392691-83-7Relevant academic research and scientific papers
Human β3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides
Naylor, Elizabeth M.,Parmee, Emma R.,Colandrea, Vincent J.,Perkins, Leroy,Brockunier, Linda,Candelore, Mari R.,Cascieri, Margaret A.,Colwell Jr., Lawrence F.,Deng, Liping,Feeney, William P.,Forrest, Michael J.,Hom, Gary J.,MacIntyre, D. Euan,Strader, Catherine D.,Tota, Laurie,Wang, Pei-Ran,Wyvratt, Matthew J.,Fisher, Michael H.,Weber, Ann E.
, p. 755 - 758 (1999)
The cyclopentylpropylimidazolidinone L-766,892 is a potent β3 AR agonist (EC50 5.7 nM, 64% activation) with 420- and 130-fold selectivity over binding to the β1 and β2 ARs, respectively. In anesthetized rhesus monkeys, L-766,892 elicited dose-dependent hyperglycerolemia (ED50 0.1 mg/kg) with minimal effects on heart rate.
Activation of Phenyl 4-(2-Oxo-3-Alkylimidazolidin-1-yl)benzenesulfonates Prodrugs by CYP1A1 as New Antimitotics Targeting Breast Cancer Cells
Fortin, Sébastien,Charest-Morin, Xavier,Turcotte, Vanessa,Lauvaux, Coraline,Lacroix, Jacques,C?té, Marie-France,Gobeil, Stéphane,Gaudreault, René C.
, p. 4963 - 4982 (2017/06/28)
Prodrug-mediated utilization of the cytochrome P450 (CYP) 1A1 to obtain the selective release of potent anticancer products within cancer tissues is a promising approach in chemotherapy. We herein report the rationale, preparation, biological evaluation, and mechanism of action of phenyl 4-(2-oxo-3-Alkylimidazolidin-1-yl)benzenesulfonates (PAIB-SOs) that are antimicrotubule prodrugs activated by CYP1A1. Although PAIB-SOs are inert in most cells tested, they are highly cytocidal toward several human breast cancer cells, including hormone-independent and chemoresistant types. PAIB-SOs are N-dealkylated into cytotoxic phenyl 4-(2-oxo-3-imidazolidin-1-yl)benzenesulfonates (PIB-SOs) in CYP1A1-positive cancer cells, both in vitro and in vivo. In conclusion, PAIB-SOs are novel chemotherapeutic prodrugs with no equivalent among current antineoplastics and whose selective action toward breast cancer is tailored to the characteristic pattern of CYP1A1 expression observed in a large percentage of human breast tumors.
SUBSTITUTED 2-IMIDAZOLIDONES AND ANALOGS
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Page/Page column 28; 107, (2011/09/19)
Compounds of formula (I): wherein R1, R2, R3, R4, R7, R6, R7, R8, R9, A, X and Y as defined herein are provided as useful for the treatment of cancer or for
Substituted 2- (S) -hydroxy-3- (piperidin-4-yl-methylamino) -propyl ethers and substituted 2-aryl-2- (R) - hydroxy-1- (piperidin-4-yl-methyl) -ethylamine beta-3 adrenergic receptor agonists
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, (2008/06/13)
This invention provides compounds of Formula I having the structure wherein A, B, Z, R and R1 are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.
