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Synthesis of New Cephalosporins of Expected Improved Activity and Resistance Against -Lactamases
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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.

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Publication Date
Sat Jan 01 2022
Journal Name
Journal Of Pharmaceutical Negative Results
Synthesis, Characterization and Study Electrical Conductivity of New Poly Thiadizole Derivatives, Silica Nanocomposites
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Heterocyclic polymers / silica nanocomposite one of important materials because of excellent properties such as thermal , electrical , and mechanical properties , so that hybrid nanomaterial are widely used in many fields, in this paper nanocomposite had prepared by modification of silica nanoparticals by using acrylic acid and functionalized the surface of nanoparticles, and using free Radical polymerization by AIBN as initiators and anhydrous toluene as solvent to polymerize functionalize silica nanoparticles with heterocyclic monomers to prepare heterocylic polymers / silica nanocomposite and study electrical conductivity , The nanocomposite which had prepared characterized by many analysis technique to study thermal properties such

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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of New Opioid Analgesic Peptide Analogues to Enkephalin (Leucine- and Methionine-Enkephalin)
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A small number of researches were done in the design and synthesis of enkephalin analogues that are able to resist degradation effect of proteolytic enzymes with good bioavailability and half-lives.Through studying structure activity relationships we tried to incorporate phthalyl group, tryptophan and lysine amino acids in different positions in the basic backbone structure of the naturally occurring opioid Leu5- and Met5- enkephalin, in the hope that such insertion of these amino acids could induce interesting addition in the biological activity of these analogues with enhancement of their bioavailability, in addition to decrease side effects as addiction liability.

These synthesized peptides are:

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    Publication Date
    Sun Dec 04 2016
    Journal Name
    Baghdad Science Journal
    A study of anti fungal activity of a combination of essential oils from medical herbs against water molds
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    The aim of this study is to evaluate the anti fungal activity of a combination of essential oils against water molds. HPLC analysis was done to evaluate the quantity and quality of the active compounds in this combination which extracted from three herbs( Peppermint Menthapiperita ,Thyme Thymusvulgaris, Common sage Salvia officinalis L.) and the active compounds are Camphor,Menthol,,Thujone and Thymol with different concentrations. In this study (MIC) , (MFC) were measured and (LD50) determined after 48,96 h from fingerlings treatment of common carp in aquariums .The results of (MIC) were 0.025µl/ml for Aphanomyces sp. and 0.015µl/ml for both Achlya sp. and Fusariumsolani which showed significant differences(p<0.05) from Malachite gre

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    Publication Date
    Thu Feb 16 2023
    Journal Name
    Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
    Evaluation of Antileishmanial Activity of Osteospermum ecklonis Extract of Aerial Parts against Leishmania donovani: in vitro(Conference Paper) #
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    Abstract

     

    Lack of safe available non-resistant treatment for visceral leishmaniasis (Kala-azar) keeps limiting the complete cure of this disease ,drugs that have  toxic side effects or lack of effectiveness  have led to disease relapse ,all these factors have lightened  the way to the search for imperative drugs from natural resources that have been shown to have antileishmanial activity through literature survey

    . In the present study, the comparative in vitro anti-leishmania activity of various fractions of Osteospermum ecklonis aerial parts fractions have been evaluated. Extracts were prepared through maceration and Soxhlet apparatus using 85% meth

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    Publication Date
    Thu Jun 01 2023
    Journal Name
    Baghdad Science Journal
    Synthesis and Characterization of Some New Pyridine and Pyrimidine Derivatives and Studying Their Biological Activities
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    Heterocyclic systems, which are essential in medicinal chemistry due to their promising cytotoxic activity, are one of the most important families of organic molecules found in nature or produced in the laboratory. As a result of coupling N-(4-nitrophenyl)-3-oxo-butanamide (3) using thiourea, indole-3-carboxaldehyde, or piperonal, the pyrimidine derivatives (5a and 5b) were produced. Furthermore, pyrimidine 9 was synthesized by reacting thiophene-2-carboxaldehyde with ethyl cyanoacetate and urea with potassium carbonate as a catalyst. The chalcones 11a and 11b were synthesized by reacting equal molar quantities of 1-naphthaldehy

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    Publication Date
    Thu Jan 15 2009
    Journal Name
    Ibn Al-haitham Jour. For Pure & Appl. Sci.
    Synthesis of 3-C-Spiro Ring Nucleoside Analogues, of Possible Biological Activity
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    In this study, new derivatives of 3-C-spiro ring nucleoside analogues were synthesized. The structures of these derivatives were characterized by infrared spectroscopy,1 HNMR (some of them) and elemental analysis. The nucleoside derivatives were tested for inhibition of E-coli and were all found to be active.

