Reducing of ethyl 4-((2-hydroxy-3-methoxybenzylidene)amino)benzoate (1) afford ethyl 4-((2-hydroxy-3-methoxybenzyl) amino)benzoate (2). Reaction of this compound with Vilsmeier reagent affords novel 2-chloro-[1,3] benzoxazine ring (3). The corresponding acid hydrazide of compound 3 was synthesized from reaction of compound (3) with hydrazine hydrate. Newly series of hydrazones(5a–i) were synthesized from reaction of acid hydrazide with various aryl aldehydes. Antibacterial activity of the hydrazones wassecerned utilizing gram-negative and gram-positive bacteria. Compound (5b) and (5c) exhibited significant antibacterial ability against both gram-negative and gram-positive bacteria, while the compounds(5a) showed mild antibacterial activity. Compounds (5d–i) did not display notable activity. The molecular docking of synthesised compounds were tested inside the pocket of bacterial gyrase enzyme target site by using MOE 2015 software, which acts as Adenosine triphosphate (ATP)-binding domain bacterial gyrase enzyme pocket and novobiocin was used as reference.
In this study, new derivatives of 3-C-spiro ring nucleoside analogues were synthesized. The structures of these derivatives were characterized by infrared spectroscopy,1HNMR (some of them) and elemental analysis. The nucleoside derivatives were tested for inhibition of E-coli and were all found to be active.
The present study envisaged utilizing 4-aminoantipyrine as key intermediate for the synthesis of some new derivatives bearing anti-bacterial and anti-cancer activities moieties viz., antipyrine diazenyl benzaldehydes 2(ad) which were obtained by coupling of diazotized 4-aminoantipyrine (1) with substituted benzaldehydes at 0◦C (iced) temperature. The other antipyrine derivatives where containing bis heterocycles like bis thiazolidinone-antipyrine (4), bis imidazolidinone -antipyrine (5) and bis azetidinone -antipyrine (6).These compounds were prepared through the reaction between 4- aminoantipyrine and terephthaldicarboxaldehyde to get (3) which were reacted with mercaptoacetic acid , glycine or chloroacetyl chloride separately to get com
... Show MoreAbstract Organic compounds with pyrazole cores have a variety of uses, notably in the pharmaceutical and agrochemical sectors. The interest in creating pyrazole compounds, examining their many features, and looking for potential uses is growing. Our work has concert with synthesis of chalcones and pyrazolines, then finally pyrazoline-aniline derivatives and evaluation their anti-inflammatory, antibacterial and antifungal activities
A new Mannich base ligand was prepared by reacting the 2-chloro.-N-(5-mercapto-1, 3, 4-thiadazol -2-yl) acetamide and Piperidine in the presence (formaldehyde) (L) ligand. A series of ligand complexes were prepared from (L) with the metal ion Co (II), Ni (II), Cu (II), Pd (II), Pt (IV), and Au (III). Various spectroscopic techniques such as C.H.N.S, FTIR, UV-VIS, , 1HNMR, 13CNMR, Magnetic moment, and molar conductivity successfully characterize the obtained compounds. The M: L ratio was determined using the molar ratio method in solution. All prepared compounds' antibacterial and antifungal activity was studied against two types of bacteria and one type of fungi at a rate of 0.02M. The standard ΔH°
... Show MoreThe reaction of LAs-Cl8 : [ (2,2- (1-(3,4-bis(carboxylicdichloromethoxy)-5-oxo-2,5dihydrofuran-2-yl)ethane – 1,2-diyl)bis(2,2-dichloroacetic acid)]with sodium azide in ethanol with drops of distilled water has been investigated . The new product L-AZ :(3Z ,5Z,8Z)-2azido-8-[azido(3Z,5Z)-2-azido-2,6-bis(azidocarbonyl)-8,9-dihydro-2H-1,7-dioxa-3,4,5triazonine-9-yl]methyl]-9-[(1-azido-1-hydroxy)methyl]-2H-1,7-dioxa-3,4,5-triazonine – 2,6 – dicarbonylazide was isolated and characterized by elemental analysis (C.H.N) , 1H-NMR , Mass spectrum and Fourier transform infrared spectrophotometer (FT-IR) . The reaction of the L-AZ withM+n: [ ( VO(II) , Cr(III) ,Mn(II) , Co(II) , Ni(II) , Cu(II) , Zn(II) , Cd(II) and
... Show MoreThis research includes the synthesis of some new different heterocyclic derivatives of 5-Bromoisatin. New sulfonylamide, diazine, oxazole, thiazole and 1,2,3-triazole derivatives of 5-Bromoisatin have been synthesized. The synthesis process started by the reaction of 5-Bromoisatin with different reagents to obtain schiff bases of 5-Bromoisatin intermediate compounds(1, 8, 19) by using glacial acetic acid as a catalyst in three routes. The first route, 5-Bromoisatin reacted with p-aminosulfonylchloride to product compound(1), then converted to sulfonyl amide derivatives(2-7) by the reaction of compound(1) with different substituted primary aromatic amine in absolute ethanol. The second route includes the reaction of 5-Bromoisatin rea
... Show More4,4'-(pyridine-2,6-diylbis(1,3,4-oxadiazole-5,2-diyl))bisphenol monomer (3)was synthesized from cyclization of N'2,N'6-bis(4-hydroxybenzylidene)pyridine-2,6-dicarbohydrazide (2)in the presence of bromine in glacialacetic acid. Newly five polymers (P1-P5) were synthesized from reaction bis-1,3,4-oxadiazole bisphenolmonomer with five different di acid chloride. The antibacterial activity of the synthesized polymers was screened against gram positive and gram negative bacteria. Polymers P4 and P5 exhibited significant antibacterial against all microorganisms, as well these polymers showed highest antifungal activity.
This work includes the synthesis of some new five- seven heterocyclic rings derived from benzenesulfonylhydrazide as starting material. Its condensation with 4-methoxy and 4nitro benzaldehyde gives the Schiff bases (1a,b). Schiff bases were reacted with cyclic anhydrides given Oxazepine, Thiazepine derivatives(2,3,4 a,b)(seven membered ring) and with 2-mercapto benzoic acid gives thiazine derivatives (6a,b)(six membered ring) finally with thioglycolic acid give thiazolidine ring(five membered ring) scheme(3). The synthesized compounds have been characterized by melting points,FT-IR, 1H-NMR spectroscopy ,13CNMR and Elemental analysis. some of synthesized compounds were tested for their antibacterial activity
... Show MoreSmall ring heterocycles containing nitrogen and sulfur have been under investigation for a long time because of their important medicinal properties. Among the wide range of heterocycles explored to develop pharmaceutically important molecules, thiadiazoles had played an important role in medicinal chemistry. A survey of literature had shown that compounds having thiadiazole nucleus possess a broad range of biological activities such as anti-inflammatory (1), antibacterial (2), and antifungal activities (3). Thiazine-4-one and their derivatives are import classes of compounds in organic and medicinal chemistry. The thiazine-4-one ring system is a core structure in various synthetic pharmaceutical agents, displaying a broad spectrum of biolo
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