scholarly journals Synthesis and Antimicrobial Activities of Some New Synthesized Imide and Schiff's Base Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Nermien M. Sabry ◽  
Eman M. Flefel ◽  
Mohamed A. Al-Omar ◽  
Abd El-Galil E. Amr
Keyword(s):  
Acetic Acid ◽  
Fusidic Acid ◽  
Spectroscopic Data ◽  
Glacial Acetic Acid ◽  
Aromatic Aldehydes ◽  
Antimicrobial Activities ◽  
Schiff’S Bases ◽  
Schiff’S Base ◽  
Antimicrobial Screening ◽  
Positive Controls

A series of 2,6-bis(substituted thiazolopyrimi-dinyl) pyridine(2a,b)and corresponding Schiff's bases(3a–j)were synthesized from 2,6-bis-(3-amino-2-methyl-4-oxo-9-substituted-3,4-dihydropyrido-[30,20 : 4,5]-thieno[3,2-d]pyrimidin-7-yl)pyridines(1a,b)as starting materials. The compounds1a,bwere reacted with 2,3,4,5-tetrachlorophthalic anhydride in glacial acetic acid to give the corresponding bis-imides(2a,b). But they are treated with aromatic aldehydes in refluxing ethanol to afford the Schiff’s base derivatives(3a–j). The antimicrobial screening showed that many of these newly synthesized compounds had good antimicrobial activities comparable to streptomycin and fusidic acid as positive controls. The detailed synthesis, spectroscopic data, and antimicrobial activities of the synthesized compounds were reported.

Synthesis, Characterization, Antimicrobial Screening of 5-Bromobenzofuranyl Aryl Ureas and Carbamates

2019 ◽  
Vol 4 (4) ◽  
pp. 232-235
Author(s):  
H.M. Naveena Kumari ◽  
Manjunath Harihara Mathada ◽  
Mahesh Kumar ◽  
K.T. Suda ◽  
K.M. Basavaraja
Keyword(s):  
Acetic Acid ◽  
Hydrazine Hydrate ◽  
Sodium Nitrite ◽  
Potassium Carbonate ◽  
Anhydrous Potassium Carbonate ◽  
Antimicrobial Activities ◽  
Anhydrous Toluene ◽  
Ethyl Carbamate ◽  
Primary Amines ◽  
Antimicrobial Screening

Present work reports the biologically important benzofuran aryl ureas and carbamates. The benzofuran ring was formed by reacting bromo salicylaldehyde with diethyl bromomalonate in presence of dry acetone and anhydrous potassium carbonate to obtain 5-bromo-2-ethyl carboxylate (1). The obtained ester (1) was converted into corresponding hydrazide (2) by treating with hydrazine hydrate in ethanol. Compound 2 was then converted into 5-bromobenzofuran-2-carbonyl azide (3) by treating it with sodium nitrite in dioxane and acetic acid. The compound 3 is converted into 5-bromobenzofuranyl aryl ureas (4a-e) after treating primary amines and anhydrous toluene. 5-Bromobenzofuranyl aryl carbamate (5) and ethyl carbamate (6) were also synthesized by treating compound 3 with substituted phenol in toluene and ethanol respectively. All the compounds were characterized by NMR, IR and screened for antimicrobial activities.

Synthesis, Characterization and Biological Studies of Some Bioactive Thiazolotriazole Derivatives

2010 ◽  
Vol 65 (12) ◽  
pp. 1509-1515 ◽  
Author(s):  
Manjunatha Kumsi ◽  
Boja Poojary ◽  
Prajwal Lourdes Lobo ◽  
Nalilu Suchetha Kumari ◽  
Anoop Chullikana
Keyword(s):  
Acetic Acid ◽  
Acetic Anhydride ◽  
Good Yield ◽  
Sodium Acetate ◽  
Aromatic Aldehydes ◽  
Antimicrobial Activities ◽  
One Pot ◽  
Biological Studies ◽  
Elemental Analyses

The key precursor rac-2-(4-isobutylphenyl)ethyl-1,2,4-triazole-5-thione (3) was synthesized in good yield from Ibuprofen (1). One-pot three-component reactions of 3 with 5-aryl-furan-2-carboxaldehydes/ substituted aromatic aldehydes and monochloroacetic acid in acetic acid in the presence of acetic anhydride and anhydrous sodium acetate afforded substituted thiazolo[3,2-b][1,2,4]triazole derivatives 4 and 5. The structures of the newly synthesized compounds were elucidated by elemental analyses and spectral data. The compounds were tested for their in-vitro antimicrobial activities.

