413606-58-3Relevant academic research and scientific papers
Design, synthesis, characterization and biological evaluation of Thieno[2,3?b]pyridines?chitosan nanocomposites as drug delivery systems for colon targeting
Elghanam, Amal E.,Elsiginy, Samia M.,Khodair, Ahmed I.,Mansour, Hanaa
, (2020)
Thieno[2,3?b]pyridine derivatives DATPa?c have been synthesized based on Thorpe?Ziegler Cyclization. The reaction of arylidene malononitrile derivatives (Ia?c) with thiocyanoacetamide (II) in basic medium (piperidine) followed by alkylation using ethyl chloroacetate and finally, cyclization in sodium ethoxide yielded DATPa?c. Thieno[2,3?b]pyridine?chitosan nanocomposites CS?DATPa?c were prepared from the DATPa?c and CS nanoparticles using sodium tripolyphosphate (TPP). CS?DATPa?c nanocomposites were characterized using FTIR, TEM and XRD techniques and showed a relatively narrow size distribution of monodispersed nanoparticles with the average size of 14–78 nm. The in vitro release studies of CS?DAΤPa?c nanocomposites were investigated and showed that the drug release rate is pH-dependent and the trend is as follows: basic > neutral > acidic. The faster release rate in basic medium effectively prolongs drug delivery in gastric pH. Additionally, the antibacterial investigation showed that DATPa?c and CS?DATPa?c nanocomposites exhibited antibacterial activity against both Gram-positive and Gram-negative bacteria but CS?DATPa?c nanocomposites showed much higher antibacterial activity compared to the DATPa?c, which in agreement with the particle size measurements as DATPa?c are in the bulky structure whereas, CS?DATPa?c are in the nanostructure. The results may have applications of drug design for colon targeting.
Synthesis of Novel Fused Heterocycles Based on 6-Amino-4-phenyl-2-thioxo-1,2-dihydropyridine-3,5-dicarbonitrile
Abdel-Ghany,El-Sayed,Amer,Ahmed
, p. 2013 - 2019 (2016/11/23)
Under phase transfer catalysis conditions, 6-amino-4-phenyl-2-thioxo-1,2-dihydropyridine-3,5-dicarbonitrile (1) was allowed to react with halo compounds, acrylonitrile, chloroacetyl chloride, ethyl cyanoacetate, formamide, triethylorthoformate, or formic acid to give new derivatives of fused pyridines 2–22, respectively. Acetylation of compound 1 using acetic anhydride afforded product 23, which in turn underwent intramolecular cyclization in pyridine to give the corresponding pyrido[2,3-d]pyrimidine 24.
PYRIDOTHIOPHENE COMPOUNDS
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Page/Page column 16, (2008/06/13)
The use of compounds of formula (I) in therapy, particularly for the treatment of a disorder mediated by excessive or inappropriate HSP90 activity formula (I), wherein R2 is a group of formula (IA): -(Arl)m-(Alkl)p-(Z)r-(Alk2)S-Q (IA) Arl,Alk1, Z, Alk2 and Q being as defined in the specification; m, p, r and s are independently 0 or 1; R3 is hydrogen, an optional substituent, or an optionally substituted (Cl-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group; or a salt, N-oxide, hydrate, or solvate thereof.
