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Serendipitous synthesis of cross-conjugated dienes by cascade deconstructive esterification of thiomorpholinone-tethered alkenoic acids.
Farah AO, Garcia J, Borg C, Beng TK. Farah AO, et al. RSC Adv. 2023 Jan 23;13(5):3181-3185. doi: 10.1039/d2ra07916j. eCollection 2023 Jan 18. RSC Adv. 2023. PMID: 36756410 Free PMC article.
In a succinct manifestation of this 'scaffold hopping' concept, we herein describe a cascade reaction, which converts thiomorpholinone-tethered alkenoic acids to 1,1-disubstituted amino-1,3-dienes. ...Several control experiments have revealed that the alkenyl substituent i …
In a succinct manifestation of this 'scaffold hopping' concept, we herein describe a cascade reaction, which converts thiomorpholinone …
Enantioselective synthesis of dialkylated N-heterocycles by palladium-catalyzed allylic alkylation.
Numajiri Y, Jiménez-Osés G, Wang B, Houk KN, Stoltz BM. Numajiri Y, et al. Org Lett. 2015 Mar 6;17(5):1082-5. doi: 10.1021/ol503425t. Epub 2015 Feb 25. Org Lett. 2015. PMID: 25714704 Free PMC article.
These catalytic conditions enable access to various heterocycles, such as morpholinone, thiomorpholinone, oxazolidin-4-one, 1,2-oxazepan-3-one, 1,3-oxazinan-4-one, and structurally related lactams, all bearing fully substituted alpha-positions. ...
These catalytic conditions enable access to various heterocycles, such as morpholinone, thiomorpholinone, oxazolidin-4-one, 1,2-oxaze …
Bafilomycins produced in culture by Streptomyces spp. isolated from marine habitats are potent inhibitors of autophagy.
Carr G, Williams DE, Díaz-Marrero AR, Patrick BO, Bottriell H, Balgi AD, Donohue E, Roberge M, Andersen RJ. Carr G, et al. J Nat Prod. 2010 Mar 26;73(3):422-7. doi: 10.1021/np900632r. J Nat Prod. 2010. PMID: 20028134
The new bafilomycins F (1), G (2), H (3), and J (5) along with several co-occurring known analogues showed potent inhibition of autophagy in microscopy and biochemical assays. The thiomorpholinone fragment present in bafilomycin F (1) has not previously been found in a nat …
The new bafilomycins F (1), G (2), H (3), and J (5) along with several co-occurring known analogues showed potent inhibition of autophagy in …
Discovery and pharmacological characterization of aryl piperazine and piperidine ethers as dual acting norepinephrine reuptake inhibitors and 5-HT1A partial agonists.
Gray DL, Xu W, Campbell BM, Dounay AB, Barta N, Boroski S, Denny L, Evans L, Stratman N, Probert A. Gray DL, et al. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6604-7. doi: 10.1016/j.bmcl.2009.10.014. Epub 2009 Oct 12. Bioorg Med Chem Lett. 2009. PMID: 19854053
Targeted screening of NRI-active compounds for binding to the 5-HT(1A) receptor provided a series of thiomorpholinone hits with this dual activity profile. Several iterations of design, synthesis, and testing led to substituted piperidine diphenyl ethers which are potent N …
Targeted screening of NRI-active compounds for binding to the 5-HT(1A) receptor provided a series of thiomorpholinone hits with this …
Combinatorial chemistry: from peptides and peptidomimetics to small organic and heterocyclic compounds.
Nefzi A, Dooley C, Ostresh JM, Houghten RA. Nefzi A, et al. Bioorg Med Chem Lett. 1998 Sep 8;8(17):2273-8. doi: 10.1016/s0960-894x(98)00412-0. Bioorg Med Chem Lett. 1998. PMID: 9873527
The solid phase synthesis of heterocyclic compounds such as diazepine and thiomorpholinone are also described....
The solid phase synthesis of heterocyclic compounds such as diazepine and thiomorpholinone are also described....
11 results