Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation

Bioorganic and Medicinal Chemistry Letters

Volumn 8, Issue 20, 1998, Pages 2897-2902

  Sauerberg, Per ^a   Jeppesen, Lone ^a   Olesen, Preben H ^a   Sheardown, Malcolm J ^a   Fink Jensen, Anders ^a   Rasmussen, Thøger ^a   Rimvall, Karin ^a   Shannon, Harlan E ^b   Bymaster, Frank P ^b   DeLapp, Neil W ^b   Calligaro, Dave O ^b   Ward, John S ^b   Whitesitt, Celia A ^b   Thomsen, Christian ^a  

^a NOVO NORDISK A S   (Denmark)

^b ELI LILLY AND COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

6 [3 (3 PHENYL 2 PROPYN 1 YLTHIO) 1,2,5 THIADIAZOL 4 YL]1 AZBICYCLO[3.2.1]OCTANE; MUSCARINIC M1 RECEPTOR AGONIST; UNCLASSIFIED DRUG; XANOMELINE;

ARTICLE; DRUG CONFORMATION; DRUG POTENCY; DRUG RECEPTOR BINDING; HUMAN; RECEPTOR AFFINITY; RECEPTOR UPREGULATION; STRUCTURE ACTIVITY RELATION;

ANIMALS; CELLS, CULTURED; CHO CELLS; CRICETINAE; HUMANS; INHIBITORY CONCENTRATION 50; MUSCARINIC AGONISTS; PYRIDINES; RATS; RECEPTOR, MUSCARINIC M1; RECEPTORS, MUSCARINIC; STRUCTURE-ACTIVITY RELATIONSHIP; THIADIAZOLES; TRANSFECTION;

EID: 0032552847     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(98)00509-5     Document Type: Article

References (12)

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11. 1H-NMR (DMSO) δ: 7.36 (5H, s), 7.4-6.8 (2H, br. s), 4.43 (2H, s), 4.08 (2H, s), 3.86-3.74 (1H, m), 3.15-3.39 (2H, m), 3.30-3.10 (3H, m), 3.09-2.90 (2H, m), 1.75-1.55 (1H, m), 1.20-1.05 (1H, m). Mp 170-172 °C.
12. 1H-NMR (DMSO) δ: 7.50-7.46 (5H, m), 5.32 (2H, s), 3.33 (2H, s), 3.10 (2H, d), 3.03 (2H, d), 2.52 (2H, s). Mp 182-185 °C.