- Potent oxindole based human β3 adrenergic receptor agonists
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The synthesis and biological evaluation of a series of oxindole β3 adrenergic receptor agonists is described. A modulation of rat atrial tachycardia was observed with substitution at the 3-position of the oxindole moiety.
- Stevens, F. Craig,Bloomquist, William E.,Borel, Anthony G.,Cohen, Marlene L.,Droste, Christine A.,Heiman, Mark L.,Kriauciunas, Aidas,Sall, Daniel J.,Tinsley, Frank C.,Jesudason, Cynthia D.
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p. 6270 - 6273
(2008/09/17)
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- Non-nucleoside reverse transcriptase inhibitors
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Compounds represented by formula I: wherein R1 is H, halogen, (C1-4)alkyl, O(C1-4)alkyl, and haloalkyl; R2 is H or (C1-4)alkyl; R3 is H or (C1-4)alkyl; R4 is (C1-4)alkyl, (C1-4)alkyl(C3-7)cycloalkyl, or (C3-7)cycloalkyl; and Q is a fused phenyl-5 or 6-membered saturated heterocycle having one to two heteroatoms selected from O and N, said Q being optionally substituted with hydroxy, or (C1-4)alkyl which in turn maybe optionally substituted with pyridinyl-N-oxide or C(O)OR wherein R is H or (C1-4)alkyl; or a salt thereof. The compounds have inhibitory activity against Wild Type, and single and double mutants strains, of HIV.
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- Novel substituted 4-aminomethylpiperidines as potent and selective human β3-agonists. Part 1: Aryloxypropanolaminomethylpiperidines
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The synthesis and SAR of a series of human β3 adrenoreceptor agonists based on a template derived from a common pharmacophore coupled with 4-aminomethylpiperidine is described. Potent and selective agents were identified such as 26 that was in vitro active in CHO cells expressing human β3-AR (EC50=49 nM, IA=1.1), and in vivo active in a transgenic mouse model.
- Steffan, Robert J.,Ashwell, Mark A.,Solvibile, William R.,Matelan, Edward,Largis, Elwood,Han, Stella,Tillet, Jeffery,Mulvey, Ruth
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p. 2957 - 2961
(2007/10/03)
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