Histone deacetylase inhibitors with zinc binding groups often exhibit drawbacks like non-selectivity or toxic effects. Thus, there are continuous efforts to modify the currently available inhibitors or to discover new derivatives to overcome these problems. One approach is to synthesize new compounds with novel zinc binding groups. The present study describes the utilization of acyl thiourea functionality, known to possess the ability to complex with metals, to be a novel zinc binding group incorporated into the designed histone deacetylase inhibitors. N-adipoyl monoanilide thiourea (4) and N-pimeloyl monoanilide thiourea (5) have been synthesized and characterized successfully. They showed inhibition of growth of human colon adenocarcinoma and mouse hepatoblastoma cells with low cytotoxic effect against normal human breast cells. Their binding mode to the active site of several histone deacetylases has been studied by docking and the results gave a preliminary indication that they could be successful histone deacetylase inhibitors.
Till 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 MoreAmoxicillin 1 was treated with thiosemicarbazide and Phosphoryl chloride to obtain a new derivatives that contains 1,3,4-thiadiazole moiety 2. Schiff bases compounds were synthesized by the reaction of compound 2 with different aldehydes such as benzaldehyde and some substituted Benzaldehyde; p-hydroy, p-Chloro, p-Nitro, p-Dimethylamino, p-Methyl, p-Methoxy, p-Ethoxy to give compounds 3a-h. The obtained compounds have tested towards gram -ve and gram +ve bacteria. The compound shows good to moderate result towards the bacteria.
The design of fabrics and fashion is manifested by aesthetic advantages betting with the movement of society in its quest to develop as an independent art in itself that is linked to the values and aesthetic concepts of other arts and what appears in them of intellectual systems calling for renewal and modernity. Which brought about a wide change in public taste, as well as a desire for innovation . Which made fashion an interesting aesthetic phenomenon and taste is always subject to change constantly to comply with the social variables that occur in human life, as the fashion that appears in a certain era of time and takes a great distance from spreading as something new and out of the ordinary is in fact the fruit of the development of
... Show MoreTwo series of Schiff Bases [VI]n and thiazolidin-4-one derivatives[VII]n were synthesized by many steps starting from cyclization of 4- hydroxyacetophenon with thiourea in iodine to yield 1,3-thiazole compound which was reacted with pentoxy bromide in anhydrous potassium carbonate to converted compound[II] and this reacted with Phenol to yield azo compound[III]. The azo compound reacted with ethyl chloro acetate in basic medium to get a new easter compound[IV] which is converted to their acid hydrazid[V]. The later compound condensation with n-alkoxy benzaldehyde to give new Schiff bases[VI]n . Imine group undergoes addition cyclization with thioglycolic acid to get thiazolidinone compounds[VII]n .Also, two new series of Schiff Bases [XII]n
... Show MoreComplexes of Lanthanide ione Ln(III) =La(III) , Ce(III),Pr(III) and Nd(III) withligands of nicotinamide (na) and Benzimidazole (BIMD) have been prepared withgeneral formula [M(na)3(BIMD)3](NO3) where :M = Ln(III) = La(III) , Ce(III) , Gd(III) , Nd(III) .Na = nicotinamide = C7H6N2OBIMD = Benzimidazole = C7H6N2All compounds have been characterized by spectroscopic methods [FT-IR , UV-VIS ,AAS] , microanalysis (C.H.N) Along with conductivity measurements , solubility ,melting point , theroitical measurment by using chem office 3D prog .Model (2000) .Frome the above data the proposed moleculer structure for all complexes with its ionsis octahydral geometries
ABSTRACT. The reaction between benzil and hexamethylenediamine formed a new ligand [L], [(1Z,3Z)-2,3-diphenyl-5,6,7,8,9,10-hexahydro-1,4-diazecine], of the type [N2], was synthesized by the condensation reaction through Schiff base reaction between benzil and hexamethylenediamine. The new Schiff base ligand reacts with Mnп, Niп and Coп metal ions to give the complexes with the general formula: [M(L)Cl2]. The elemental investigations have been used to analyze the ligand and its complexes by CHN, FT-IR, UV-Vis, TLC, mass spectrum, melting point with the study of biological activity to the formed compounds. From the data obtained, the proposed molecular structure adopts square planar structure about the metal ions. The study reveals
... 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 MoreTwelve compounds containing a sulphur- or oxygen-based heterocyclic core, 1,3- oxazole or 1,3-thiazole ring with hydroxy, methoxy and methyl terminal substituent, were synthesized and characterized. The molecular structures of these compounds were performed by elemental analysis and different spectroscopic tequniques. The liquid crystalline behaviors were studied by using hot-stage optical polarizing microscopy and differential scanning calorimetry. All compounds of 1,4- disubstituted benzene core with oxazole ring display liquid crystalline smectic A (SmA) mesophase. The compounds of 1,3- and 1,4-disubstituted benzene core with thiazole ring exhibit exclusively enantiotropic nematic liquid crystal phases.
characteristic tissues and cells, exerting their pharmacological aspects and alleviating a lot of diseased processes. Accordingly, this research is about introducing some isatins to be nucleophilically attacked at C3 forming products of azomethine ylide functionality. These iminium compounds were made by allowing certain isatins to be reacted with the secondary amino acid, proline, at acetic acid and methanol medium and then collected after purification to be identified with total Leukocyte count (TLC) and melting point. The structural characterization was performed by fourier-transform infrared spectroscopy (FTIR), proton nuclear magnetic resonance (1H-NMR), and community health nursing (CHN) analysis. The microbiological evaluatio
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