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Publikationer i urvalet

43 träffar

Bibliografisk träff 2023-11-25

Synthetic GPR40/FFAR1 agonists: An exhaustive survey on the most recent chemical classes and their structure-activity relationships.

Paul A, Nahar S, Nahata P, Sarkar A, Maji A, Samanta A, Karmakar S, Maity TK.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2023.115990

Bibliografisk träff 2023-03-11

Discovery of orally effective and safe GPR40 agonists by incorporating a chiral, rigid and polar sulfoxide into β-position to the carboxylic acid.

Chen C, Guo SM, Sun Y, Li H, Hu N, Yao K, Ni H, Xia Z, Xu B, Xie X, Long YQ.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2023.115267

Bibliografisk träff 2022-11-02

Optimization of First-in-Class Dual-Acting FFAR1/FFAR4 Allosteric Modulators with Novel Mode of Action.

Lückmann M, Shenol A, Nissen TAD, Petersen JE, Kouvchinov D, Schwartz TW, Frimurer TM.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.2c00160

Bibliografisk träff 2022-10-31

Discovery of a structurally novel, potent, and once-weekly free fatty acid receptor 1 agonist for the treatment of diabetes.

Wang B, Cai Z, Yao H, Jiao S, Chen S, Yang Z, Huang W, Ren Q, Cao Z, Chen Y, Zhang L, Li Z.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2022.114883

Bibliografisk träff 2022-09-15

Inhibiting Sodium Taurocholate Cotransporting Polypeptide in HBV-Related Diseases: From Biological Function to Therapeutic Potential.

Chen S, Zhang L, Chen Y, Fu L.

J Med Chem · research support, non-u.s. gov't; review; journal article · DOI 10.1021/acs.jmedchem.2c01097

Bibliografisk träff 2021-12-21

Discovery of new and highly effective quadruple FFA1 and PPARα/γ/δ agonists as potential anti-fatty liver agents.

Zhou Z, Ren Q, Jiao S, Cai Z, Geng X, Deng L, Wang B, Hu L, Zhang L, Yang Y, Li Z.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2021.114061

Bibliografisk träff 2021-09-01

Discovery and development of CPL207280 as new GPR40/FFA1 agonist.

Mach M, Bazydło-Guzenda K, Buda P, Matłoka M, Dzida R, Stelmach F, Gałązka K, Wąsińska-Kałwa M, Smuga D, Hołowińska D, Dawid U, Gurba-Bryśkiewicz L, Wiśniewski K, Dubiel K, Pieczykolan J, Wieczorek M.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2021.113810

Bibliografisk träff 2021-03-23

FFAR1/GPR40: One target, different binding sites, many agonists, no drugs, but a continuous and unprofitable tug-of-war between ligand lipophilicity, activity, and toxicity.

Governa P, Caroleo MC, Carullo G, Aiello F, Cione E, Manetti F.

Bioorg Med Chem Lett · review; journal article · DOI 10.1016/j.bmcl.2021.127969

Bibliografisk träff 2020-10-28

Synthesis and evaluation of 3-(4-(phenoxymethyl)phenyl)propanoic acid and N-phenylbenzenesulfonamide derivatives as FFA4 agonists.

Xu F, Zhao Y, Zhou H, Li C, Zhang X, Hou T, Qu L, Wei L, Wang J, Liu Y, Liang X.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2020.127650

Bibliografisk träff 2020-09-09

Design and Identification of a GPR40 Full Agonist (<b>SCO-267</b>) Possessing a 2-Carbamoylphenyl Piperidine Moiety.

Furukawa H, Miyamoto Y, Hirata Y, Watanabe K, Hitomi Y, Yoshitomi Y, Aida J, Noguchi N, Takakura N, Takami K, Miwatashi S, Hirozane Y, Hamada T, Ito R, Ookawara M, Moritoh Y, Watanabe M, Maekawa T.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.0c00843

Bibliografisk träff 2020-06-02

Discovery of novel potent GPR40 agonists containing imidazo[1,2-a]pyridine core as antidiabetic agents.

Ye Z, Liu C, Zou F, Cai Y, Chen B, Zou Y, Mo J, Han T, Huang W, Qiu Q, Qian H.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2020.115574

Bibliografisk träff 2019-08-14

Design, synthesis and biological evaluation of benzamide derivatives as novel NTCP inhibitors that induce apoptosis in HepG2 cells.

Zhao S, Zhen Y, Fu L, Gao F, Zhou X, Huang S, Zhang L.

Bioorg Med Chem Lett · research support, non-u.s. gov't; evaluation study; journal article · DOI 10.1016/j.bmcl.2019.126623

Bibliografisk träff 2019-07-01

Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold.

Li Z, Liu C, Yang J, Zhou J, Ye Z, Feng D, Yue N, Tong J, Huang W, Qian H.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2019.06.087

Bibliografisk träff 2019-05-02

Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.

Pio B, Chobanian HR, Guo Y, Josien H, Hagmann WK, Miller M, Trujillo ME, Kirkland M, Kosinski D, Mane J, Pachanski M, Cheewatrakoolpong B, Ashley E, Orr R, Wright MJ, Bugianesi R, Souza S, Zhang X, Di Salvo J, Weinglass AB, Tschirret-Guth R, Samuel K, Chen Q, Shang J, Lamca J, Ehrhart J, Nargund R, Howard AD, Colletti SL.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2019.04.050

Bibliografisk träff 2019-01-17

Synthesis and biological evaluation of novel potent FFA1 agonists containing 2,3-dihydrobenzo[b][1,4]dioxine.

