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Synthesis and Preliminary Antimicrobial Study of 2-Amino-5-Mercapto-1,3,4-Thiadiazole Derivatives
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Nitrogen heterocycles are of a special interest because they constitute an important class of natural and non natural products, many of which exhibit useful biological activities.Among these nitrogen heterocycles are 1, 3, 4-thiadiazole containing compounds. The therapeutic effects of these derivatives have been well studied for a number of pathological conditions including inflammation, pain, or hypertension. Moreover, synthesis of thiadiazoles has attracted wide-spread attention due to their diverse applications as antibacterial, anticancer, antifungal anti-inflammatory and antidepressant agents.According to this information’s new derivatives of 1, 3, 4-thiadiazole were designed and synthesized and in the hope of having some activities as antibacterial and antifungal. These are:

  • 4-(((5-mercapto-1,3,4-thiadiazol-2-yl)imino)methyl)-2-methoxyphenol.
  • Tert-butyl (1- ((2- ((5- (methylsulfonyl) -1,3,4- thiadiazol-2-yl) amino) -2- oxoethyl)amino) -1-oxopropan - 2-yl) carbamate.

Key words: 1, 3, 4-thiadiazole, biological activity, peptides, Schiff base.

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Publication Date
Thu Apr 20 2023
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis a Novel Complexes of VO(II),Mn(II),Fe(II) ,Co(II), Ni(II), Cu(II)and Pt(IV) Derived from Schiff’s Base of Pyridoxal and 2-amino-4-nitrophenol and Study their Biological Activates
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This work describes the synthesis of novel ligand (H2L2) (4-((2-hydroxy-5-nitrophenyl)imino)methyl)-5(hydroxymethyl)-2methylpyridin-3-ol)  type (NOO) donor atoms. When it coordinates with metal ions[V2+,Mn2+,Fe2+,Co2+,Ni2+,Cu2+and Pt4+] with the general formula K2[M(L2)2].XH2O and K2[VO(L2)(OSO3)].H2O . This ligand can form tridentate structures. The ligand was synthesized from the reaction of pyridoxal hydrochloride with 2-amino-4-nitrophenol in ethanol (as a solvent) at a mole ratio of 1:1 and thoroughly mixed and refluxed for 6-8  hrs . The reaction

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Publication Date
Thu Dec 29 2016
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis of Barbiturate Derivatives of D-Erythroascorbic Acid
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 The   aim  of   this   work   is   the   synthesis  of   new   derivatives  of   barbiturate   of  D-erythroascorbic acid. To obtain these derivatives, the 5,6-O-isopropylidene-L-ascorbic acid (4) was chosen, which was prepared from the reaction of L-ascorbic acid (3) as a starting material with dry acetone in the presence of hydrogen chloride. The esterification of hydroxyl groups at C-2 and C-3 positions with excess of benzoyl chloride in dry pyridine was obtained compound (5). Hydrolysis for compound (5) in acetic acid (65%) gave the compound (6). Oxidation of the product (6) with sodium periodate results an Al

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Publication Date
Tue Sep 19 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis of New Derivatives of P­ Lactam Antibiotics
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New    Derivatives    for   Known    P-   Jactam  antibiotics   were

synthesized  utilizing  the  free  amino  group  pres nt  in  the  parent compounds as the site for derivatization. The objectives for this study

are to have new compounds which could have an increased potential resistance to the degradative enzymes knowing to be able to destroy

the antibacterial activity of 13· lactam antibiotics- Besides. these new

derivatives  could  be  congeners  of     known  agents,  or  may  be  a

pott:ntial pro-drugs for thes

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Publication Date
Mon Jan 30 2023
Journal Name
Iraqi Journal Of Science
Synthesis, Characterization of Some Thiourea Derivatives Based on 4-Methoxybenzoyl Chloride as Antioxidants and Study of Molecular Docking
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     Ten new thiourea derivatives 1-10 were prepared in this work using a two-step process that involved reacting 4-methoxybenzoyl chloride with KSCN to afford 4-methoxybenzoyl isothiocyanate. This was followed by reaction with various amines (primary amines, secondary amines, and diamines) to give the aforementioned title products 1-10. These products were characterized by FT-IR, 1H NMR and 13C NMR spectroscopy. Using the DPPH scavenging method, the antioxidant activity of thiourea products was investigated, and derivative 8 had the greatest antioxidant activity in comparison to the other derivatives. Moreover, molecular dockin

