A new series of schiff base and aminothiadiazole derivatives of N- substituted phthalimide (I-VI) were synthesized. In this work, the intermediate 4-(1,3-dioxoisoindolin-2-yl)benzaldehyde compound (I), was formed by reaction of 4-amino benzaldehyde with phthalic anhydride in glacial acetic acid(GAA). A series of Schiff bases (IV-VI) was prepared by the reaction of benzidine with compound (I) in ethanol and presence of GAA as a catalyst to form compound (IV) which react with compound (I) and p-nitro benzyldehyde to give compound (V) and (VI) respectively. A new phthalimide thiosemi-carbazone derivative (ll) was prepared by reaction of compound (l) with thiosemi-carbazide HCl in the presence of equimolar amount of sodium acetate. Finally, a new phthalimide containing (1,3,4- thiadiazole ring) compound (III) was formed by bromine mediated “oxidative intramolecular cyclization” of compound (I) in the presence of sodium acetate. All of the final target compounds' structures were successfully synthesized and confirmed using analytical and spectroscopic data. These compounds were identified and confirmed by melting points, TLC, FT IR, and 1H NMR. While the antimicrobial effect of the new derivatives has been assessed in vitro against G-positive, G-negative bacteria and fungi activity. All screened compounds exhibited no activity against G-positive bacteria (Staph. Aureus, and Bacillus subtilis). Many of synthesized compounds displayed moderate effect against “G-negative bacteria Escherichia coli, and Klebsiella pneumonia and against Candida tropicalis”. While the best antifungal activity was obtained from compound I which has high activity against Candida tropicalis.
Aromaticity, antiaromaticity and chemical bonding in the ground (S0), first singlet excited (S1) and lowest triplet (T1) electronic states of disulfur dinitride, S2N2, were investigated by analysing the isotropic magnetic shielding, σiso(r), in the space surrounding the molecule for each electronic state. The σiso(r) values were calculated by state-optimized CASSCF/cc-pVTZ wave functions with 22 electrons in 16 orbitals constructed from gauge-including atomic orbitals (GIAOs). The S1 and T1 electronic states were confirmed as 11Au and 13B3u, respectively, through linear response CC3/aug-cc-pVTZ calculations of the vertical excitation energies for eight singlet (S1–S8) and eight triplet (T1–T8) electronic states. The aromaticities of S
... Show MoreThe effectiveness inhibitory to extract alcohol for the leaf and flower to plant sage Salvia pratensis each of Staphylococcus aureus, streptococcus epidermidis, Salmonella typhi, Pseudomonas aeroginosa, Escherichia coli, Aspergillus niger and Candida albicans whom had any inhibition to aqueous extracts of the parts itself species bacterial and fungal. The study also demonstrated that the extract of plant containing compounds chemical such as tannins, Alkaloids, Flavonoieds, and saponins, which owns effectiveness of medical. The MIC, MBC and inhibition zones for crud extract were determinated for microbial agents.
: Partial purification of phosphoenolpyruvate carboxykinase (PEPCK) from type 2 diabetic patients sera take place using some purification steps such as participation with ammonium sulphate (55-80%) and filtered through dialysis, then ion exchange chromatography by DEAE sepharose anion column, gel filtration chromatography by sephadex G-100 column. In ion exchange step, there are four peak are obtained, the highest enzyme activity obtained by (0.4 M Nacl) with purification fold (2.18), yield (44.3) of enzyme and specific activity (13.5) mg/ng, which obtained a single peak by gel filtration chromatography, the degree of purification (5.34) fold, yield of enzyme (20%) with specific activity (33.109mg/ng). The purified enzyme had an optimum tem
... Show MoreThe study aimed to purification of acid phosphatase (ACP) from sera of obesetype 2 diabetes mellitus patients, this study included from thirty T2DM patients and thirty control, purification process was done with several steps included precipitation with inorganic salt (NH4 ) 2SO4 30%-80%, dialysis, ion exchange chromatography by DEAE sepharose anion column and size exclusion chromatography by Sepharose 6B.ACP, BMI, FBS, HbA1c, Lipid profile, Urea, Creatinie, Insuline, Homa-IR were determined. Results showed the precipitate and concentrated protein appeared four peaks in ion exchange column. ACP located in the first and second peak with purification fold (21.1), (37.2) yield of enzyme and specific activity (173.3) IU/ml, which obtained a si
... Show MoreObjective: Matrix tablet approach is one of the delivery systems intended for poorly water-soluble drugs, like candesartan cilexetil (CC). CC is a class II drug used for the treatment of hypertension. Methods: Matrix tablets from (F1x to F18z) were prepared in the presence of β‑cyclodextrin. Matrix tablet formulation ensures control release of the drug and higher dissolution by β‑cyclodextrin. Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC) were used to study compatibility. Results: The angle of repose determination showed good flow for most of the formulas, besides having good compressibility. Weight variation test for all formulas showed accepted value. Drug content measurement sho
... Show MoreObjective: Matrix tablet approach is one of the delivery systems intended for poorly water-soluble drugs, like candesartan cilexetil (CC). CC is a class II drug used for the treatment of hypertension. Methods: Matrix tablets from (F1x to F18z) were prepared in the presence of β‑cyclodextrin. Matrix tablet formulation ensures control release of the drug and higher dissolution by β‑cyclodextrin. Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC) were used to study compatibility. Results: The angle of repose determination showed good flow for most of the formulas, besides having good compressibility. Weight variation test for all formulas showed accepted value. Drug content measurement sho
... Show MoreNon-steroidal anti-inflammatory drugs (NSAIDs) contain free –COOH which thought to be responsible for the GI irritation associated with all traditional NSAIDs. The esterification of this group is one of an approach to ultimate aim for reduce the gastric irritation; so in this study we synthesized and preliminarily evaluated new ester compounds as new analogues with expected selectivity toward COX-2 enzyme. Synthetic procedures have been successfully developed for the generation of the target compounds (III a and b). The synthetic approach involved multi-steps procedures which include: Synthesis of 4-hydroxy benzene sulphonamide ( I b ), synthesis of Naproxen and Ibuprofen acyl chloride and then reacting them with 4-hydroxy benzene sulphon
... Show MoreCilnidipine is a dihydropyridine class of calcium channel blockers, it is classified as a BCS class II drug, characterized by a low oral bioavailability of 13%. Consequently, the utilization of nanoparticle preparation is anticipated to enhance its bioavailability. The objective of the research is to integrate cilnidipine nanoparticles into oral films as a means of enhancing patient adherence. The optimal polymers for producing Cilnidipine films were PVA cold and or HPMC E5 at different concentrations using a casting technique with glycerol as a plasticizer. The Nano suspension-based preparation of Cilnidipine's oral film containing the combination of polymers exhibited a significant enhancement in vitro dissolution, with a percentage excee
... Show More