Background: The isatin molecule is present in many natural substances, including plants and animals, and is used to prepare compounds with various biological activities. Objectives: To synthesize a new series of isatin derivatives with the expectation that they will have antimicrobial activity. Methods: Thiazole Schiff bases were synthesized from various Mannich bases of isatin to evaluate their antimicrobial properties. Initially, Mannich bases (2a–e) were synthesized by reacting isatin with formaldehyde and different secondary amines. Subsequently, they were treated with 2-aminothiazole to yield the final compounds (3a–e). Spectroscopic characterization was done via FT-IR and 1H-NMR. The antimicrobial screening was conducted on all derivatives. Molecular docking and ADMET analysis were performed on the final compounds, comparing them with standard drugs (ciprofloxacin and fluconazole). Results: The antimicrobial activity was assessed on two Gram-positive bacteria, Staphylococcus aureus and Bacillus licheniformis; two Gram-negative bacteria, Escherichia coli and Acinetobacter baumannii; and one fungus species, Candida albicans. Molecular docking has recorded higher docking scores for 3d and 3e compared to ciprofloxacin and fluconazole. The virtually active molecules showed an adequate drug-like profile and desired pharmacokinetic properties in the ADMET analysis. Conclusions: Most derivatives displayed significant antimicrobial activity, with compound 3e being the most active, followed by compound 3b. Molecular docking revealed higher scores for compound 3e compared to fluconazole and for compounds 3d and 3e compared to ciprofloxacin. ADMET analysis of compound 3e showed excellent absorption, consistent with its strong GIT absorption.
Quercetin, one of the flavonoids family member, can be found in many vegetables, fruits, and beverages with a noticeable nutritional pharmacological properties. This study was aimed to evaluate the ability of quercetin to inhibit lipopolysaccharide (LPS) that induced lethal toxicity in vivo, and to elucidate the importance of the quercetin as an antitumor agent in breast cancer cell line MCF-7.In vivo experiments included the effect of hesperidin and LPS on the liver and spleen of male mice. In the liver, the antioxidant activity was measured by estimating the concentration of glutathione (GSH), and catalase (CAT), while in the spleen, the concentration of cytokines was measured including IL-33 and TNF-α. In vitro experiments included MTT
... Show MoreAnastrozole (ANZ) is considered constitute of the fourth –generation of Non–steroidal aromatase blockage, ANZ has use for hormone receptor positive breast cancer in postmenopausal women. The serious side effects of ANZ including, vaginal dryness, hot flashes, irritability, breast tenderness and un–stability in circulation.
Nanostructured lipid carriers (NLCs) have recently emerged as a multifunctional platform for drug delivery in cancer therapy.
Five formula were composed of (200 mg of glyceryl monostearate, 40 mg of oleic acid , 1% (w/w) Tween 80, 1% (w/w) Poloxamer 407, 1% (w/w) soy lecithin and Vitamin E Polyethylene Glycol Succinate.
The mean particle size, polydispersity index, zeta potential, entrapme
... Show MoreOsteoporosis (OP) is a systemic skeletal disorder that is characterized by reduced bone mass and micro-architectural deterioration of bone tissue, with a consequent increase in bone fragility and susceptibility to fracture. The most frequent osteoporotic fractures are fractures of the hip, wrist, and spine. The exact causes of OP are still unknown; several factors contribute to the disorder. Subjects and Methods: This study consists of patient groups, this group (Group A) was composed of 80 postmenopausal women with OP and osteopenia and the patient group was subdivided into two group; First group (GroupA1) was composed of 50 postmenopausal women with OP and the second group (Group A2) composed of (30) Postmenopausal Women with oste
... Show MoreIn spite of the contemporary development over the world in pertaining of modernization and its differences about the transformation of the knowledge but, the important instrument to transfer the thoughts and information did not have change except the language. So the evolutionary process became as a torrent or fusillade above the cliff which drifted anything. So that the objective inquiry and impressed with varieties of development the casement to evaluate the linguistic or re - correction highlight article in order to preserve on the origins of the language and its sobriety.
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Aspirin and clopidogrel are considered the most important oral platelets aggregation inhibitors. So it is widely used for treatment and prophylaxis of cardiovascular and peripheral vascular diseases related to platelets aggregation .In this study aspirin and clopidogrel were formulated together as floating bilayer tablet system. Three different formulas of 75 mg aspirin were prepared by wet granulation method as immediate release layer; different disintegrants used to achieve rapid disintegration. Formula with crosscarmellose as disintegrant achieve rapid disintegration was selected for preparation of bilayer tablet.
Different formulas of 75 mg clopidogrel were prepared as sustained release floating layer by wet granulation (effe
... Show MoreBackground: The present study involved the following parts, the first part is evaluation of the levels of glycated hemoglobin(HbA1c), creatinine, uric acid(UA) and albumin in patients with diabetic nephropathy comparison with the group of healthy as a control group. The second part is the measurement and evaluation of oxidative stress represented in the malondihydehyde(MDA) as a biomarker of oxidative stress as well as the identification of vitamins C and E as an antioxidant in patients with diabetic nephropathy(DN) compared with the healthy group. Objective: The objective of this study is to estimate oxidative stress by calculate malondialdehyd as biomarker and evaluate some vitamins such as vit C and vit E as antioxidants in diabetic neph
... Show MoreThe purpose of my thesis is to synthesis two new bidentate ligands which were used to prepare series of metal complexes by reacting the ligands with (M+2 = Mn, Co, Ni, Cu, Cd and Hg) Succinyl chloride was used as starting material to synthesis two bidentate ligands (L1) and (L2) by reaction it with 4-chloroaniline (L1) and (4-aminoacetophenone) (L2) in dichloromethane as a solvent, that are: (L1) = N1,N4-bis (4-chloro phenyl ) succinamide (L2) =N1,N4-bis(4-acetylphenyl)succinamide The new ligands were characterize by using spectroscopic study (Fourier-transform infrared spectroscopy (FT-IR), electronic spectra ( UV-Vis) ,nuclear magnetic resonance(1H,13C-NMR), Mass spectra
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