scholarly journals Synthesis of Schiff’s Bases from 2-Amino-4H-1, 3-Oxazine / Thiazine and Substituted Aldehydes and their Transition Metal Complexes

2021 ◽  
Vol 04 (07) ◽  
Author(s):  
D.T. Biradar ◽  
Keyword(s):  
Acetic Acid ◽  
Metal Complexes ◽  
Bioactive Molecules ◽  
Schiff’S Bases ◽  
Schiff’S Base ◽  
One Pot ◽  
Solvent Free Condition ◽  
Synthetic Strategy ◽  
Schiff's Bases

Objective: Many methods can be found in literature for the synthesis a Oxazines and Thiazines. Few are reported for one-pot multi component cyclo-condensation of an alkayane urea / Thiourea and Aldehyde to 2- amino-4H-1, 3-Oxazines or Thiazines. Different catalysts are reported like Trifluoro-acetic acid, glacial acetic acid under reflux condition Mandal and Co-workers have utilized perchloric acid (HClO4) supported on silica gel as catalyst under solvent free condition ytterbium trifluorate [Yb(OTF)3] plays role of Lewis acid. It is also used in several Diel’s-Alder cyclo-addition reactions. Inspired these observations, development of simple effective synthetic strategy for the synthesis of 2-amino-4H-1, 3-Oxazium & Thiazines was attempted. Material and Methods: One pot multi-component synthesis of Schiff’s base as new ligand an their complexes with Ni, Fe, Co and Cu and developed using 2-amino-4H-1,3 Oxazines /Thiazines and substituted Aldehydes, different catalyst are used to synthesize of 2-amino 4H-1,3 Oxazines. Its characterization is confirmed by taking IR, NMR spectra. The Schiff’s base act as ligand is bidentate, when it is treated to metal complexes in 1:1 ratio (metal: ligand) complexes are formed. Result: By using the bioactive molecules like 2-amino-4H-1, 3 Oxazine / Thiazines, Schiff’s Bases can be synthesized by using different aldehydes. These Schiff’s Bases has antitumor, antipyretic, anti-inflammatory property. And these Schiff’s bases treated with bioactive metals like Co, Fe, Cu, Zn which enhances their bio-activity. Conclusion: All these synthesized Schiff’ Bases and their metal complexes having bioactive properties.

scholarly journals Synthesis of New Substituted Tetrazole and 4-Thiazolidinone from Schiff's Bases

2020 ◽  
Vol 63 (1) ◽  
pp. 1-11
Author(s):  
Amena Alyas Ahmed ◽  
Natiq Ghanim Ahmed ◽  
Ahmad Khuder Ahmad
Keyword(s):  
Acetic Acid ◽  
13C Nmr ◽  
Nmr Spectra ◽  
Glacial Acetic Acid ◽  
Thioglycolic Acid ◽  
Absolute Ethanol ◽  
13C Nmr Spectra ◽  
Schiff’S Bases ◽  
Schiff's Bases ◽  
Tetrazole Derivatives

  The present work involved the synthesis of compound (1) (1-amino-4-methyl-6-phenyl pyrimidine- 2-(1H)-thione). This compound reacts with different aromatic aldehyde using glacial acetic acid as catalytic on absolute ethanol to give a new series of Schiff's bases (2-7). New thiazolidine-4-one were prepared from reactions of Schiff's bases (2,3,4,7) with thioglycolic acid in absolute ethanol giving compounds (8-11). Finally the preparation of new tetrazole derivatives (12-15) by reaction of Schiff's bases (2,3,4,7) with sodium azide in THF. The structure of the synthesized compounds are confirmed by I.R., 1H-NMR and 13C-NMR spectra and some physical  data.  

scholarly journals SYNTHESIS OF SOME NEW HETEROCYCLIC COMPOUNDS DERIVED FROM N-(Ñ-PHENYL GLYCYL) SACCHARIN AND STUDY THEIR BIOLOGICAL ACTIVITY

