135432-77-8Relevant articles and documents
Identification of BR102910 as a selective fibroblast activation protein (FAP) inhibitor
Jung, Hui Jin,Nam, Eun Hye,Park, Jin Young,Ghosh, Prithwish,Kim, In Su
supporting information, (2021/02/26)
Fibroblast activation protein (FAP) belongs to the family of prolyl-specific serine proteases and displays both exopeptidase and endopeptidase activities. FAP expression is undetectable in most normal adult tissues, but is greatly upregulated in sites of tissue remodeling, which include fibrosis, inflammation and cancer. Due to its restricted expression pattern and dual enzymatic activities, FAP inhibition is investigated as a therapeutic option for several diseases. In the present study, we described the structure–activity relationship of several synthesized compounds against DPPIV and prolyl oligopeptidase (PREP). In particular, BR102910 (compound 24) showed nanomolar potency and high selectivity. Moreover, the in vivo FAP inhibition study of BR102910 (compound 24) using C57BL/6J mice demonstrated exceptional profiles and satisfactory FAP inhibition efficacy. Based on excellent in vitro and in vivo profiles, the potential of BR102910 (compound 24) as a lead candidate for the treatment of type 2 diabetes is considered.
A chiral picolinic acid ligand, Cl-NAPH-PyCOOH, for CPRU-catalyzed dehydrative allylation: Design, synthesis, and properties
Tanaka, Shinji,Suzuki, Yusuke,Kimura, Takahiro,Kitamura, Masato
, p. 1707 - 1720 (2019/10/01)
A CpRu/Br?nsted acid-combined catalyst, CpRu(II)/pico-linic acid (PyCOOH), acts as an efficient catalyst for the allyl protection/deprotection of alcohols. This discovery has resulted in the development of a new axially chiral ligand, Cl-Naph-PyCOOH (2a;
Design, Synthesis, and Evaluation of Novel Auxin Mimic Herbicides
Do-Thanh, Chi-Linh,Vargas, Jose J.,Thomas, Joseph W.,Armel, Gregory R.,Best, Michael D.
, p. 3533 - 3537 (2016/06/01)
Due to the key roles of auxins as master regulators of plant growth, there is considerable interest in the development of compounds with auxin-like properties for growth management and weed control applications. Herein, we describe the design and multiste
EP2 RECEPTOR AGONISTS
-
Page/Page column 193, (2008/06/13)
A compound of Formula (I) or a salt, solvate and chemically protected form thereof, wherein: R5 is an optionally substituted C5-20 aryl or C4-20 alkyl group; A is selected from the group consisting of Formulae (Ai), (Aii), (Aiii) D is selected from Formulae (Di), (Dii), (Diii), (Div), (Dv) B is selected from the group consisting of Formulae (Bi), (Bii), (Biii), (Biv) (Bv).