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Items: 22

1.

Oxadiazole Derivatives as Dual Orexin Receptor Antagonists: Synthesis, Structure-Activity Relationships, and Sleep-Promoting Properties in Rats.

Brotschi C, Roch C, Gatfield J, Treiber A, Williams JT, Sifferlen T, Heidmann B, Jenck F, Bolli MH, Boss C.

ChemMedChem. 2019 Jul 3;14(13):1257-1270. doi: 10.1002/cmdc.201900242. Epub 2019 Jun 5.

PMID:
31066976
2.

Cenerimod, a novel selective S1P1 receptor modulator with unique signaling properties.

Piali L, Birker-Robaczewska M, Lescop C, Froidevaux S, Schmitz N, Morrison K, Kohl C, Rey M, Studer R, Vezzali E, Hess P, Clozel M, Steiner B, Bolli MH, Nayler O.

Pharmacol Res Perspect. 2017 Dec;5(6). doi: 10.1002/prp2.370.

3.

The Discovery of Macitentan - A Standard Medicinal Chemistry Program?

Bolli MH.

Chimia (Aarau). 2017 Aug 9;71(7):420-429. doi: 10.2533/chimia.2016.420.

PMID:
28779766
4.

Discovery of Highly Potent Dual Orexin Receptor Antagonists via a Scaffold-Hopping Approach.

Heidmann B, Gatfield J, Roch C, Treiber A, Tortoioli S, Brotschi C, Williams JT, Bolli MH, Abele S, Sifferlen T, Jenck F, Boss C.

ChemMedChem. 2016 Oct 6;11(19):2132-2146. doi: 10.1002/cmdc.201600175. Epub 2016 Jul 8.

PMID:
27390287
5.

From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective.

Boss C, Bolli MH, Gatfield J.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3381-94. doi: 10.1016/j.bmcl.2016.06.014. Epub 2016 Jun 10. Review.

PMID:
27321813
6.

Novel S1P1 receptor agonists - Part 4: Alkylaminomethyl substituted aryl head groups.

Lescop C, Müller C, Mathys B, Birker M, de Kanter R, Kohl C, Hess P, Nayler O, Rey M, Sieber P, Steiner B, Weller T, Bolli MH.

Eur J Med Chem. 2016 Jun 30;116:222-238. doi: 10.1016/j.ejmech.2016.03.048. Epub 2016 Mar 23.

PMID:
27061986
7.

Novel S1P1 receptor agonists - Part 5: From amino-to alkoxy-pyridines.

Bolli MH, Lescop C, Birker M, de Kanter R, Hess P, Kohl C, Nayler O, Rey M, Sieber P, Velker J, Weller T, Steiner B.

Eur J Med Chem. 2016 Jun 10;115:326-41. doi: 10.1016/j.ejmech.2016.03.020. Epub 2016 Mar 12.

PMID:
27027817
8.

The metabolism of the dual endothelin receptor antagonist macitentan in rat and dog.

Treiber A, Miraval T, Bolli MH, Funel JA, Segrestaa J, Seeland S.

Xenobiotica. 2016;46(3):253-67. doi: 10.3109/00498254.2015.1070302. Epub 2015 Sep 4.

PMID:
26337830
9.

Distinct ETA receptor binding mode of macitentan as determined by site directed mutagenesis.

Gatfield J, Mueller Grandjean C, Bur D, Bolli MH, Nayler O.

PLoS One. 2014 Sep 16;9(9):e107809. doi: 10.1371/journal.pone.0107809. eCollection 2014.

10.

Sphingosine-1-phosphate (S1P) displays sustained S1P1 receptor agonism and signaling through S1P lyase-dependent receptor recycling.

Gatfield J, Monnier L, Studer R, Bolli MH, Steiner B, Nayler O.

Cell Signal. 2014 Jul;26(7):1576-88. doi: 10.1016/j.cellsig.2014.03.029. Epub 2014 Apr 2.

PMID:
24704119
11.

Novel S1P(1) receptor agonists--part 3: from thiophenes to pyridines.

Bolli MH, Abele S, Birker M, Bravo R, Bur D, de Kanter R, Kohl C, Grimont J, Hess P, Lescop C, Mathys B, Müller C, Nayler O, Rey M, Scherz M, Schmidt G, Seifert J, Steiner B, Velker J, Weller T.

J Med Chem. 2014 Jan 9;57(1):110-30. doi: 10.1021/jm4014696. Epub 2013 Dec 24.

