Synthesis and In Vitro Anti-HIV Activity of Some New Schiff Base Ligands Derived from 5-Amino-4-phenyl-4H-1,2,4-triazole-3-thiol and Their Metal Complexes

2009 ◽  
Vol 184 (11) ◽  
pp. 2891-2901 ◽  
Author(s):  
Najim A. Al-Masoudi ◽  
Nazik M. Aziz ◽  
Abdulalah T. Mohammed
Author(s):  
AMAL M ALOSAIMI ◽  
INES EL MANNOUBI ◽  
SAMI A ZABIN

Objective: This work aimed at synthesizing tridentates asymmetrical Schiff base ligands containing sulfur atom and using them for preparing metal complexes with the iron triad metals. The prepared compounds were assayed in vitro for antimicrobial potential and in vivo molluscicidal activity. Methods: The unsymmetrical tridentate Schiff bases (SL1, SL2, and SL3) were prepared using 2-aminothiophenol as primary amine and condensed with 2-carboxybenzaldehyde, 2-hydroxy-1-naphthaldehyde, and 7-formyl-8-hydroxyquinoline. These ligands were used in preparing metal complexes with iron triad metals. The synthesized Schiff base ligands and their corresponding metal complexes were characterized and their proposed structures were confirmed using different physical and spectroscopic analytical techniques. All ligands and their corresponding metal complexes were assayed against different bacterial and fungal strains using the agar disk-diffusion technique. The molluscicidal activity was performed according to the standard reported methods as cited in the literature and by observing the toxicity and lethal dose according to the WHO guidelines. Results: The synthesized ligands behave as tridentate (NOS) ligands and form mononuclear complexes with the general formula [M(SL)2] with an octahedral geometry around the central metal ion. Metal complexes were non-electrolytic in nature. The in vitro antibacterial and antifungal examination results showed weak activity of the ligands, and there was enhanced activity with the complexes. The in vivo molluscicidal activity of the tested compounds showed good activity. Conclusion: The targeted compounds were prepared successfully, characterized, and showed some biological activity but lower than the standard reference drugs.


2011 ◽  
Vol 8 (s1) ◽  
pp. S245-S252 ◽  
Author(s):  
Praveen S. Mane ◽  
Sanjiv M. Salunke ◽  
Balagi S. More

The solid complexes of Cu(II), Ni(II), Co(II), Mn(II) and Fe(III) with Schiff base ligands derived from heterocyclic compounds 3-acetyl-6-methyl-(2H)-pyran-2,4(3H)-dione (Dehydroacetic acid) ando-chloroaniline were synthesized and characterized by elemental analysis, conductance, magnetic, thermal, UV-Vis and1H-NMR spectroscopy. The ligand field parameters have been evaluated for Cu(II), Ni(II), Co(II), Mn(II) and Fe(III) complexes which suggest an octahedral geometry for each of them. The magnetic moment and spectral data suggest the dimeric nature of Mn(II) complexes with octahedral geometry. The fungicidal activities of the ligands and their metal complexes have been screened in vitro againstAspergillus nigerand the percentage inhibition of the metal complexes is found to be increased considerably then that of their corresponding ligands and the order is Cu>Ni>Fe>Mn>Co.


2010 ◽  
Vol 75 (8) ◽  
pp. 1075-1084 ◽  
Author(s):  
Muhammad Imran ◽  
Mitu Liviu ◽  
Shoomaila Latif ◽  
Zaid Mahmood ◽  
Imtiaz Naimat ◽  
...  

The condensation reactions of biacetyl with orthohydroxyaniline and 2-aminobenzoic acid to form bidendate NO donor Schiff bases were studied. The prepared Schiff base ligands were further utilized for the formation of metal chelates having the general formula [ML2.2H2O] where M = Co(II), Ni(II), Cu(II) and Zn(II) and L = HL1 and HL2. These new compounds were characterized by conductance measurements, magnetic susceptibility measurements, elemental analysis, and IR, 1H-NMR and electronic spectroscopy. Both Schiff base ligands were found to have a mono-anionic bidentate nature and octahedral geometry was assigned to all metal complexes. All the complexes contained coordinated water which was lost at 141-160 ?C. These compounds were also screened for their in-vitro antibacterial activity against four bacterial species, namely; Escherichia coli, Staphylococcus aureus, Salmonella typhi and Bacillus subtillis. The metal complexes were found to have greater antibacterial activity than the uncomplexed Schiff base ligands.


2008 ◽  
Vol 61 (4) ◽  
pp. 288 ◽  
Author(s):  
Lei Shi ◽  
Rui-Qin Fang ◽  
Jia-Yu Xue ◽  
Zhu-Ping Xiao ◽  
Shu-Hua Tan ◽  
...  

