17452-79-8Relevant academic research and scientific papers
COMPOSITIONS AND METHODS FOR CONTROL OF DISEASE
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Paragraph 0317; 0351, (2018/08/30)
Compounds, compositions and methods for controlling root-originating diseases are described herein. The compounds include oxazoles, oxadiazoles and thiadiazoles. The compounds may be administered to plants, seeds, and/or soil.
Discovery of an Isothiazole-Based Phenylpropanoic Acid GPR120 Agonist as a Development Candidate for Type 2 Diabetes
Zhang, Xuqing,Cai, Chaozhong,Sui, Zhihua,Macielag, Mark,Wang, Yuanping,Yan, Wen,Suckow, Arthur,Hua, Hong,Bell, Austin,Haug, Peter,Clapper, Wilma,Jenkinson, Celia,Gunnet, Joseph,Leonard, James,Murray, William V.
supporting information, p. 947 - 952 (2017/09/22)
We have discovered a novel series of isothiazole-based phenylpropanoic acids as GPR120 agonists. Extensive structure-activity relationship studies led to the discovery of a potent GPR120 agonist 4x, which displayed good EC50 values in both calcium and β-arrestin assays. It also presented good pharmaceutical properties and a favorable PK profile. Moreover, it demonstrated in vivo antidiabetic activity in C57BL/6 DIO mice. Studies in WT and knockout DIO mice showed that it improved glucose handling during an OGTT via GPR120. Overall, 4x possessed promising antidiabetic effect and good safety profile to be a development candidate.
Synthesis of spiroindene-1,3-dione isothiazolines via a cascade michael/1,3-dipolar cycloaddition reaction of 1,3,4-oxathiazol-2-one and 2-arylidene-1,3-indandiones
Aitha, Anjaiah,Yennam, Satyanarayana,Behera, Manoranjan,Anireddy, Jaya Shree
supporting information, p. 578 - 581 (2017/01/17)
The reaction of 1,3,4-oxathiazol-2-one derivative with 2-arylidene-1,3-indandione to furnish novel spiroindene-1,3-dione isothiazoline derivatives by Michael/1,3-dipolar [3+2]-cycloaddition reaction was investigated. The key 1,3-dipolar cycloaddition reaction step was examined in toluene solvent at reflux temperature to obtain mixture of two regioisomers (6a and 6b – 14a and 14b) and single isomers (15–20). The scope of this new reaction was demonstrated with many examples with high reactivity and yields.
SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUNDS USEFUL AS GPR120 AGONISTS
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Page/Page column 49, (2017/12/29)
The present invention relates to a compound represented by formula (I) and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, NASH, inflammation related disorders, and related di
COMPOSITIONS AND METHODS FOR IMPROVING AGRONOMIC CHARACTERISTICS OF PLANTS
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Paragraph 0439, (2016/07/05)
Compounds, compositions and methods for improving one or more agronomic characteristics of desired crop plants are described herein. The compounds include oxazoles, oxadiazoles and thiadiazoles.
Isothiazole derivatives as GPR120 agonists for the treatment of type II diabetes
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Page/Page column 28, (2015/07/07)
Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) as follows: wherein R1, G, and Q are defined herein.
ISOTHIAZOLE DERIVATIVES AS GPR120 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES
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Page/Page column 37-38, (2015/11/02)
Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) as follows: wherein R1, G, and Q are defined herein.
GPR120 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES
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Paragraph 0620; 0621, (2014/09/30)
Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, G, and Q are defined herein; and wherein R11, R21, R41, RB1 and G1, are defined herein.
3H-1,2,4-Dithiazol-3-one compounds as novel potential affordable antitubercular agents
Yang, Jianzhong,Pi, Weiyi,Xiong, Li,Ang, Wei,Yang, Tao,He, Jun,Liu, Yuanyuan,Chang, Ying,Ye, Weiwei,Wang, Zhenling,Luo, Youfu,Wei, Yuquan
, p. 1424 - 1427 (2013/03/14)
Small molecules with oxathiazol-2-one moiety were recently reported as potent inhibitors of Mycobacterium bovis var. bacilli Calmette-Guérin (BCG), among which HT1171 was the most potent and selective proteasome inhibitor. Herein we synthesized a series of novel compounds by bioisosteric replacement of the oxathiazol-2-one ring with 3H-1,2,4-dithiazol-3-one, and also fifteen 1,3,4-oxathiazol-2-one molecules in order for potency comparison and structure-activity relationship elucidation since their antibacterial effects on the virulent strains were not evaluated before. All the compounds were assessed for antitubercular activities on the virulent H37Rv strain by a serial dilution method. Among the tested compounds, 3H-1,2,4-dithiazol-3-one compound 4n was found to be the most active with a lowest MIC90 value of 1 μg/mL. Furthermore, the cytotoxicities of all the compounds against normal human liver cell line L02 were determined by an MTT method. Compound 4n displayed a lower inhibitory ratio than HT1171 at the concentration of 100 μM, indicating its better safety profile.
MICROBICIDES
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Page/Page column 48-49, (2012/02/05)
The present invention relates to a compound of formula (I): wherein the substituents have the definitions as defined in claim 1 or a salt or a N-oxide thereof, their use and methods for the control and/or prevention of microbial infection, particularly fu
