- 3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists
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The design, synthesis, and structure-activity relationship (SAR) for a series of β-substituted 3-(4-aryloxyaryl)propanoic acid GPR40 agonists is described. Systematic replacement of the pendant aryloxy group led to identification of potent GPR40 agonists. In order to identify candidates suitable for in vivo validation of the target, serum shifted potency and pharmacokinetic properties were determined for several compounds. Finally, further profiling of compound 7 is presented, including demonstration of enhanced glucose tolerance in an in vivo mouse model.
- Walsh, Shawn P.,Severino, Alexandra,Zhou, Changyou,He, Jiafang,Liang, Gui-Bai,Tan, Carina P.,Cao, Jin,Eiermann, George J.,Xu, Ling,Salituro, Gino,Howard, Andrew D.,Mills, Sander G.,Yang, Lihu
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scheme or table
p. 3390 - 3394
(2011/06/24)
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- Benzisoxazole compounds useful as herbicides
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A herbicidal compound of formula (I): STR1 in which Ar is an optionally substituted aryl or heterocyclic ring system: R1 and R2 are independently selected from H, optionally substituted alkyl, alkenyl or akynyl, halogen, NRa Rb, or R1 and R2 together with the carbon to which they are attached form an optionally substituted alkenyl or cycloalkyl group; R3 is CO2 R4, CN, COR4, CH2 OR4, CH4 (OH)R4, CH(OR4)R5, CH2 OSO6 R4, CH2 OSO6 R4, CH2 ONR6 R7, CSNH2, COSR4, SCOR4, COHNSO2 R4, CONR6 R7, CONHNR6 R7, CONHN+ R6 R7 R8 Y-2, CO2- M+ or COON=CR6 R7 ; M+ is an agriculturally acceptable cation; Y- is an agriculturally acceptable anion; R4, and R5 are independently selected from H or an optionally substituted alkyl, aryl, alkenyl or alkynyl group; R6, R7, R8, R9, Ra and Rb are independently selected from H or an optionally substituted alkyl alkenyl, aryl or akynyl group or any two of R6, R7, R8, R9, Ra and Rb together with the atom to which they are attached form a cycloalkyl or heterocyclic ring; R6 and R7 may also be a heterocyclic ring; W is O or NR10 where R10 is H or lower alkyl; X is (CH2)n, CH=CH, CH(ORc)CH2, COCH2 ; where Rc is H or an optionally substituted alkyl, aryl, alkynyl or alkynyl group; and n is O, 1 or 2.
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- Simple preparation of 4-aryl- and 4-alkyl-2(5H)-furanones from β-substituted crotonic esters
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Treatment of β-aryl- or β-alkylcrotonic esters with selenium dioxide in acetic acid in the presence of a catalytic amount of perchloric acid gave 4-substituted 2(5H)-furanones in moderate to good yields.
- Kagabu,Shimizu,Ito,Moriya
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p. 830 - 832
(2007/10/02)
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