PMID:
24367923
12.

Novel S1P(1) receptor agonists--part 2: from bicyclo[3.1.0]hexane-fused thiophenes to isobutyl substituted thiophenes.

Bolli MH, Velker J, Müller C, Mathys B, Birker M, Bravo R, Bur D, de Kanter R, Hess P, Kohl C, Lehmann D, Meyer S, Nayler O, Rey M, Scherz M, Steiner B.

J Med Chem. 2014 Jan 9;57(1):78-97. doi: 10.1021/jm401456d. Epub 2013 Dec 17.

PMID:
24345087
13.

Novel S1P1 receptor agonists--part 1: From pyrazoles to thiophenes.

Bolli MH, Müller C, Mathys B, Abele S, Birker M, Bravo R, Bur D, Hess P, Kohl C, Lehmann D, Nayler O, Rey M, Meyer S, Scherz M, Schmidt G, Steiner B, Treiber A, Velker J, Weller T.

J Med Chem. 2013 Dec 12;56(23):9737-55. doi: 10.1021/jm4014373. Epub 2013 Nov 22.

PMID:
24266709
14.

Sphingosine 1-phosphate (S1P) receptor agonists mediate pro-fibrotic responses in normal human lung fibroblasts via S1P2 and S1P3 receptors and Smad-independent signaling.

Sobel K, Menyhart K, Killer N, Renault B, Bauer Y, Studer R, Steiner B, Bolli MH, Nayler O, Gatfield J.

J Biol Chem. 2013 May 24;288(21):14839-51. doi: 10.1074/jbc.M112.426726. Epub 2013 Apr 15.

15.

The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist.

Bolli MH, Boss C, Binkert C, Buchmann S, Bur D, Hess P, Iglarz M, Meyer S, Rein J, Rey M, Treiber A, Clozel M, Fischli W, Weller T.

J Med Chem. 2012 Sep 13;55(17):7849-61. doi: 10.1021/jm3009103. Epub 2012 Aug 16.

PMID:
22862294
16.

The selective sphingosine 1-phosphate receptor 1 agonist ponesimod protects against lymphocyte-mediated tissue inflammation.

Piali L, Froidevaux S, Hess P, Nayler O, Bolli MH, Schlosser E, Kohl C, Steiner B, Clozel M.

J Pharmacol Exp Ther. 2011 May;337(2):547-56. doi: 10.1124/jpet.110.176487. Epub 2011 Feb 23.

PMID:
21345969
17.

Synthetic sphingosine 1-phosphate receptor modulators--opportunities and potential pitfalls.

Bolli MH, Lescop C, Nayler O.

Curr Top Med Chem. 2011;11(6):726-57. Review.

PMID:
21261590
18.

2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.

Bolli MH, Abele S, Binkert C, Bravo R, Buchmann S, Bur D, Gatfield J, Hess P, Kohl C, Mangold C, Mathys B, Menyhart K, Müller C, Nayler O, Scherz M, Schmidt G, Sippel V, Steiner B, Strasser D, Treiber A, Weller T.

J Med Chem. 2010 May 27;53(10):4198-211. doi: 10.1021/jm100181s.

PMID:
20446681
19.

Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist.

Iglarz M, Binkert C, Morrison K, Fischli W, Gatfield J, Treiber A, Weller T, Bolli MH, Boss C, Buchmann S, Capeleto B, Hess P, Qiu C, Clozel M.

J Pharmacol Exp Ther. 2008 Dec;327(3):736-45. doi: 10.1124/jpet.108.142976. Epub 2008 Sep 9.

PMID:
18780830
20.

Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists.

Bolli MH, Marfurt J, Grisostomi C, Boss C, Binkert C, Hess P, Treiber A, Thorin E, Morrison K, Buchmann S, Bur D, Ramuz H, Clozel M, Fischli W, Weller T.

J Med Chem. 2004 May 20;47(11):2776-95.

PMID:
15139756
21.

The use of sulfonylamido pyrimidines incorporating an unsaturated side chain as endothelin receptor antagonists.

Bolli MH, Boss C, Clozel M, Fischli W, Hess P, Weller T.

Bioorg Med Chem Lett. 2003 Mar 10;13(5):955-9.

PMID:
12617929
22.

Bis-sulfonamides as endothelin receptor antagonists.

Boss C, Bolli MH, Weller T, Fischli W, Clozel M.

Bioorg Med Chem Lett. 2003 Mar 10;13(5):951-4.

PMID:
12617928

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