The purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of inflammation and infections in colon)
The purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of inflammation and infections in colon).
Key words: Mutual prodrug, Ester linkage, Azo bond, Colon targeting
A new ligand [N-(acetyl amino) thioxomethyl] valine was prepared from the reaction of acetyl iso thiocyanate with valine. The ligand was characterized by FT-IR, UV- vis and 1HNMR spectrum, The complexes with some metal ions (M +2 =Co,Ni,Cu,Zn,Cd,Hg) have been prepared and characterized. The structural diagnosis were established by IR,UV-Vis spectrum, flame atomic absorption spectroscopy conductivity and magnetic susceptibility ,the complexes showed tetrahedral geometry around the metal l.
Schiff bases of Ceftizoxime sodium were synthesized in an attempt to improve the antimicrobial spectrum of Ceftizoxime. Aminothiazole ring of Ceftizoxime is linked directly through an imino group to different aromatic aldehydes reacted by nucleophilic addition using trimethylamine (TEA), as a catalyst and refluxed in methanol. The antimicrobial activity was evaluated for such Schiff bases using disc diffusion method. Molecular docking was conducted on certain penicillin-binding proteins (PBPs) and carboxypeptidases using 1- click docking software. Schiff bases of Ceftizoxime were prepared with reasonable yields and their chemical structures were confirmed by spectral analysis (FTIR, 1H-NMR) and elemental microanalysis (CHNS). The antibacter
... Show Moren this work, a series of new nucleoside analogues (β-glucose liked to pyrazoline moiety) was synthesized. In the beginning, chalcone [1-3] was formed from the reaction of acetophenone and benzaldehyde derivatives in the presence of sodium hydroxide. Pyrazolines [4-6] were obtained from the reaction of the prepared chalcones and hydrazine hydrate in the presence of ethanol absolute. These pyrazolines were treated with β-glucose pentaacetate to afford a series of desirable protected nucleoside analogues [8-10]. After that hydrolysis of protected nuclioside analogues in sodium methoxide gave free nucleoside analogues [11-13]. These new formed compounds were diagnosed by 13C-NMR and 1H- NMR for some of them and FT-IR spectroscopy.
This work involves the synthesis and characterization of asymmetrical pyromellitdiimide
derivatives [IV]a-f
by four sequence steps selective reaction . One mole of pyromellitic dianhydride
was reacted with one mole of various primary aromatic amines [ 4-nitro aniline , 4-chloro aniline , 4-toludine and 4-anisidine] in excess of dry acetone to produce six compounds (N-substituted-pyromellitamic monoacid) [I]a-f . These new compounds [I]a-d were converted to the corresponding
N- substituted- pyromellitmonoimide [II]a-d via their heating at (80-90)
0
C in sodium acetate-acetic
anhydride mixture .
The compounds [II]a-f
were allowed to react with one mole of another primary amines in
excess of dry acetone t
Polyacetal was synthesized from the reaction of Polyethylene glycol with4- dimethylaminobenzaldehyde.Polymer metal complex was synthesized by the reaction with Ag+; polymer blend with polyvinyl alcohol was synthesized solution casting technique. All synthesized compounds were characterized by FT-IR in addition to the antimicrobial activity. The FT-IR spectra indicate the formation of the polyacetal. The DSC resultsindicatethe thermal stability regarding the synthesized polymer blends. The synthesized polyacetal, its metal complex and PA blend against four types of bacteria (gram+ve) Staphylococcus aureas, Bacillus subtilis and (gram –ve)Klebsiella pneumoniae, Escherichia Coli w
... Show MoreMushrooms have bioactive compounds that have antimicrobial, anti-cancer and antioxidant activities among other medicinal benefits. In the present study, we examined the anti-cell proliferation activities of mushrooms from eight genera obtained from the wild in Nigeria. Saccharomyces cerevisiae was used as a model organism to screen mushroom extracts for anti-cell proliferation activity. Polyphenols, high molecular weight polysaccharides and low molecular weight compounds from aqueous extracts were obtained from the test mushrooms using methanol and water respectively. The extracts were screened in vitro at different concentrations of extracts with the CyQuant cell proliferation assay. The high molecular
... Show MoreThe present work included a study of benthic algae on two substrates: rocks and clay on a section of the Tigris River at the Al-Atifiyah site in the fall of 2018. The result of this study was recorded 89 species belong to 50 genus of benthic algae on both substrates and composed of Bacillariophyceae (59.6%, 61.2%), Chlorophyceae (25.8%, 20.4%) and Cyanophyceae (14.5%, 18.3%) respectively on epilithic and epipelic algae. The present study was recorded the highest total algae cell density (1173.2 cells *103/cm2) on epilithic algae while the lowest total algae cell density was recorded on epipelic algae (76.95 cells *103/gm). For measure div