38700-15-1Relevant academic research and scientific papers
SYNTHESIS OF CAROTENOID ANALOGUES HAVING PYRIDINE, FURAN, AND TIOPHENE RINGS AS TERMINAL GROUPS
Brahmana, Hemat R.,Katsuyama, Kazuki,Inanaga, Junji,Katsuki, Tsutomi,Yamaguchi, Masaru
, p. 1695 - 1696 (1981)
Heteroaromatic carotenoid analogues having 2-pyridyl, 3-pyridyl, 2-furyl, 3-furyl, 2-thienyl, and 3-thienyl groups at both the ends of tetramethyloctadecanonaene chain, were synthesized and their spectral properties were examined.
Wittig reaction on calixarene upper rim. Access to conjugated bipyridyl and pyridyl podands
Regnouf-de-Vains, Jean-Bernard,Lamartine, Roger
, p. 6311 - 6314 (1996)
Monoformyl-tris-(p-Bu(t)calix[4]arene was synthesised and reacted in smooth conditions with phosphonium salts of 6-bromomethyl-6'-methyl-2,2'-bipyridine and 2-chloromethyl-pyridine, affording the corresponding conjugated mono-armed macrocycles.
Cascade 8πElectrocyclization/Benzannulation to Access Highly Substituted Phenylpyridines
Du, Luan,Gong, Yiliang,Han, Jingpeng,Li, Baosheng,Li, You,Luo, Han,Tian, Yi,Xin, Xiaolan
supporting information, p. 7966 - 7971 (2021/10/25)
A cascade 8πelectrocyclization/benzannulation reaction was developed to obtain the synthetically important highly substituted phenyl-pyridines. This method shows great potential in the rapid and inexpensive application of the scalable and operationally simple production of accessible substrates. On the basis of the resulting phenyl-pyridine products, a new Ru catalyst and bidentate ligand were designed and prepared, further demonstrating its high practicability.
Borane-Catalyzed Chemoselective and Enantioselective Reduction of 2-Vinyl-Substituted Pyridines
Hu, Chen-Yu,Li, Xiang,Liang, Xin-Shen,Liu, Ning,Tian, Jun-Jie,Tu, Xian-Shuang,Wang, Xiao-Chen,Yang, Zhao-Ying
supporting information, p. 18452 - 18456 (2020/08/21)
Herein, we report that highly chemoselective and enantioselective reduction of 2-vinyl-substituted pyridines has been achieved for the first time. The reaction, which uses chiral spiro-bicyclic bisboranes as catalysts and HBpin and an acidic amide as reducing reagents, proceeds through a cascade process involving 1,4-hydroboration followed by transfer hydrogenation of a dihydropyridine intermediate. The retained double bond in the reduction products permits their conversion to natural products and other useful heterocyclic compounds by simple transformations.
NOVEL HYDRAZIDE CONTAINING COMPOUNDS AS BTK INHIBITORS
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Page/Page column 55, (2018/02/03)
The present invention relates to novel hydrazide containing compounds as Bruton tyrosine kinase inhibitors, process of preparation thereof, and to the use of the compounds in the preparation of pharmaceutical compositions for the therapeutic treatment of disorders involving mediation of Bruton tyrosine kinase in humans.
PROSTAGLANDIN D SYNTHASE INHIBITORY PIPERIDINE COMPOUNDS
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Paragraph 0147; 0148, (2013/07/05)
The present invention provides a piperidine compound represented by Formula (I) (wherein X1, X2, X2, A, B and N are as defined in the Description); or a salt thereof.
