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Items: 1 to 20 of 103

1.

Synthesis and profiling of a diverse collection of azetidine-based scaffolds for the development of CNS-focused lead-like libraries.

Lowe JT, Lee MD 4th, Akella LB, Davoine E, Donckele EJ, Durak L, Duvall JR, Gerard B, Holson EB, Joliton A, Kesavan S, Lemercier BC, Liu H, Marié JC, Mulrooney CA, Muncipinto G, Welzel-O'Shea M, Panko LM, Rowley A, Suh BC, Thomas M, Wagner FF, Wei J, Foley MA, Marcaurelle LA.

J Org Chem. 2012 Sep 7;77(17):7187-211. doi: 10.1021/jo300974j. Epub 2012 Aug 10.

2.

Synthesis of novel angular spirocyclic azetidines.

Guérot C, Tchitchanov BH, Knust H, Carreira EM.

Org Lett. 2011 Feb 18;13(4):780-3. doi: 10.1021/ol103050c. Epub 2011 Jan 14.

PMID:
21235246
3.

Diversity by divergence: Solution-phase parallel synthesis of a library of N-diversified 1-oxa-7-azaspiro[4.5]decan-2-yl-propanes and -butanes.

Kumar S, Thornton PD, Santini C.

ACS Comb Sci. 2013 Nov 11;15(11):564-71. doi: 10.1021/co4001056. Epub 2013 Oct 9.

PMID:
24079459
4.

Spiro-piperidine azetidinones as potent TRPV1 antagonists.

Xiao D, Palani A, Aslanian R, McKittrick BA, McPhail AT, Correll CC, Phelps PT, Anthes JC, Rindgen D.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):783-7. doi: 10.1016/j.bmcl.2008.12.024. Epub 2008 Dec 10.

PMID:
19114307
5.

Synthesis of a stereochemically diverse library of medium-sized lactams and sultams via S(N)Ar cycloetherification.

Gerard B, Duvall JR, Lowe JT, Murillo T, Wei J, Akella LB, Marcaurelle LA.

ACS Comb Sci. 2011 Jul 11;13(4):365-74. doi: 10.1021/co2000218. Epub 2011 Apr 28.

6.

2,6-Diazaspiro[3.3]heptanes: synthesis and application in Pd-catalyzed aryl amination reactions.

Burkhard J, Carreira EM.

Org Lett. 2008 Aug 21;10(16):3525-6. doi: 10.1021/ol801293f. Epub 2008 Jul 17.

PMID:
18630921
7.

Easy access to constrained peptidomimetics and 2,2-disubstituted azetidines by the unexpected reactivity profile of α-lithiated N-Boc-azetidines.

Parisi G, Capitanelli E, Pierro A, Romanazzi G, Clarkson GJ, Degennaro L, Luisi R.

Chem Commun (Camb). 2015 Nov 4;51(85):15588-91. doi: 10.1039/c5cc06323j.

PMID:
26355560
8.

Synthesis of a Spirocyclic Oxetane-Fused Benzimidazole.

Gurry M, McArdle P, Aldabbagh F.

Molecules. 2015 Jul 30;20(8):13864-74. doi: 10.3390/molecules200813864.

9.

Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor.

Kung DW, Coffey SB, Jones RM, Cabral S, Jiao W, Fichtner M, Carpino PA, Rose CR, Hank RF, Lopaze MG, Swartz R, Chen HT, Hendsch Z, Posner B, Wielis CF, Manning B, Dubins J, Stock IA, Varma S, Campbell M, DeBartola D, Kosa-Maines R, Steyn SJ, McClure KF.

Bioorg Med Chem Lett. 2012 Jul 1;22(13):4281-7. doi: 10.1016/j.bmcl.2012.05.024. Epub 2012 May 17.

PMID:
22677316
10.

Discovery of spirofused piperazine and diazepane amides as selective histamine-3 antagonists with in vivo efficacy in a mouse model of cognition.

Brown DG, Bernstein PR, Griffin A, Wesolowski S, Labrecque D, Tremblay MC, Sylvester M, Mauger R, Edwards PD, Throner SR, Folmer JJ, Cacciola J, Scott C, Lazor LA, Pourashraf M, Santhakumar V, Potts WM, Sydserff S, Giguère P, Lévesque C, Dasser M, Groblewski T.