2018 ◽  
Vol 11 (10) ◽  
pp. 555
Author(s):  
Esraa M Ali ◽  
Ahmed W. Naser ◽  
Muthanna S. Farhan
Keyword(s):  
Acetic Acid ◽  
Schiff Bases ◽  
Heterocyclic Compounds ◽  
Glacial Acetic Acid ◽  
Cycloaddition Reaction ◽  
Aromatic Aldehydes ◽  
Positive Bacterium ◽  
Thiazole Derivatives ◽  
Gram Positive ◽  
Cyclic Imides

Objective: In the present work, a variety of new heterocyclic compounds namely aza-β- lactam, cyclicimides, 1,3-thiazole, and 1,2,4-triazole.Methods: Procedure includes the synthesis of aza-β- lactam, cyclic imides, 1,3-thiazole, and 1,2,4-triazole. The synthesis was carried out in eleven steps using N-(Ñ-substituted phenylglycyl) saccharin derivatives (1a,b) as a starting material and converted to benzoic acid derivatives (2a,b) and then to ester derivatives (3a,b), which finally convers to benzohydrazide derivatives (4a,b). The cyclization of (4a,b) with carbon disulfide and hydrazine hydrate (80%) in the presence of potassium hydroxide gives 1,2,4-triazole compounds (5a,b), and subsequently (5a,b) derivatives reacted with different aromatic aldehydes in the presence of few drops of glacial acetic acid to give Schiff bases (6a-f). Compounds (7a-b) was prepared by the reaction of compounds (4a,b) with chloroacetyl chloride. 1,3-thiazole derivatives (8a,b) were synthesized through the cyclization of compounds (7a,b) with thiourea. Schiff bases (9a-f) were obtained by condensation of (4a,b) with different aromatic aldehydes in the presence of few drops of glacial acetic acid. Aza-β-lactam compounds (10a-f) were prepared by the cycloaddition of Schiff-bases (9a-f) with phenyl isocyanate through [2+2] cycloaddition reaction. Reaction (4a,b) with various acid anhydrides in presence of acetic acid gave the corresponding cyclic imide (11a-f). The newly prepared.Results: The results showed that compounds (5a) and (10e) have a good activity against Gram-positive bacterium and no activity against Gram-negative bacterium, compared to standard drugs (ciprofloxacin and amoxicillin), while compounds (8a) and (6b) have a high activity against fungi, compared to standard drugs (metronidazole benzoate), and the other tested compounds have low-to-moderate activity.Conclusion: 1,2,4-triazole is a most potent assemblage of Gram-positive bacterium retardants and cyclic imides are a most potent assemblage of fungi retardants.

scholarly journals Synthesis of Bioactive Fluorinated 10H-Phenothiazines and their Sulfone Derivatives

2008 ◽  
Vol 5 (s1) ◽  
pp. 1063-1068 ◽  
Author(s):  
Yogesh Dixit ◽  
Rahul Dixit ◽  
Naveen Gautam ◽  
D. C. Gautam
Keyword(s):  
Hydrogen Peroxide ◽  
Acetic Acid ◽  
Spectroscopic Data ◽  
Halogen Atom ◽  
Glacial Acetic Acid ◽  
Present Communication ◽  
Smiles Rearrangement ◽  
Antimicrobial Studies ◽  
Sulfone Derivatives

The present communication deals with the synthesis of a series of fluorinated 10H-phenothiazines. 10H-phenothiazines is prepared by Smiles rearrangement of substituted 2-foramido-2´-nitrodiphenylsulfide. Substituted 2-foramido-2´-nitrodiphenylsulfide were obtained by the reaction of 2-amino-3-fluorobenzenethiol witho-halonitrobenzenes followed by formylation and 1-nitro/1-halo-10H-phenothiazines have been prepared by the reaction of substituted 2-aminobenzenethiols with reactiveo-halonitrobenzene containing a nitro group or halogen atom ato-position to the reactive halogen atom directly yielded 1-nitro/1-halo-10H-phenothiazines in situ. 10H-phenothiazine sulfone derivatives have been synthesized by the oxidation of 10H-phenothiazines by 30% hydrogen peroxide in glacial acetic acid. The structure of the synthesized compounds has been characterized by spectroscopic data and elemental analysis. Antimicrobial studies of the synthesized compounds have also been included.

scholarly journals Synthesis, Identification and Biological Activity of New Heterocyclic Compounds from Reaction of New Schiff-Bases with Phathalic Anhydride

