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The following term was not found in PubMed: dec-7-en-10-one
Unknown field was ignored: [5.3.0]
Page 1
Synthesis, biological evaluation and docking studies of a novel class of sulfur-bridged diazabicyclo[3.3.1]nonanes.
Murineddu G, Asproni B, Corona P, Gessi S, Merighi S, Battistello E, Sturaro C, Calò G, Galeotti N, Temml V, Herdlinger S, Schuster D, Pinna GA. Murineddu G, et al. Bioorg Chem. 2020 Sep;102:104072. doi: 10.1016/j.bioorg.2020.104072. Epub 2020 Jul 6. Bioorg Chem. 2020. PMID: 32693307
A small library of 3-thia-7,9-diazabicyclo[3.3.1]nonanes was synthesized and their opioid receptors affinity and selectivity evaluated. Among these novel sulfur-bridged compounds, the (E) 9-[3'-(3-chlorophenyl)-but-2'-en-1'-yl]-7-propionyl-3-thia-7,9-diaza …
A small library of 3-thia-7,9-diazabicyclo[3.3.1]nonanes was synthesized and their opioid receptors affinity and selectivity e …
Novel diazabicycloalkane delta opioid agonists.
Loriga G, Lazzari P, Manca I, Ruiu S, Falzoi M, Murineddu G, Bottazzi ME, Pinna G, Pinna GA. Loriga G, et al. Bioorg Med Chem. 2015 Sep 1;23(17):5527-38. doi: 10.1016/j.bmc.2015.07.036. Epub 2015 Jul 27. Bioorg Med Chem. 2015. PMID: 26252963
In particular, we have simplified the diazatricyclodecane motif of delta opioid agonist prototype 1a with bridged bicyclic cores. 3,6-diazabicyclo[3.1.1]heptane, 3,8-diazabicyclo[3.2.1]octane, 3,9-diazabicyclo[3.3.1]nonane, 3,9-diazabicyclo[4.2. …
In particular, we have simplified the diazatricyclodecane motif of delta opioid agonist prototype 1a with bridged bicyclic cores. 3,6-diazab …
Rigid Scaffolds: Synthesis of 2,6-Bridged Piperazines with Functional Groups in all three Bridges.
Gao D, Penno C, Wünsch B. Gao D, et al. ChemistryOpen. 2020 Aug 27;9(8):874-889. doi: 10.1002/open.202000188. eCollection 2020 Aug. ChemistryOpen. 2020. PMID: 32884883 Free PMC article.
Whereas reaction of such an aldehyde with base provided the bicyclic alcohol 9-benzyl-6-hydroxy-3-(4-methoxybenzyl)-3,9-diazabicyclo[3.3.1]nonane-2,4-dione in only 10 % yield, the corresponding sulfinylimines reacted with base to give N-(2,4-dioxo-3,9-diaz …
Whereas reaction of such an aldehyde with base provided the bicyclic alcohol 9-benzyl-6-hydroxy-3-(4-methoxybenzyl)-3,9-diazabicyc …
Synthesis of 7,9-diazabicyclo[4.2.2]decanes as conformationally restricted kappa receptor agonists: fine tuning of the dihedral angle of the ethylenediamine pharmacophore.
Sunnam SK, Rack E, Schepmann D, Wünsch B. Sunnam SK, et al. Eur J Med Chem. 2011 Jun;46(6):1972-82. doi: 10.1016/j.ejmech.2011.01.064. Epub 2011 Feb 3. Eur J Med Chem. 2011. PMID: 21481987
In order to slightly modify the orientation of the pharmacophoric structural elements of the potent kappa agonists 7 and 8, the three-membered bridge of these compounds was enlarged to four carbon atoms. ...
In order to slightly modify the orientation of the pharmacophoric structural elements of the potent kappa agonists 7 and 8, the three …
Synthesis, modelling, and mu-opioid receptor affinity of N-3(9)-arylpropenyl-N-9(3)-propionyl-3,9-diazabicycl.
Pinna GA, Murineddu G, Curzu MM, Villa S, Vianello P, Borea PA, Gessi S, Toma L, Colombo D, Cignarella G. Pinna GA, et al. Farmaco. 2000 Aug;55(8):553-62. doi: 10.1016/s0014-827x(00)00036-7. Farmaco. 2000. PMID: 11132733
A series of N-3-arylpropenyl-N-9-propionyl-3,9-diazabicyclo[3.3.1]nonanes (1a-g) and of reverted N-3-propionyl-N-9-arylpropenyl isomers (2a-g), as homologues of the previously reported analgesic 3,8-diazabicyclo[3.2.1]octanes (I-II), were synthesized and eval …
A series of N-3-arylpropenyl-N-9-propionyl-3,9-diazabicyclo[3.3.1]nonanes (1a-g) and of reverted N-3-propionyl-N-9-arylpropeny …
Antagonistic activities of N-3389, a newly synthesized diazabicyclo derivative, at 5-HT3 and 5-HT4 receptors.