J Med Chem. 2014 Feb 13;57(3):733-58. doi: 10.1021/jm4014828. Epub 2014 Jan 27.

PMID:
24410637
11.

Synthesis of dihydrouracils spiro-fused to pyrrolidines: druglike molecules based on the 2-arylethyl amine scaffold.

Blanco-Ania D, Valderas-Cortina C, Hermkens PH, Sliedregt LA, Scheeren HW, Rutjes FP.

Molecules. 2010 Mar 30;15(4):2269-301. doi: 10.3390/molecules15042269.

12.

Regioselective preparation of saturated spirocyclic and ring-expanded fused pyrazoles.

Merchant RR, Allwood DM, Blakemore DC, Ley SV.

J Org Chem. 2014 Sep 19;79(18):8800-11. doi: 10.1021/jo501624t. Epub 2014 Aug 28.

PMID:
25148419
13.

Synthesis of a family of spirocyclic scaffolds: building blocks for the exploration of chemical space.

Kumar S, Thornton PD, Painter TO, Jain P, Downard J, Douglas JT, Santini C.

J Org Chem. 2013 Jul 5;78(13):6529-39. doi: 10.1021/jo400738b. Epub 2013 Jun 26.

14.

Design, synthesis and decoration of molecular scaffolds for exploitation in the production of alkaloid-like libraries.

Craven P, Aimon A, Dow M, Fleury-Bregeot N, Guilleux R, Morgentin R, Roche D, Kalliokoski T, Foster R, Marsden SP, Nelson A.

Bioorg Med Chem. 2015 Jun 1;23(11):2629-35. doi: 10.1016/j.bmc.2014.12.048. Epub 2014 Dec 29.

PMID:
25600406
15.

Aminomethylhydroxylation of alkenes: Exploitation in the synthesis of scaffolds for small molecule libraries.

Colomer I, Adeniji O, Burslem GM, Craven P, Rasmussen MO, Willaume A, Kalliokoski T, Foster R, Marsden SP, Nelson A.

Bioorg Med Chem. 2015 Jun 1;23(11):2736-40. doi: 10.1016/j.bmc.2015.01.058. Epub 2015 Feb 11.

PMID:
25740633
16.

Reagent-based DOS: developing a diastereoselective methodology to access spirocyclic- and fused heterocyclic ring systems.

Damerla VS, Tulluri C, Gundla R, Naviri L, Adepally U, Iyer PS, Murthy YL, Prabhakar N, Sen S.

Chem Asian J. 2012 Oct;7(10):2351-60. doi: 10.1002/asia.201200385. Epub 2012 Aug 7.

PMID:
22887684
17.

Highly stereoselective, one-pot synthesis of azetidines and 2,4-dioxo-1,3-diazabicyclo[3.2.0] compounds mediated by I2.

Miao CB, Dong CP, Zhang M, Ren WL, Meng Q, Sun XQ, Yang HT.

J Org Chem. 2013 May 3;78(9):4329-40. doi: 10.1021/jo400181r. Epub 2013 Apr 19.

PMID:
23573992
18.

Impact of stereospecific intramolecular hydrogen bonding on cell permeability and physicochemical properties.

Over B, McCarren P, Artursson P, Foley M, Giordanetto F, Grönberg G, Hilgendorf C, Lee MD 4th, Matsson P, Muncipinto G, Pellisson M, Perry MW, Svensson R, Duvall JR, Kihlberg J.

J Med Chem. 2014 Mar 27;57(6):2746-54. doi: 10.1021/jm500059t. Epub 2014 Feb 26.

19.

Adventures in drug-like chemistry space: from oxetanes to spiroazetidines and beyond!

Rogers-Evans M, Knust H, Plancher JM, Carreira EM, Wuitschik G, Burkhard J, Li DB, Guérot C.

Chimia (Aarau). 2014;68(7-8):492-9. doi: 10.2533/chimia.2014.492.

PMID:
25437389
20.

Emulating the logic of monoterpenoid alkaloid biogenesis to access a skeletally diverse chemical library.

Liu S, Scotti JS, Kozmin SA.

J Org Chem. 2013 Sep 6;78(17):8645-54. doi: 10.1021/jo401262v. Epub 2013 Aug 27.

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