29270-33-5Relevant academic research and scientific papers
Synthesis of di-, tri-, and tetrasubstituted pyridines from (phenylthio)carboxylic acids and 2-[aryl(tosylimino)methyl]acrylates
Stark, Daniel G.,O'Riordan, Timothy J. C.,Smith, Andrew D.
supporting information, p. 6496 - 6499 (2015/02/05)
An isothiourea-catalyzed Michael addition-lactamization followed by the sulfide oxidation-elimination/N- to O-sulfonyl transfer sequence for the formation of 2,3,5- and 2,3-substituted pyridine 6-tosylates from (phenylthio)acetic acids and α,β-unsaturated
Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11β-hydroxysteroid dehydrogenase type 1 inhibitors: Reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model
Fotsch, Christopher,Bartberger, Michael D.,Bercot, Eric A.,Chen, Michelle,Cupples, Rod,Emery, Maury,Fretland, Jenne,Guram, Anil,Hale, Clarence,Han, Nianhe,Hickman, Dean,Hungate, Randall W.,Hayashi, Michael,Komorowski, Renee,Liu, Qingyian,Matsumoto, Guy,St. Jean Jr., David J.,Ursu, Stefania,Véniant, Murielle,Xu, Guifen,Ye, Qiuping,Yuan, Chester,Zhang, Jiandong,Zhang, Xiping,Tu, Hua,Wang, Minghan
experimental part, p. 7953 - 7967 (2009/12/07)
A series of compounds containing the 2-amino-1,3-thiazol-4(5H)-one core were found to be potent inhibitors of the enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). One of our lead compounds from this series activated the human nuclear xenobiotic
Anti-viral compounds
-
, (2008/06/13)
The present invention relates to compounds of Formula (I) below, which inhibit the growth of picornaviruses, Hepatitus viruses, enteroviruses, cardioviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus. wherein: A is phenyl, pyridyl, substituted phenyl, substituted pyridyl, or benzyl; R is hydrogen, COR4, or COCF3; X is N—OH, O, or CHR1; R1is hydrogen, halo, CN, C1-C4alkyl, —C≡CH, CO(C1-C4alkyl), CO2(C1-C4alkyl), or CONR2R3; R2and R3are independently hydrogen or C1-C4alkyl; A′ is hydrogen, halo, C1-C6alkyl, benzyl, naphthyl, thienyl, furyl, pyridyl, pyrollyl, COR4, S(O)nR4, or a group of the formula R4is C1-C6alkyl, phenyl, or substituted phenyl; n is 0, 1, or 2; R5is independently at each occurrence hydrogen or halo; m is 1, 2, 3, or 4; and R6is hydrogen, halo, CF3, OH, CO2H, NH2, NO2, CONHOCH3, C1-C4alkyl, or CO2(C1-C4alkyl), C1-C4alkoxy; or a pharmaceutically acceptable salt thereof.
Quinolinecarboxylic Acids. 3. Synthesis and Antibacterial Evaluation of 2-Substituted-7-oxo-2,3-dihydro-7H-pyridobenzothiazine-6-carboxylic Acids Related to Rufloxacin
Cecchetti, Violetta,Fravolini, Arnaldo,Pagella, Pier Giuseppe,Savino, Angela,Tabarrini, Oriana
, p. 3449 - 3454 (2007/10/02)
A series of 2-substituted-7-oxo-2,3-dihydro-7H-pyridobenzothiazine-6-carboxylic acids has been prepared and evaluated for in vitro antibacterial activity.These derivatives were less active than corresponding desmethylated analogues.Among th
Synthesis and Antineoplastic Activity of Bisoxy>methyl>-Substituted 3-Pyrrolines as Prodrugs of Tumor Inhibitory Pyrrole Bis(carbamates)
Anderson, Wayne K.,Milowsky, Arnold S.
, p. 2241 - 2249 (2007/10/02)
A series of bispyrrolines 2-4 were synthesized from either the appropriate α-silylated iminium salt, or an aziridine, or a 2H-azirine in a sequence involving 1,3-dipolar cycloaddition reactions.The antineoplastic activities of the pyrrolines were compared to the corresponding pyrroles.The C-2 gem-dimethyl-substituted pyrroline, 4, which cannot be converted to the pyrrole in vivo, was inactive.The activity of the 2-phenyl-substituted pyrrolines 3 was markedly dependent on the nature of the phenyl substituent, although the correspondingphenylpyrroles all showed comparable activity.The differences in the activities of the pyrrolines 3 may be due to the rate of metabolic conversion of the pyrroline to the pyrrole.Electron-withdrawing substituents on the phenyl ring appear to retard this process.