INDENE DERIVATIVES AS PHARMACEUTICAL AGENTS
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Page 137-138, (2008/06/13)
Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5 and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
A series of non-quinoline cysLT1 receptor antagonists: SAR study on pyridyl analogs of Singulair
Guay, Daniel,Gauthier,Dufresne,Jones,McAuliffe,McFarlane,Metters,Prasit,Rochette,Roy,Sawyer,Zamboni
, p. 453 - 458 (2007/10/03)
The structure-activity relationship of a series of styrylpyridine analogs of MK-0476 (montelukast, Singular) is described. This work has led to the identification of a number of potent and orally active cysLT1 receptor (LTD4 receptor) antagonists including 2ab (L-733,321) as an optimized candidate.
7-alkylidenecephalosporin esters as inhibitors of human leukocyte elastase
Buynak, John D.,Srinivasa Rao,Ford, George P.,Carver, Christa,Adam, Greg,Geng, Bolin,Bachmann, Brian,Shobassy, Samir,Lackey, Stephanie
, p. 3423 - 3433 (2007/10/03)
A series of 7-alkylidenecephalosporins and 7-vinylidenecephalosporins, as their benzhydryl esters, have been tested as inhibitors of both porcine pancreatic elastase and human leukocyte elastase. Selected 7- alkylidenecephalosporin esters are found to be potent inhibitors of HLE. One category of new inhibitors is the 7-(haloalkylidene)cephalosporins. In contrast to previously reported cephalosporin-based elastase inhibitors, these haloalkylidene cephems show optimum inhibitory activity as sulfides, rather than as sulfones. They are efficient and irreversible inhibitors. A second class of active compounds is represented by the benzhydryl ester 7- (cyanomethylidene)cephalosporin sulfone. In contrast to the activity of these new inhibitors, the benzhydryl ester of the mechanism-based β-lactamase inhibitor, 7-[(2'-pyridyl)methylidene]-cephalosporin sulfone showed little inhibitory activity as an elastase inhibitor. 7-Vinylidenecephalosporins were also relatively poor inhibitors, although the terminally unsubstituted allene sulfide showed activity as an inhibitor of PPE. A modeling analysis suggests the 7-alkylidene substituents can be readily accommodated in the S1 pocket. A potential mechanism of inhibition is proposed.
Synthesis and biological activity of 7-alkylidenecephems
Buynak,Wu,Bachmann,Khasnis,Hua,Nguyen,Carver
, p. 1022 - 1034 (2007/10/02)
Several 7-alkylidenecephalosporins were synthesized and biologically evaluated as β-lactamase inhibitors. The three β-lactamase enzymes used in this study included two type C β-lactamases, derived from Enterobacter cloacae P99 and E. cloacae SC12368, and one type A β-lactamase, derived from Escherichia coli WC3310. Of the cephalosporins prepared, compound 7e, the sodium salt of 7-[(Z)-(2'-pyridyl)methylene]cephalosporanic acid sulfone, was found to have excellent inhibitory properties against both type C enzymes. Also, compound 7f, the sodium salt of 7-[(Z)-(tert- butoxycarbonyl)methylene]cephalosporanic acid sulfone showed high activity as an inhibitor of the type A enzyme. The inhibition kinetics of 7e were further explored. The IC50 value of 7e indicated that this compound was approximately 20-fold more active than tazobactam against the enzyme derived from E. cloacae P99 and 167-fold more active than tazobactam against the enzyme derived from E. cloacae SC12368. A plot of enzymatic activity vs incubation time with stoichiometric amounts of inhibitor reveals a rapid deactivation of the enzyme followed by an extremely slow reactivation. 7e exhibited a second-order rate constant of k3' = 5.3 x 106 L/mol · min, and a partition ratio of approximately 20:1 inhibitor:enzyme was determined for this inhibitor. After separation of excess inhibitor with Sephadex filtration, a rate constant of enzyme reactivation was measured at k(reactiv) = 1.0 x 10-3 s-1. Following 24 h of incubation of enzyme with a large excess of inhibitor and sephadex filtration to remove excess inhibitor, the enzyme was able to recover only 43% of its original activity, indicating an irreversible component to the inhibition. Potential mechanisms of inhibition for both 7e and 7f are suggested.
