Small molecules drug conjugate mutual prodrug design (SMDC) composed of folate and lethal agent conjugate, rigidly bonded via hydrophilic bridge and self immolative disulfide bond ; represent new interesting approaches for cancer treatment , the component of SMDC intended for targeting folate receptor , along with greater conservation of component until reaching the target tumor tissue . The designing and synthesis of compound VI and VIII derived from 6-Mercaptopurine (6-MP) and Methotrexate ( MTX) conjugate altogether as mutual prodrugs were processed forward successfully by multistep reaction procedures , and by Thin Layer Chromatography (TLC) for
... Show MoreAbstract As a part of our ongoing project on the design and synthesis of new 4-thiazolidinone derivatives with antimicrobial activity, four new 4-thiazolidinone derivatives carrying bromo, nitro, methyl, and chloro groups on the benzene ring were synthesized by starting with the 7-amino-4-methylcoumarin moiety, linking coumarin with various phenyl isothiocynate to form the thiourea group, and then cyclizing the derivatives, characterized by IR and 1HNMR, and assayed in vitro for their antimicrobial activity against Gram positive and Gram negative bacteria and fungi. Overall, 2-(4-methyl-2-oxo-2H-chromen-3-yl)-3-(4-nitrophenyl) thiazolidin-4-one to be the most powerful individuals in the series. Based on the observed data, it can be sta
... Show MoreSorption is a key factor in removal of organic and inorganic contaminants from their aqueous solutions. In this study, we investigated the removal of Xylenol Orange tetrasodium salt (XOTS) from its aqueous solution by Bauxite (BXT) and cationic surfactant hexadecyltrimethyl ammonium bromide modified Bauxite (BXT-HDTMA) in batch experiments. The BXT and BXT-HDTMA were characterized using FTIR, and SEM techniques. Adsorption studies were performed at various parameters i.e. temperature, contact time, adsorbent weight, and pH. The modified BXT showed better maximum removal efficiency (98.6% at pH = 9.03) compared to natural Bauxite (75% at pH 2.27), suggesting that BXT-HDTMA is an excellent adsorbent for the removal of XOTS from water. The equ
... Show MoreTill now, isatin derivatives have received a lot of interest in organic and medicinal chemistry due to their significant biological and pharmacological activities. Schiff’s and Mannich bases of isatins are an effective group of heterocyclic derivatives that play a significant role in medicinal chemistry as antimicrobial agents. In light of these facts, new Schiff bases and Mannich bases of isatin were synthesized. The monomer Mannich bases; 3(a-e) have been synthesized by reacting isatin with different secondary amines, piperidine, morpholine, and pyrrolidine, dimethylamine, diphenylamine, separately, and formaldehyde, while the dimer (5) formed by using piperazine and formaldehyde which then react separately with Phenylhydrazine
... Show MoreA group of amine derivatives [4-aminobenzenesulfonamide derivatives, 2-aminopyridine and 2-aminothiazole] incorporated to α-carbon of diclofenac a well known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were designed and synthesized for evaluation as a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of the selected final compounds (9, 12 and 13) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (3 mg/Kg) of diclofenac sodium. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50
... Show MoreBig data analysis is essential for modern applications in areas such as healthcare, assistive technology, intelligent transportation, environment and climate monitoring. Traditional algorithms in data mining and machine learning do not scale well with data size. Mining and learning from big data need time and memory efficient techniques, albeit the cost of possible loss in accuracy. We have developed a data aggregation structure to summarize data with large number of instances and data generated from multiple data sources. Data are aggregated at multiple resolutions and resolution provides a trade-off between efficiency and accuracy. The structure is built once, updated incrementally, and serves as a common data input for multiple mining an
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