Preferred Language
Articles
/
bijps-386
Synthesis of New Cephalosporins of Expected Improved Activity and Resistance Against -Lactamases
...Show More Authors

The development of new cephalosporins with improved activity against resistant microbes, such as, MRSA (methicillin resistant Staph. aureus), P. aeruginosa, is of high potential. Chemical synthesis of two new series of thiadiazole linked to cysteine (series 1) and cephalosporins containing thiadiazole linked to cysteine through disulfide bond (series 2) were achieved. The chemical structures of the synthesized compounds were confirmed using spectral (FT-IR, 1H-NMR) and elemental microanalysis. The incorporation of privileged chemical moieties, such as, thiadiazole, Schiff base, cysteine and sulfonamide, has been found to have great contribution to the antimicrobial activities. Compounds of series 1 (1b-d), containing a Schiff base or a sulfonamido moiety, showed reasonable activity and were less potent than cephalexin with respect to E. coli and Staph. aureus. The new cephalosporins (series 2) showed remarkable activities on E. coli (62.5-15.6µg/ml) and staph. aureus (31.2-62.5µg/ml) when compared with cephalexin (250 and 125 µg/ml) respectively. Moreover, compounds 1 and 3 showed very promising activity against MRSA (250 and 500µg/ml) respectively. The incorporation of a sulfonamido moiety to the cephalosporin molecule was successfully achieved. This is a very interesting finding which may open a new approach in the synthesis of newer cephalosporins.   

Keywords: Cephalosporins, Cysteine, Schiff base, Sulfonamides, Thiadiazole.

Crossref
View Publication Preview PDF
Quick Preview PDF
Publication Date
Mon Dec 05 2016
Journal Name
Iraqi
Synthesis, spectroscopic and Antibacterial activity study of N-]2(2-phenyl hydrazinyl) phenyl benzothiazol-2-amine complexes.
...Show More Authors

Publication Date
Wed Mar 29 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of Coumarin Derivatives Coupled to Amino Acid Esters and Studying their Biological Activity as Antimicrobial Agents
...Show More Authors

A series of coumarin derivatives linked to amino acid ester side chains were synthesized and evaluated of their antibacterial and antifungal activity. The coumarin derivatives was alkylated by the ethyl bromoacetate and then using potassium carbonate to get alkylated hymecromone. Conventional solution method for amide bond formation was used as a coupling method between the carboxy-protected amino acids with acetic acid side chain of coumarin derivatives. The DCC/ HOBt coupling reagents were used for peptide bond formation. The proposed analogues were successfully synthesized and their structural formulas were consistent with the proposed struct

... Show More
View Publication Preview PDF
Crossref
Publication Date
Wed Jan 01 2020
Journal Name
Biochemical & Cellular Archives
ECO-FRIENDLY SYNTHESIS OF MAGNESIUM OXIDE NANOPARTICLES USING FICUS BENGHALENSIS LEAF EXTRACT AND ITS ANTI-LEISHMANIASIS ACTIVITY
...Show More Authors

Scopus (5)
Scopus
Publication Date
Fri Mar 01 2024
Journal Name
Baghdad Science Journal
First Transition Metal Complexes Salts of Diazonium Derived from Nitrogen Heterocyclic Compound, Synthesis, Characterization and Biological Activity
...Show More Authors

Metal complexes chrome(III), manganese(II), iron(III), cobalt(II), nickel(II), cupper(II) and zinc(II) with diazonium of 3-amino-2-chloropyridine of general formula [2-Cl-C5H3N≡N]n[MXm], where n=2 or 3 for divalent and trivalent metal, m= 4 or 6  were synthesized. The complexes have been characterized by flame atomic absorption, (C.H.N), molar conductance, magnetic susceptibility UV-vis spectra, infrared spectra,1H-NMR spectroscopy and thermo gravimetric analysis (TGA and DTA). The measurements showed that the divalent metal ion complexes (M2+) have (1:2) M:L ratio with tetrahedral geometry around metal ions while the trivalent metal ions (M3+) formed (1:3) m

... Show More
View Publication Preview PDF
Scopus Crossref
Publication Date
Sat Nov 10 2018
Journal Name
Oriental Journal Of Chemistry
New Series of Substituted Heterocyclics Derived from α , β – Unsaturated Ketone and Their Cytotoxic Activity Tumor Cell Lines
...Show More Authors

The aldol condensation of 2-acetylnaphthalene with 9-anthracene carboxaldehyde afforded α, β-unsaturated keton (1) . New heterocyclic compounds containing: cyclohexenone[2], indazole[3], pyrimidinethion [4], thiazolo fused pyrimidine[5], isoxazoline[6], substituted pyrazoline[7]a-d and pyrimidinone[8] rings system were synthesized from α, β-unsaturated keton[1]. Cyclization of [1] with ethylacetoacetate gave the mentioned heterocycle cyclohexanone [2]. The cyclo condensation of [2] with hydrazine gave the new indazole derivative [3]. furthermore, the reation of [1]with thiourea gives thiopyrmidine derivative [4]. The cyclo condensation of [4] with chloroacetic acid gave the fused rings [5]. Then reacted compound[1] with hydroxy