2020 ◽  
Vol 8 (1) ◽  
pp. 12-18
Author(s):  
Alya A. Dawood ◽  
Shireen R. Mmohammed ◽  
Mohammed Mahmoud
Keyword(s):  
Acetic Acid ◽  
Schiff Bases ◽  
Heterocyclic Compounds ◽  
Mass Spectra ◽  
Glacial Acetic Acid ◽  
Biological Activities ◽  
Condensation Reaction ◽  
Aromatic Aldehydes ◽  
Heterocyclic Ring ◽  
Second Step

Series of new Schiff bases and their derivatives (Oxazepine) have been synthesized during two steps. The first step synthesis of imines derivatives (1-10) by the condensation reaction of 1, 7-diaminohepatane and 1,8-diaminooctane with different substituted aromatic aldehydes by using glacial acetic acid as catalyst. The second step includes reaction of the prepared Schiff bases derivatives with phathalic anhydride in dry benzene to obtain   seven-membered heterocyclic ring derivatives (11-15).  The biological activities of some prepared compounds were also studied against different kinds of bacteria. The new derivatives were confirmed by suing a range of experimental techniques including 1HNMR, 13C NMR, IR and Mass spectra.

Synthesis, characterization and biological activity of Pyrazoline derivatives

2021 ◽  
pp. 6223-6227
Author(s):  
Saras Kumar Jain ◽  
Rohit Singhal ◽  
Neetesh K. Jain
Keyword(s):  
Crystal Structure ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Acetic Acid ◽  
Biological Activity ◽  
Spectroscopic Data ◽  
Glacial Acetic Acid ◽  
Retardation Factor ◽  
Physical Parameters ◽  
Pyrazoline Derivative

Pyrazoline is dihydropyrazole having only one endocyclic double bond. Synthesis of pyrazoline derivatives from chalcones is an active arena of investigation due to established pharmacological result. In present study, chalcones were prepared by reacting of acetophenone with benzaldehyde. Then prepared chalcones react with isoniazid in the presence of glacial acetic acid results pyrazoline derivative. Physical parameters such as color, crystal structure, solubility, melting point, retardation factor (Rf) and % yield was evaluated. Confirmations of structures of all synthesized derivatives, were done by spectroscopic data of IR, 1HNMR and Mass spectroscopy. Also, all synthesized compounds were evaluated for antibacterial activity against B. subtilis, S. aureus, P.aeruginosa and E.coli, and antifungal activity was accomplished against C. albicans and A. niger at the different conc. and concluded that some compounds have excellent antimicrobial activity and most of the synthesized compounds exhibits moderate antimicrobial activity.

scholarly journals Synthesis and Antimicrobial Activity of Some 1-arylideneamino-4-(4-chlorobenzylidene)-2-methyl- 1H-imidazolin-5(4H)-one Compounds

2019 ◽  
Vol 35 (2) ◽  
pp. 822-828
Author(s):  
Cong Tien Nguyen ◽  
Dao Thi Hong Dinh ◽  
Thin Van Nguyen ◽  
Giang Duc Le ◽  
Hien Cao Nguyen
Keyword(s):  
Antimicrobial Activity ◽  
Hydrazine Hydrate ◽  
Spectral Data ◽  
1H Nmr ◽  
Aromatic Aldehydes ◽  
Antimicrobial Activities ◽  
Gram Negative Bacteria ◽  
Schiff’S Bases ◽  
Gram Negative ◽  
Schiff's Bases

4-Chlorobenzylidene-2-methyl-(4H)-oxazol-5-one, which were prepared from 4-chlorobenzaldehyde and acetylglycine in reaction with hydrazine hydrate in ethanol gave 1-amino-4-(4-chlorobenzylidene)-2-methyl-1H-imidazolin-5(4H)-one. However, treatment of 4-chlorobenzylidene-2-methyl-(4H)-oxazol-5-one with hydrazine hydrate in pyridine yielded 3-(4-chlorophenyl)propanohydrazide. Reaction of 1-amino-4-(4-chlorobenzylidene)-2-methyl-1H-imidazolin-5(4H)-one with aromatic aldehydes gave eight corresponding Schiff’s bases namely 1-arylideneamino-4-(4-chlorobenzylidene)-2-methyl-1H-imidazolin-5(4H)-ones. The structure of the 3-(4-chlorophenyl)propanohydrazide and the imidazoline-5-one compounds was confirmed by IR, 1H-NMR and MS spectral data. The Schiff’s bases were tested for antimicrobial activities against several strains of Gram-positive, Gram-negative bacteria, molds and yeasts.

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