Kong D, Guo S, Yang Y, Guo B, Xie X, Hu W.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2019.01.014

Bibliografisk träff 2018-12-27

Discovery of first-in-class thiazole-based dual FFA1/PPARδ agonists as potential anti-diabetic agents.

Li Z, Chen Y, Zhou Z, Deng L, Xu Y, Hu L, Liu B, Zhang L.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2018.12.069

Bibliografisk träff 2018-12-03

Discovery of a GPR40 Superagonist: The Impact of Aryl Propionic Acid α-Fluorination.

Huang H, Meegalla SK, Lanter JC, Winters MP, Zhao S, Littrell J, Qi J, Rady B, Lee PS, Liu J, Martin T, Lam WW, Xu F, Lim HK, Wilde T, Silva J, Otieno M, Pocai A, Player MR.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.8b00444

Bibliografisk träff 2018-10-22

Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.

Guo B, Guo S, Huang J, Li J, Li J, Chen Q, Zhou X, Xie X, Yang Y.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2018.10.019

Bibliografisk träff 2018-10-01

Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.

Li Z, Zhou Z, Deng F, Li Y, Zhang D, Zhang L.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2018.09.071

Bibliografisk träff 2018-08-31

Design, synthesis, and biological evaluations of phenylpropiolic acid derivatives as novel GPR40 agonists.

Jiang XW, Jiang BE, Liu H, Liu ZT, Hu LL, Liu M, Lu W, Zhang HK.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2018.08.075

Bibliografisk träff 2018-08-02

Design, synthesis and biological evaluation of a series of novel GPR40 agonists containing nitrogen heterocyclic rings.

Sun Z, Zhou T, Pan X, Yang Y, Huan Y, Xiao Z, Shen Z, Liu Z.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2018.07.048

Bibliografisk träff 2018-07-31

Nitric oxide donor-based FFA1 agonists: Design, synthesis and biological evaluation as potential anti-diabetic and anti-thrombotic agents.

Li Z, Xu X, Liu R, Deng F, Zeng X, Zhang L.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2018.07.050

Bibliografisk träff 2018-01-12

Discovery of a novel potent GPR40 full agonist.

Meegalla SK, Huang H, Martin T, Xu J, Zhao S, Liu J, Hall M, Gunnet J, Wang Y, Rady B, Silva J, Otieno M, Arnoult E, Paul Lee S, Pocai A, Player MR.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2018.01.013

Bibliografisk träff 2017-12-24

Identification of highly potent and orally available free fatty acid receptor 1 agonists bearing isoxazole scaffold.

Li Z, Liu C, Shi W, Cai X, Dai Y, Liao C, Huang W, Qian H.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2017.12.030

Bibliografisk träff 2017-12-12

Discovery of novel benzo[b]thiophene tetrazoles as non-carboxylate GPR40 agonists.

Huang H, Winters MP, Meegalla SK, Arnoult E, Paul Lee S, Zhao S, Martin T, Rady B, Liu J, Towers M, Otieno M, Xu F, Lim HK, Silva J, Pocai A, Player MR.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2017.12.022

Bibliografisk träff 2017-11-21

SAR Studies of Indole-5-propanoic Acid Derivatives To Develop Novel GPR40 Agonists.

Yoon DO, Zhao X, Son D, Han JT, Yun J, Shin D, Park HJ.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.7b00460

Bibliografisk träff 2017-10-31

Improving metabolic stability with deuterium: The discovery of GPU-028, a potent free fatty acid receptor 4 agonists.

Li Z, Xu X, Li G, Fu X, Liu Y, Feng Y, Wang M, Ouyang Y, Han J.

Bioorg Med Chem · journal article · DOI 10.1016/j.bmc.2017.10.040

Bibliografisk träff 2017-03-17

Discovery of Potent and Orally Bioavailable GPR40 Full Agonists Bearing Thiophen-2-ylpropanoic Acid Scaffold.

Li H, Huang Q, Chen C, Xu B, Wang HY, Long YQ.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.6b01357

Bibliografisk träff 2017-03-02

Design, synthesis and structure-activity relationship studies of novel free fatty acid receptor 1 agonists bearing amide linker.

Yang J, Li Z, Li H, Liu C, Wang N, Shi W, Liao C, Cai X, Huang W, Qian H.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2017.03.001

Bibliografisk träff 2017-01-23

Design and Synthesis of Novel, Selective GPR40 AgoPAMs.

Plummer CW, Clements MJ, Chen H, Rajagopalan M, Josien H, Hagmann WK, Miller M, Trujillo ME, Kirkland M, Kosinski D, Mane J, Pachanski M, Cheewatrakoolpong B, Nolting AF, Orr R, Christensen M, Campeau LC, Wright MJ, Bugianesi R, Souza S, Zhang X, Di Salvo J, Weinglass AB, Tschirret-Guth R, Nargund R, Howard AD, Colletti SL.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.6b00443