    Publication Date
    Thu Jul 01 2021
    Journal Name
    International Journal Of Drug Delivery Technology
    Synthesis and Diagnosis of Some Derivatives of 1,2,4-Triazole-3-Dicarboxylic Acid and Study their Biological Activity
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    Newly prepared derivatives of Heterocyclic of dicarboxylic acid include 1, 2, 4-Triazoledicarboxylic acid. Thiocarbohydrazine (TCH) reacts with aliphatic and aromatic dicarboxylic acids, and when these resulting compounds interact with compounds containing a group of carbonyl they result in Schiff base, which are very important in the industrial and medical fields and the acids used (oxalic acid, succinic, terephthalic) to prepare the triazole, then the reaction with Para-chlorobenzendihaide. and some physical properties were measured for these products. The biological activity of the prepared compounds has been studied, and it has been shown that they have different effects on the bacteria, compounds prepared with Fourier Transform Infrare

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    Scopus
    Publication Date
    Sun Dec 15 2019
    Journal Name
    Journal Of Global Pharma Technology
    synthesis and characterization of heterocyclic compounds and polymers with studying the biological activity for some of them
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    This paper deals with the preparation of new monomers and polymers which including heterocyclic unit. The diacid chlorides compounds [1-3] were prepared from the reaction of glutaric acid, adipic acid, terephthalic acid with thionyl chloride. Succinic acid reacted with ethanol to produce compound [4]. Compound [4] reacted with hydrazine hydrate to obtain succinic hydrazide [5].Compound [5] reaction with CS2 and KOH in absolute ethanol to produce compound [6].The polymers [7-12] have been created by reacting diacid chlorides compounds [1-3] with compound[5] or [6] in dry pyridine with some drops of DMF. The topology of produced compounds has characterized through their spectral and analytical data as in FT-IR spectra, Thermal analysis [DSC,

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    Scopus
    Publication Date
    Mon Jan 01 2024
    Journal Name
    5th International Conference On Biomedical And Health Sciences
    Exploiting Vpusm 8 Lytic Phage for The Bio- Control of V. Cholerae: A Novel Approach Against Cholera in The Era of Antibiotic Resistance
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    Objective: The purpose of this study was to assess the effectiveness of Vibriophage Universiti Sains Malaysia 8 (VPUSM 8), a bacteriophage that destroys bacteria, in managing the proliferation of Vibrio cholerae, specifically the El Tor serotype, as an alternate therapeutic strategy. Methods: The study entailed subjecting water samples from Kelantan, Malaysia, to reproduce the natural circumstances that promote the growth of V. cholerae. Subsequently, the samples were contaminated with the V. cholerae O1 El Tor Inaba strain and treated using VPUSM 8. The study employed a controlled experimental design, wherein the samples were divided into three groups, each experiencing different treatment methods. Quantifying the number of colony-

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    Publication Date
    Mon Dec 30 2024
    Journal Name
    Wasit Journal For Pure Sciences
    Synthesis, Structural Investigation and Biological Activity of a Heterocyclic Schiff-Base Ligand and Its Coordination Complexes
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    This study reports the formation, characterisation and biological evaluation of a Schiff base ligand and its corresponding metal complexes. The Schiff base ligand (HL) was prepared through a condensation reaction involving isonicotinohydrazide and N'-((1R,2R,4R,5S, E)-2,4-bis(4-chlorophenyl)-3-azabi cyclo[3.3.1]nonan-9-ylidene) isonicotinohydrazide (M) in EtOH solvent and (3-5) drops of conc. HCl. The interaction of HL with selected metal chlorides including Mn(+2), Co(+2), Ni(+2), Cu(+2) and Zn(+2) in a 2:1 (L:M) mole ratio resulted in the synthesis of complexes with the general formula [M(HL)Cl2] (where: M = Mn(+2),Co(+2) and Ni(+2)) and [M`(HL)Cl2] (where M` =  Cu(+2) and Zn(+2)). The characterisation of the prepared compounds w

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