The synthesis of 16 metal complexes from four Schiff bases prepared from 5-chloro-2-hydroxybenzaldehyde and primary amines has been described. The synthesized Schiff base ligands and their complexes were characterized by elemental analyses, spectroscopic (UV, IR, 1H and 13C NMR, electrospray ionization-mass spectrometry) methods, and magnetic and conductance measurements. Furthermore, complexes 1a, 1b, 3d, 4a, and 4d were characterized by X-ray diffraction analysis. After the structural characterization, all the compounds were tested in vitro for their antibacterial (Bacillus subtilis, Escherichia coli, Pseudomonas fluorescens, and Staphylococcus aureus) activities. The cytotoxic activities of the synthesized compounds were evaluated in vitro against human chronic myeloid leukaemia cells (K562) and a human nasopharyngeal epidermoid tumour cell line. The results indicated that most of the complexes showed good cytotoxic activity against human cancer cell lines but weak cytotoxic activity against a human normal cell line (L02). Among the compounds tested, the cobalt complexes 1a, 2a, 3a, and 4a showed the most favourable antibacterial and cytotoxic activities.


2020 ◽  
Vol 18 (1) ◽  
pp. 591-607
Author(s):  
Hanan A. Althobiti ◽  
Sami A. Zabin

AbstractThe purpose of this work was to prepare Schiff base ligands containing quinoline moiety and using them for preparing Cu(ii) and Zn(ii) complexes. Four bidentate Schiff base ligands (SL1–SL4) with quinoline hydrazine scaffold and a series of mononuclear Cu(ii) and Zn(ii) complexes were successfully prepared and characterized. The in vitro antibacterial and antifungal potential experimentation revealed that the ligands exhibited moderate antibacterial activity against the Gram-positive bacterial types and were inactive against the Gram-negative bacteria and the fungus strains. The metal complexes showed some enhancement in the activity against the Gram-positive bacterial strains and were inactive against the Gram-negative bacteria and the fungus strains similar to the parent ligands. The complex [Cu(SL1)2] was the most toxic compound against both Gram-positive S. aureus and E. faecalis bacteria. The in silico physicochemical investigation revealed that the ligand SL4 showed highest in silico absorption (82.61%) and the two complexes [Cu(SL4)2] and [Zn(SL4)2] showed highest in silico absorption with 56.23% for both compounds. The in silico pharmacokinetics predictions showed that the ligands have high gastrointestinal (GI) absorption and the complexes showed low GI absorption. The ligands showed a good bioavailability score of 0.55 where the complexes showed moderate to poor bioavailability.


2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Ramesh S. Yamgar ◽  
Y. Nivid ◽  
Satish Nalawade ◽  
Mustapha Mandewale ◽  
R. G. Atram ◽  
...  

The synthesis and antimicrobial activity of novel Zn(II) metal complexes derived from three novel heterocyclic Schiff base ligands 8-[(Z)-{[3-(N-methylamino)propyl]imino}methyl]-7-hydroxy-4-methyl-2H-chromen-2-one, 2-[(E)-{[4-(1H-1,2,4-triazol-1-ylmethyl)phenyl]imino}methyl]phenol, and (4S)-4-{4-[(E)-(2-hydroxybenzylidene)amino]benzyl}-1,3-oxazolidin-2-one have been described. These Schiff base ligands and metal complexes are characterised by spectroscopic techniques. According to these data, we propose an octahedral geometry to all the metal complexes. Antimicrobial activity of the Schiff base ligand and its metal complexes was studied against Gram negative bacteria:E. coliandPseudomonas fluorescens, Gram positive bacteria:Staphylococcus aureus,and also against fungi, that is,C. albicansandA. niger. Some of the metal complexes show significant antifungal activity (MIC < 0.2 μg/mL). The “in vitro” data has identified [Zn(NMAPIMHMC)2]·2H2O, [Zn(TMPIMP)2]·2H2O, and [Zn(HBABO)2]·2H2O as potential therapeutic antifungal agents againstC. albicansandA. niger.


2018 ◽  
Vol 69 (7) ◽  
pp. 1678-1681
Author(s):  
Amina Mumtaz ◽  
Tariq Mahmud ◽  
M. R. J. Elsegood ◽  
G. W. Weaver

New series of copper (II), cobalt (II), zinc (II), nickel (II), manganese (II), iron (II) complexes of a novel Schiff base were prepared by the condensation of sulphadizine and pyridoxal hydrochloride. The ligand and metal complexes were characterized by utilizing different instrumental procedures like microanalysis, thermogravimetric examination and spectroscopy. The integrated ligand and transition metal complexes were screened against various bacteria and fungus. The studies demonstrated the enhanced activity of metal complexes against reported microbes when compared with free ligand.


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