- Design, synthesis and SAR of a novel series of heterocyclic phenylpropanoic acids as GPR120 agonists
-
A novel series of 5-membered heterocycle-containing phenylpropanoic acid derivatives was discovered as potent GPR120 agonists with low clearance, high oral bioavailability and in vivo antidiabetic activity in rodents.
- Zhang, Xuqing,Cai, Chaozhong,Winters, Michael,Wells, Michele,Wall, Mark,Lanter, James,Sui, Zhihua,Ma, Jingyuan,Novack, Aaron,Nashashibi, Imad,Wang, Yuanping,Yan, Wen,Suckow, Arthur,Hua, Hong,Bell, Austin,Haug, Peter,Clapper, Wilma,Jenkinson, Celia,Gunnet, Joseph,Leonard, James,Murray, William V.
-
p. 3272 - 3278
(2017/07/07)
-
- A field-based disparity analysis of new 1,2,5-oxadiazole derivatives endowed with antiproliferative activity
-
A series of 1,2,5-oxadiazoles were synthesized as new potential antiproliferative agents. The in vitro cytotoxic activity evaluation of title compounds through MTT assay revealed that some of them showed significant activity against the HCT-116 cancer cell line. The field-based disparity analysis provided indications about the electrostatic, hydrophobic, and shape features underlying the cytotoxicity, suggesting that increasing the negative electrostatic field on the heterocyclic core of the structure has positive effects on the activity. The structure–activity relationships (SAR) around a particular compound can be explained allowing for a structural rationale for the differences in activity. The SAR provided by this series of compounds can be exploited to carry out further lead optimization.
- Porta, Federica,Gelain, Arianna,Barlocco, Daniela,Ferri, Nicola,Marchianò, Silvia,Cappello, Valentina,Basile, Livia,Guccione, Salvatore,Meneghetti, Fiorella,Villa, Stefania
-
p. 820 - 839
(2017/10/03)
-
- PROCESS FOR THE PREPARATION OF ISOXAZOLYL- METHOXY NICOTINIC ACIDS
-
The present invention relates to a process for the preparation of a compound of formula (I) wherein R1 and R2 are as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.
- -
-
Paragraph 0230
(2013/05/08)
-
- PROCESS FOR THE PREPARATION OF ISOXAZOLYL-METHOXY-NICOTINIC ACIDS
-
The present invention relates to a process for the preparation of a compound of formula (I) which is useful as an intermediate in the preparation of active pharmaceutical compounds from a compound of formula (IV) wherein R1 and R2 ar
- -
-
Page/Page column 35; 36
(2013/05/09)
-
- Synthesis and Herbicidal Activity of 3-Aryl-5-(haloalkyl)-4-isoxazolecarboxamides and Their Derivatives
-
A series of unique 3-aryl-5-(haloalkyl)-4-isoxazolecarboxamides have been prepared which exhibit, in both greenhouse and field studies, significant preemergent and postemergent herbicidal activity in the grams per hectare range against broadleaf and narro
- Hamper, Bruce C.,Leschinsky, Kindrick L.,Massey, Steven S.,Bell, Crystal L.,Brannigan, Lawrence H.,Prosch, S. Douglas
-
p. 219 - 228
(2007/10/02)
-
- 3-Aryl-4-isothiazolecarboxylic acid and 3-aryl-4-isoxazolecarboxylic acid derivatives and their use as herbicides
-
Carboxylic acid derivatives having the formula STR1 have been found to be effective herbicides. They are especially effective when applied as a pre-emergent herbicide.
- -
-
-
- 3-Aryl-4-isoxazolecarboxylic acids as plant growth regulants
-
3-Aryl-4-isothiazolecarboxylic acids as well as 3-aryl-4-isoxazolecarboxylic acids have been found to be effective plant growth regulants especially when applied to soybean plants.
- -
-
-