934405-34-2Relevant academic research and scientific papers
Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HT2C Receptor Agonists
Carpenter, Joseph,Wang, Ying,Wu, Gang,Feng, Jianxin,Ye, Xiang-Yang,Morales, Christian L.,Broekema, Matthias,Rossi, Karen A.,Miller, Keith J.,Murphy, Brian J.,Wu, Ginger,Malmstrom, Sarah E.,Azzara, Anthony V.,Sher, Philip M.,Fevig, John M.,Alt, Andrew,Bertekap, Robert L.,Cullen, Mary Jane,Harper, Timothy M.,Foster, Kimberly,Luk, Emily,Xiang, Qian,Grubb, Mary F.,Robl, Jeffrey A.,Wacker, Dean A.
, p. 6166 - 6190 (2017/08/02)
Agonism of the 5-HT2C receptor represents one of the most well-studied and clinically proven mechanisms for pharmacological weight reduction. Selectivity over the closely related 5-HT2A and 5-HT2B receptors is critical as their activation has been shown to lead to undesirable side effects and major safety concerns. In this communication, we report the development of a new screening paradigm that utilizes an active site mutant D134A (D3.32) 5-HT2C receptor to identify atypical agonist structures. We additionally report the discovery and optimization of a novel class of nonbasic heterocyclic amide agonists of 5-HT2C. SAR investigations around the screening hits provided a diverse set of potent agonists at 5-HT2C with high selectivity over the related 5-HT2A and 5-HT2B receptor subtypes. Further optimization through replacement of the amide with a variety of five- and six-membered heterocycles led to the identification of 6-(1-ethyl-3-(quinolin-8-yl)-1H-pyrazol-5-yl)pyridazin-3-amine (69). Oral administration of 69 to rats reduced food intake in an ad libitum feeding model, which could be completely reversed by a selective 5-HT2C antagonist.
Rynaxypyr: A new insecticidal anthranilic diamide that acts as a potent and selective ryanodine receptor activator
Lahm, George P.,Stevenson, Thomas M.,Selby, Thomas P.,Freudenberger, John H.,Cordova, Daniel,Flexner, Lindsey,Bellin, Cheryl A.,Dubas, Christine M.,Smith, Ben K.,Hughes, Kenneth A.,Hollingshaus, J. Gary,Clark, Christopher E.,Benner, Eric A.
, p. 6274 - 6279 (2008/03/14)
Rynaxypyr is a highly potent and selective activator of insect ryanodine receptors with exceptional activity on a broad range of Lepidoptera. A strong correlation between insecticidal activity and ryanodine receptor activation is observed along with selective activity against insect over mammalian receptors. The synthesis and biological results are presented.
HYDRAZIDE COMPOUND AND PESTICIDAL USE OF THE SAME
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Page/Page column 487-488, (2008/06/13)
A hydrazide compound represented by the formula (1): has excellent pesticidal activity.
CYANO ANTHRANILAMIDE INSECTICIDES
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Page 26, (2010/02/07)
This invention provides compounds of Formula (I), N -oxides and suitable salts thereof INSERT FORMULA I HERE wherein R1 is Me, Cl, Br or F; R2 is F, Cl, Br, C1-C4 haloalkyl or C1-C4 haloalkoxy; R3 is F, Cl or Br; R4 is H or C1-C4 alkyl,C3-C4 alkenyl, C3-C4 alkynyl, C3-C5 cycloalkyl, or C4-C6 cycloalkylalkyl, each optionally substituted with one substituent selected from the group consisting of halogen, CN, SMe S(O)Me, S(O)2Me and OMe; R5 is H or Me; R6 is H, F or Cl; and R7 is H, F or Cl. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula (I), anN-oxide thereof or a suitable salt of the compound (e.g., as a composition described herein). This invention also pertains to a composition for controlling an invertebrate pest comprising a biologically effective amount of a compound of Formula (I), an N-oxide thereof or a suitable salt of the compound and at least one additional component selected from the group consisting of a surfactant, a solid diluent and a liquid diluent.
