9d
https://doi.org/10.1042/bj2650871

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Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency

Autor: Michelle R. Levy, K.J. Stauffer, Roger M. Freidinger, E V Lis, Mark G. Bock, Stuart R. Michelson, Douglas J. Pettibone, D. S. Perlow, Christopher A. Salvatore, Marlene A. Jacobson, B. E. Evans, Joseph M. Pawluczyk, Amy G. Quigley, C. J. Woyden, Maribeth T. Guidotti, Peter D. Williams, Michelle S. Kuo, Steven N. Gallicchio, Duane R. Reiss

Publikováno v: Bioorganicmedicinal chemistry letters. 9(9)

Structure-activity studies on the oxytocin antagonist 1 (L-371,257; Ki = 9.3 nM) have led to the identification of a related series of compounds containing an ortho-trifluoroethoxyphenylacetyl core which are orally bioavailable and have significantly

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5060b712acd7d054079f1d505f8a7310
https://pubmed.ncbi.nlm.nih.gov/10340620

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Renin inhibitors. Syntheses of subnanomolar, competitive, transition-state analogue inhibitors containing a novel analogue of statine

Autor: J, Boger, L S, Payne, D S, Perlow, N S, Lohr, M, Poe, E H, Blaine, E H, Ulm, T W, Schorn, B I, LaMont, T Y, Lin

Publikováno v: Journal of medicinal chemistry. 28(12)

Analogues of the renin octapeptide substrate were synthesized in which replacement of the scissile dipeptide with (3S,4S)-4-amino-3-hydroxy-6-methylheptanoic acid (statine, Sta) transformed the substrate sequence into potent, transition-state analogu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d25555479b6c710c8eedef351672e520
https://pubmed.ncbi.nlm.nih.gov/3906131

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