New series of 4,4'-((2-(Aryl)-1H-benzo[d]imidazole-1,3(2H)-diyl)bis(methylene))Diphenol(3a-g) was successfully synthesized from cyclization of the reduction product of bis Schiff bases (2) with aryl aldehydes bearing phenolic hydroxyl in the presence of acetic acid. The structure of these compounds was identified from FT-IR, 1H NMR, 13C NMR and EIMs. The Antioxidant capability was screened by DPPH and FRAP assays. Both assays showed antioxidant capability more than BHT as well. Compounds 3b and 3c showed antioxidant capacity slightly less than ascorbic acid. The docking study for theses compound was carried out as III DNA polymerase inhibitor. The results of docking demonstrated that the increase in hinderances around phenolic hydroxyl for the aryl attached position two for benzimidazole decrease the capability of interaction and give less bending and smaller docking score and there is inverse relationship between increasing hindrances around phenolic hydroxyl and DNA polymerase inhibition for these compounds.
Compound 4-(((6-amino-7H-[1, 2, 4] triazolo [3, 4-b][1, 3, 4] thiadiazin-3-yl) methoxy) methyl)-2, 6-dimethoxyphenol (6) was synthesized by multi steps. The corresponding acetonitrile thioalkyl (7) was cyclized by refluxing with acetic acid to afford 4-(((6-amino-7H-[1, 2, 4] triazolo [3, 4-b][1, 3, 4] thiadiazin-3-yl) methoxy) methyl)-2, 6-dimethoxyphenol (8). Two new series of 4-(((6-(3-(4-aryl) thioureido)-7H-[1, 2, 4] triazolo [3, 4-b][1, 3, 4] thiadiazin-3-yl) methoxy) methyl)-2, 6-dimethoxyphenol (9a-c) and of 4-(((6-(substitutedbenzamido) 7H-[1, 2, 4] triazolo [3, 4-b][1, 3, 4] thiadiazin-3-yl) methoxy) methyl)-2, 6-dimethoxyphenol (10a-c) were synthesized as new derivatives for fused 1, 2, 4-trizaole-thiadiazine (8). The antioxidant
... Show MoreCompound 4-(((6-amino-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazin-3-yl)methoxy)methyl)- 2,6-dimethoxyphenol (6) was synthesized by multi steps. The corresponding acetonitrile thioalkyl (7) was cyclized by refluxing with acetic acid to afford 4-(((6-amino-7H-[1,2,4]triazolo[3,4- b][1,3,4]thiadiazin-3-yl)methoxy)methyl)-2,6-dimethoxyphenol (8). Two new series of 4-(((6-(3- (4-aryl)thioureido)-7H-[1,2,4]triazolo[3,4-b][1,3,4] thiadiazin-3-yl)methoxy)methyl)-2,6- dimethoxyphenol (9a-c) and of 4-(((6-(substitutedbenzamido)7H-[1,2,4]triazolo[3,4- b][1,3,4]thiadiazin-3-yl)methoxy)methyl)-2,6-dimethoxyphenol (10a-c) were synthesized as new derivatives for fused 1,2,4-trizaole-thiadiazine(8). The antioxidants of newly compounds were evaluated by DPPH
... Show MoreCreatinine and Schiff`s bases are well known for their diverse range of biological activities and are thought to be emerging and useful therapeutic targets for the treatment of several diseases. The present work was aimed at the synthesis of new imidazolidine-4-one, thiazolidine-4-one, and oxazolidine-4-one derivatives derived from creatinine and to illustrate their influence on a colon cancer cell line and assess their antioxidant activity. Creatinine was reacted with α-chloroethyl acetate to produce 2-ethyl acetate creatinine 1. Then, the reaction of compound 1 with n-propyl bromide afforded N-propyl-2-ethylacetate creatinine 2. Compound 2
... Show MoreTwo series of Schiff Bases and 2,3-disubstituted-1,3-thiazolidin-4-one derivatives were synthesized . Reaction of 2-mercaptobenzothiazole with α-chloro acetic acid gave compound[I]. Esterification of carboxylic moity of compound [I] , using absolute methanol in the presence of conc . H2SO4 yielded acorresebonding ester [II] , wich was condensation with hydrazine hydrate to give acid hydrazide [III] . The new Schiff bases [V]n were synthesized by reaction of acid hydrizide with dialdehyde [IV]n in the presence of glacial acetic acid . The thiazolidinone derivatives [VI]n have been obtained from the azomethines through the addition of thioglycolic acid . Their chemical structures have been confirmed by mel
... Show MoreIn this study new derivatives of O-[2-{''2-Substituted Aryl (''1,''3,''4 thiadiazolyl) ['3,'4-b]-'1,'2,'4- Triazolyl]-Ethyl]-p- chlorobenzald oxime (6-11)have been synthesized from the starting material p-chloro – E- benzaldoxime 1.Compound 2 was synthesized by the reaction of p-chloro – E- benzaldoxime with ethyl acrylate in basic medium. Refluxing compound 2 with hydrazine hydrate in ethanol absolute afforded 3. Derivative 4 was prepared by the reaction of 3 with carbon disulphide, treated of compound 4 with hydrazine hydrate gave 5. The derivatives (6-11) were prepared by the reaction of 5 with different substitutesof aromatic acids. The structures of these compounds were characterized from their melting points, infrared spectroscopy
... Show MoreThe biological activities of some ternary nickel complexes with a Schiff base obtained from 4-dimethylaminobenzaldehyde and 2-aminophenol have been reported. The Schiff base ( HL1) acts as a primary ligand whereas, anthranilic acid ( HL2), 2-nitroaniline ( HL3), alanine ( HL4) and histidine ( HL5) act as secondary ligand or co-ligand. The anticancer activity of these compounds was studied against human colon carcinoma (HCT-116), human hepatocellular liver carcinoma (HEPG-2) and human breast carcinoma (MCF-7) cell lines. As per the results, the compounds were active against the cell lines. The antioxidant activity of the same compounds was evaluated using DPPH (1,1-diphenyl-2-picryl-hydrazyl) radical scavenging and compared with ascorbic aci
... Show MoreObjective: Hesperidin (HSP) is a pharmacologically active organic compound found in citrus fruits and peppermint. We synthesized a new HSP derivative by reacting it with 5-Amino-1,3,4-thiadiazole-2-thiol in acetic acid. Methods: This compound was characterized by Fourier-transform infrared, proton nuclear magnetic resonance, and electron impact mass spectra. A molecular docking study explores the predicted binding of the compound and its possible mode of action. Bioavailability, site of absorption, drug mimic, and topological polar surface was predicted using absorption, distribution, metabolism, and excretion (ADME) studies. Results: The docking study predicts that the new compound binds to the active sites of Aurora-B
... Show MoreA comparison study was made for the reaction of triruthenium carbonyl Ru3(CO)12 with azoarene ArN=NAr . This reaction was monitored in two kinds of solvents , toluene , and n- octane , which yielded new triruthenium carbonyl complex Ru3(μ3-NAr)2(CO)9 . The reactions of azoarenes ArN=NAr with Ru3(CO)12 formed the following trinuclear compound of Ru3((μ3- NAr)2(CO)9 (Ar-C6H4Br-4) in law yield . In addition , to new isomers species of mononuclear cyclometallated of Ru(BrC6H4N-NC6H4NBr-4)2(CO)2 in different percentages . The mechanism of the reaction domenstrates that the formation of trinuclear bis arylimido complexes , and ortho metallated was , the result of cleavage of nitrogen –nitrogen bond . Monitoring this gave evidence that the rea
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