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Publication Date
Sun Mar 04 2012
Journal Name
Baghdad Science Journal
Synthesis of New Mannich Bases from Indole Derivatives
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This work includes two steps of synthesis, the first one is the synthesis of indole which was prepared according to literature of the reaction of phenyl hydrazine with acetaldehyde in glacial acetic acid afforded phenyl hydrazone of acetaldehyde , this product was fused with zinc chloride to give the indole.Reaction of cyclohexanone with phenyl hydrazine using the same procedure for the preparing giving 1,2,3,4-Tetrahydrocarbazole.Second step involved synthesis of a series of (17) of mannich bases derivatives of indole and 1,2,3,4-Tetrahydrocarbazle. Mannich reaction involves the condensation of aldehyde usually formaldehyde with different secondary amine and with compound containing an activated hydrogen.The reaction illustrated by the fo

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis, Characterization of Derivatives Tetrazoles for Trimethoprim Drug
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The present work involved synthesis of serval new substituted tetrazole via Schiff bases for trimethoprim drug by two steps. The first step involved direct reaction of different ketones and aldehydes with trimethoprim producing the corresponding Schiff bases (1-10), whereas the second step, involved preparation new tetrazoles derivatives (11-20) through reaction of the ready Schiff bases (in the first step) with sodium azidein in dioxin. The prepared compounds were characterized by UV, FT-IR, and some of them by 13C-NMR, 1H-NMR spectroscopy and physical properties.

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Publication Date
Fri Jul 05 2013
Journal Name
Pharmacie Globale International Journal Of Comprehensive Pharmacy
SYNTHESIS OF NEW PROPRANOLOL DERIVATIVES AS POSSIBLE PRODRUGS
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Propranolol is a nonselective-adrenergic blocker used in the treatment of hypertension, cardiac arrhythmias, and angina pectoris. A significant problem in propranolol therapy is that it undergoes extensive presystemic metabolism after oral administration leading to reduced bioavailability. In this study, two new propranolol derivatives have been designed, synthesized and characterized. These compounds were formed by acylation of propranolol followed by nucleophilic substitution reaction of acylated propranolol, these derivatives were analyzed for IR, CHN, melting points, and evaluated for their lipophilic properties compared with propranolol. The lower partition coefficient of these two derivatives revealed that the prodrug approach may be

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Publication Date
Sun Apr 14 2019
Journal Name
International Journal Of Pharmaceutical Research
Synthesis, Characterization and Antibacterial of Some New 4,4-(pyridine-2,6-diylbis(1,3,4-oxadiazole-5,2-diyl))bisphenol Polymer
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4, 4s (pyridine 2, 6 diylbis (1, 3, 4 oxadiazole 5, 2 diyl)) bisphenol monomer (3) was synthesized from cyclization of Ns2, Ns6 bis (4 hydroxybenzylidene) pyridine 2, 6 dicarbohydrazide (2) in the presence of bromine in glacialacetic acid. Newly five polymers (P1P5) 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.

Publication Date
Sat Dec 01 2012
Journal Name
Journal Of Al-nahrain University Science
Synthesis and Characterization of Some Metals Complexes of {N-[(Benzoyl Amino)-Thioxo Methyl] Proline}
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Publication Date
Tue Nov 14 2006
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
[PDF] من iasj.net Synthesis and Characterization of Some New Transition Metal Complexes of Amino
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الوصف New complexes of Cu (ll), Ni (II)„Co (II), and Zn (ll) with 2-amino-5-p-Flouro Phenyl 1, 3, 4-Thiadiazole have been synthesized. The products were isolated, studied and characterized by physical measurements, ie,(FT-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