The pharmacophore 2-aminothiazole has an interesting role in pharmaceutical chemistry as this led to the synthesis of many types of compounds with diverse biological activity. Schiff base derivatives at the same time contribute to drug evolution importantly. In this review, the Schiff base derivatives of 2-aminothiazole formed and some of their metal complexes are being focused on, and the antimicrobial and anticancer activity of them is being illustrated.
Background: Type 2 diabetes mellitus (T2DM) characterized by insulin resistance (IR) and progressive decline in functional beta (β) cell mass partially due to increased β cell apoptosis rate. Pancreatic stone protein /regenerating protein (PSP/reg) is produced mainly by the pancreas and elevated drastically during pancreatic disorder. Beta cells are experiencing apoptosis that stimulate the expression of PSP/reg gene in surviving neighboring cells, and that PSP/reg protein is subsequently secreted from these cells which could play a role in their regeneration.
Objectives: To analyze serum levels of PSP/reg protein in T2DM patients and evaluate its correlation with the microvasc
... Show MoreThis study involved the effect of the aqueous extracts of two plants, Origanum vulgare L.(1), Trigonella Foenum Graecum L. (Fenugreek) seeds(2) on the growth of cancer cell lines. Rhabdomyo sarcomas (RD) of human cell line and female intestine cells of Albino mice (L20B) in vitro System. These extracts were compared with the known anticancer drug Cis-platinum(Cis-Pt) as a positive control. The phytochemical tests were used for screening the active compounds in plants. The inhibition activity assay was used as a parameter of the cytotoxic effect of these extracts. Cancer cell lines were treated with four concentrations of Cis-platin, 31.25, 62.5, 125 and 250 ?g/ml for 72 hour exposure time. The same concentrations were used for the other ext
... Show MoreEnterococci species (spp.) are naturally found in the gastrointestinal tract (GIT), oral cavity of both human and animals causing several infections including bacteremia, meningitis, endocarditis, intra-abdominal infections, wound infections, urinary tract infections (UTI), atherosclerosis and play a critical role in the riskiness or development of periodontitis, particularly in a suitable mouth environment (Comerlato et al., 2020; Mendes et al., 2020; Xiong et al., 2021; H Elaywe, 2007). Recurrent and continues antimicrobial resistance (AMR) of opportunistic microorganisms is one of the serious public health risk, enterococci spp are often intrinsic resistant to antibiotics class routinly used in treatment such as Cephalosporins, Macrolids
... Show MoreNew 2-amino thiazole ,oxodiazole, sulphonilamide and diazin derivatives of N-(α-chloro aceto)-3-(tolyl imino)-5-bromo-2-oxo-indole(2) have been synthesized .The preparation process started by the reaction of 5-bromo isatin with P-toluidine in the presence of glacial acetic acid and dimethylformamide(DMF) as a solvent to give 3-(tolyl imino)5-bromo-1H-indole-2-one.(1), Compound (1) with sodium hydride in dimethylformamide(DMF) at 0C0 gave a suspension of the sodium salt of Schiff base derivative and subsequent reaction with monochloroacetylchloride obtained the intermediate compound(2).Compound(2) was reacted with different reagents in four routes.The first route involved direct reaction with substituted 2-aminobenzothiazole u
... Show MoreOur goal in this research, some new nucleoside analogues was synthesized. Starting from ?-D glucose which was converted to per acetylated ?-D gluco pyronoside then converted to active from(1-Bromo Sugar (2) as a sugar moiety.The base moiety 2-substituted benzimidazole was prepared from condensation of phenylene diamine with different aromatic aldehydes, which were subjected to amino alkylation via Mannich reaction forming new nucleobase derivatives. Condensation of nucleobase with bromo sugar through nucleophilic substitution of anomeric carbon with nitrogen forming new protected nucleoside analogues then hydrolyzed with sodium methoxide in methanol to obtain our target, the free nucleoside analogues. All prepared compound were identified b
... Show MoreCiprofloxacin is a broad spectrum fluoroquinolone, effective in the treatment of a wide range of infections, including genitourinary tract infections.In this study, bioadhesive vaginal tablets of ciprofloxacin hydrochloride were prepared by direct compression method using a combination of bioadhesivepolymers carbopol 934P(Cp), carboxymethylcellulose (CMC) and sodium alginate (SA) in different ratios.The prepared tablet formulations were characterized by measuring their swelling capacity, surface pH, bioadhesive properties, and in-vitro drug dissolution. It was found that the bioadhesive force was directly proportional to carbopol 934P content in different formulae and was further enhanced by the inclusion of carboxymethylcellulose.
... Show MoreIn this work, a series of new maleimides linked to substituted benzothiazole moiety were synthesized. Synthesis of these new cyclic imides were performed via three steps, the first one involved preparation of a series of 2-aminobenzothiazole substituted with different substituents via reaction of different primary aromatic amines with ammonium thiocyanate and bromine in glacial acetic acid. The prepared 2- amino benzothiozoles were introduced in the second step in reaction with maleic anhydride producing a series of N-(substituted benzothiazole-2-yl) maleamic acids.The resulted maleamic acids were dehydrated in the third step via treatment with acetic anhydride and anhydrous sodium acetate to afford a series of the desirable N-(substitu
... Show MoreThe impact of a Schiff base namely 2-((thiophen-2-ylmethylene)amino)benzenethiol to corrode mild steel in 1 M HCl resolved was evaluated using different weight loss technique and scanning electron microscopy (SEM).different weight measurements to expand that the 2-((thiophen-2-ylmethylene) amino) benzenethiol inhibits the corrosion of mild steel through adsorbing of top for mild steel and block the active locality. The inhibitive impacts of 2-((thiophen-2-ylmethylene)amino)benzenethiol increase with increasing concentration and decrease with increasing temperature. SEM to checking revealed that the alloy surface was quite unaffected and formed protective film on its surface. The investigated
... Show MoreA series of 4-(methylsulfonyl)aniline derivatives were synthesized in order to obtain new compounds as a potential anti-inflammatory agents with expected selectivity against COX-2 enzyme. In vivo acute anti-inflammatory activity of the final compounds 11–14 was evaluated in rat using an egg-white induced edema model of inflammation in a dose equivalent to 3 mg/Kg of diclofenac sodium. All tested compounds produced significant reduction of paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the activity of compounds 11 and 14 was significantly higher than that of diclofenac sodium (at 3 mg/Kg) in the 120–300 minute time interval, while compound 12 expressed a comparable effect to that of di
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