... Show More
View Publication Preview PDF
Crossref (1)
Clarivate Crossref
Publication Date
Mon Sep 11 2006
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis a nd Characterization of Some New Transition Metal Complexes of Amino Thiadiazole
...Show More Authors

New complexes of Cu (ll), Ni (ll), Co (ll), and Zn (ll) wi th 2-amino-5-p-Fiouro Phenyl 1, 3, 4-Thiadiazole have been synthesized. The products were isolated, studied and characterized by physical measurements, ie,(Ff-IR), UV-Vis and the melting points were determined. The new Schiff base (L) has been used to prepare some complexes. The prepared complexes were identified and their structural geometry were suggested

Publication Date
Thu Jun 30 2022
Journal Name
International Journal Of Drug Delivery Technology
New Metal Complexes Derived from Heterocyclic Schiff-base Ligand; Preparation, Structural Investigation and Biological Activity
...Show More Authors

The formation of a Schiff-base with N2O2 donor atoms derived from the hydrazine segment and its metal complexes are reported. The Schiff-base ligand; N’-((1R,2S,4R,5S,Z)-2,4-diphenyl-3-azabicyclo[3.3.1]nonan-9-ylidene)furan-2-carbohydrazide (HL) was prepared from the reaction of furan-2-carbohydrazide with (1R, 2R, 4R, 5S)-2,4-diphenyl-3-azabicyclo[3.3.1]nonan-9-one (M1) in ethanol medium. The reaction of the title ligand with selected metal ions Cr(III), Mn(II), Ni(II), Cu(II), Zn(II) and Cd(II) gave complexes with the general formula [M(L)Cl2], (where: M = Cr(III), Mn(II), Ni(II), Cu(II), Zn(II) and Cd(II)). Spectroscopic analyses Fourier transform infrared (FT-IR), Nuclear Magnetic Resonance (NMR) Carbon-13 nuclear magnetic res

... Show More
View Publication
Scopus (6)
Crossref (3)
Scopus Crossref
Publication Date
Thu Mar 19 2015
Journal Name
Thesis
AN IMPROVED AES ENCRYPTION OF AUDIO WAVE FILES
...Show More Authors

The main objective of this study is to get a secure broadcasting in real time applications for audio files (precisely the Wave type) and to increase the degree of complexity of the encrypt/decrypt arithmetic operations in the finite . field GF(28) on these files. This objective can be achieved by implementing different proposed architectures, methods and algorithms both in block and stream cipher structure to increase the degree of complexity. For high utilization of resources and fast execution time of operations in cryptographic processes in the proposed cryptographic algorithms, the parallel computing was implemented by using OpenMP directives. The AES Rijndael algorithm has been considered as a base for the developed algorithms in the b

... Show More
Publication Date
Wed Sep 02 2020
Journal Name
International Journal Of Drug Delivery Technology
Synthesis of Levofloxacin Derivatives with some Amines and their Complexes with Copper(II) Salts and Evaluation of their Biological Activity
...Show More Authors

Levofloxacin belongs to the fluoroquinolone family; it is a potent broad-spectrum bactericidal agent. The pharmacophore required for significant antibacterial activity is the C-3 carboxylic acid group and the 4-pyridine ring with the C-4 carbonyl group, into which binding to the DNA bases occur. In this work, we tried to show that by masking the carboxyl group through amide formation using certain amines to form levofloxacin carboxamides, an interesting activity is kept. Levofloxacin carboxamides on the C-3 group were prepared, followed by the formation of their copper complexes. The target compounds were characterized by FT-IR, elemental analysis. The antimicrobial activity of the target compounds was evaluated and showed satisfactory resu

... Show More
Publication Date
Sun Dec 25 2022
Journal Name
International Journal Of Drug Delivery Technology
Synthesis of Few New Carrier Polymers Derived from 2-hydrazinylbenzo[d]thiazole
...Show More Authors

2-hydrazinylbenzo[d]thiazole compound [1] is produced from reaction of 2-mercapto-benzothiazole with hydrazine hydride in ethanol. Compound [1] reacted with maleic anhydride in DMF to produce (Z)-4-(2-(benzo[d] thiazol-2yl) hydrazinyl)-4-oxobut-2-enoic acid [compound (2)]. While the treatment of compound [2] with the ammonium persulfate (NH4)2S2O8 (as the initiator) in order to produce compound [3], then compound [3] reacted with thionyl chloride in benzene to produce compound [4], finally compound [4] reaction with various drugs: cephalexin, amoxicillin, sulfamethizole, elecoxib obtained polymers [5–8]. The structure of synthesized compounds identified by spectral data: fourier transform infrared (FTIR) and proton nuclear magneti

... Show More
View Publication Preview PDF
Scopus (6)
Crossref (3)
Scopus Crossref