Hagihara K, Hayakawa T, Arai T, Eguchi H, Mino S, Kawase S. Hagihara K, et al. Eur J Pharmacol. 1994 Dec 12;271(1):159-66. doi: 10.1016/0014-2999(94)90276-3. Eur J Pharmacol. 1994. PMID: 7698198
The antagonistic activities of compound N-3389 (endo-3,9-dimethyl-3,9- diazabicyclo[3,3,1]non-7-yl 1H-indazole-3-carboxamide dihydrochloride) at 5-HT3 and 5-HT4 receptors were examined using in vitro and in vivo assays. N-3389 showed potent 5-HT3 receptor antagonist …
The antagonistic activities of compound N-3389 (endo-3,9-dimethyl-3,9- diazabicyclo[3,3,1]non-7-yl 1H-indazole-3-carboxamide d …
Synthesis and biological evaluation of conformationally restricted sigma(1) receptor ligands with 7,9-diazabicyclo[4.2.2]decane scaffold.
Sunnam SK, Schepmann D, Rack E, Fröhlich R, Korpis K, Bednarski PJ, Wünsch B. Sunnam SK, et al. Org Biomol Chem. 2010 Dec 21;8(24):5525-40. doi: 10.1039/c0ob00402b. Epub 2010 Oct 15. Org Biomol Chem. 2010. PMID: 20953473
The key step in the synthesis of the 7,9-diazabicyclo[4.2.2]decane system was a modified Dieckmann condensation of piperazinebutyrate 11, which makes use of trapping the first cyclized intermediate with TMS-Cl. ...
The key step in the synthesis of the 7,9-diazabicyclo[4.2.2]decane system was a modified Dieckmann condensation of piperazineb …
Synthesis and transporter binding properties of bridged piperazine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909).
Zhang Y, Rothman RB, Dersch CM, de Costa BR, Jacobson AE, Rice KC. Zhang Y, et al. J Med Chem. 2000 Dec 14;43(25):4840-9. doi: 10.1021/jm000300r. J Med Chem. 2000. PMID: 11123994
The binding data indicated that compounds 7 and 11, the N-methyl- and N-propylphenyl-3,8-diaza[3.2. 1]bicyclooctane analogues of 3, showed high affinity for the DAT (IC(50) = 8.0 and 8.2 nM, respectively), and 7 had high selectivity at the DAT relative to the …
The binding data indicated that compounds 7 and 11, the N-methyl- and N-propylphenyl-3,8-diaza[3.2. 1]bicyclooctane analogues of 3, s …
Synthesis and structure-activity relationships of 7-diazabicycloalkylquinolones, including danofloxacin, a new quinolone antibacterial agent for veterinary medicine.
McGuirk PR, Jefson MR, Mann DD, Elliott NC, Chang P, Cisek EP, Cornell CP, Gootz TD, Haskell SL, Hindahl MS, et al. McGuirk PR, et al. J Med Chem. 1992 Feb 21;35(4):611-20. doi: 10.1021/jm00082a001. J Med Chem. 1992. PMID: 1311762
The diazabicycloalkyl side chains investigated at the 7-position (benzoxazine 10-position) include (1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]heptane (2), (1S,4S)-2,5-diazabicyclo[2.2.1]heptane (3), (1R,4R)-5-methyl-2,5-diazabicyclo[2.2.1]heptane (4), 8-methyl-3,8-diaz …
The diazabicycloalkyl side chains investigated at the 7-position (benzoxazine 10-position) include (1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]h …
Solid-phase parallel synthesis of natural product-like diaza-bridged heterocycles through Pictet-Spengler intramolecular cyclization.
Lee SC, Park SB. Lee SC, et al. J Comb Chem. 2006 Jan-Feb;8(1):50-7. doi: 10.1021/cc0501054. J Comb Chem. 2006. PMID: 16398553
This approach is exemplified by the preparation of a 384-member library of 3,9-diazabicyclo[3.3.1]non-6-en-2-one skeletons, fused with indole and dihydroxybenzene and diversified at two bridging nitrogen atoms, using the solid-phase parallel synthetic methodology wi …
This approach is exemplified by the preparation of a 384-member library of 3,9-diazabicyclo[3.3.1]non-6-en-2-one skeletons, fu …
11 results