Publications by authors named "Atef Kalmouch"

6 Publications

  • Page 1 of 1

Synthesis, Characterization, and Anti-diabetic Activity of Some Novel Vanadium-Folate-Amino Acid Materials.

Biomolecules 2020 05 18;10(5). Epub 2020 May 18.

Department of Chemistry, Faculty of Science, Taif University, P.O. Box 888, Al-Hawiah, Taif 21974, Saudi Arabia.

A new six intraperitoneal injections insulin-mimetic vanadyl(IV) compounds [(VO)(FA)(AA)] (where n = 1-6: AA = isoleucine, AA = threonine, AA = proline, AA = phenylalanine, AA = lysine, and AA = glutamine) were synthesized by the chemical reactions between folic acid (FA), VOSO, and amino acids (AA) with equal molar ratio 1:1:1 in neutralized media. These complexes were characterized by elemental analysis and estimation of vanadyl(IV) metal ions. The thermal stability behavior of these complexes was studied by TG-DTG-DTA analyses. The structures of these complexes were elucidated by spectroscopic methods like infrared, electron spin resonance (ESR), and solid reflectance spectroscopes. The powder X-ray diffraction (XRD) study suggested the crystalline nature of the complexes. Magnetic moments and electronic spectra revealed the square-pyramid geometrical structure of the complexes. The conductivity results refereed that all synthesized vanadyl(IV) complexes were of a non-electrolyte behavior. The infrared spectra assignments of these complexes revealed that the FAH and AA chelates act as a bidentate ligation. The chelation towards vanadyl (IV) ions existed via deprotonation of one of the carboxylic groups of FAH drug ligand, and so amino acids act as bidentate ligands via N-amino and O-carboxylate groups. Both scanning and transmission electron microscope (SEM and TEM) techniques were used to investigate the surface morphology. The main task of this research is the aim of designing a new insulin alternative antidiabetic drug agent. The antidiabetic efficiency of these complexes was evaluated in streptozotocin-induced diabetic male albino rats. Liver and kidney functions, insulin and blood glucose levels, lipid profile, and superoxide dismutase antioxidant (SOD) are verified identifiers for the efficiency of VO(IV)/FA/AA system compounds as antidiabetic drug agents.
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http://dx.doi.org/10.3390/biom10050781DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7277503PMC
May 2020

Synthesis, characterization and antidiabetic effects of vanadyl(II) adenosine monophosphate amino acid mixed-ligand complexes.

Future Med Chem 2019 Jan 15. Epub 2019 Jan 15.

Department of Chemistry, College of Science, Princess Nourah bint Abdulrahman University, Riyadh 11671, Saudi Arabia.

Aim: This research paper is aimed at designing a novel insulin alternative for the treatment of diabetes.

Materials & Methods: Six novel vanadyl(II) compounds, [(AMP)(VO)(AA )]·NH , were synthesized from an equimolar ratio of adenosine monophosphate, VOSO and amino acids (AA ).

Results: The magnetic moments and electronic spectra revealed the square pyramidal geometrical structure of the complexes. In an in vivo study, the insulin levels, blood glucose levels, lipid profiles and histology of the pancreas and liver of the animals treated with the complexes were similar to those of healthy control animals, unlike the untreated and vanadyl sulfate(II)-treated diabetic ones.

Conclusion: The data gathered in the current research illustrated that vanadyl(II)-AMP-amino acid (AA) mixed-ligand complexes can function as antidiabetic agents.
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http://dx.doi.org/10.4155/fmc-2018-0471DOI Listing
January 2019

Synthesis, antibacterial properties and 2D-QSAR studies of quinolone-triazole conjugates.

Eur J Med Chem 2018 Jan 16;143:1524-1534. Epub 2017 Oct 16.

Department of Chemistry & Physics, Augusta University, Augusta, GA 30912, USA. Electronic address:

A set of 1,2,3-triazole incorporated quinolone antibiotic conjugates 10-15, 17-19 were synthesized via microwave assisted click chemistry technique. Some of the aryl-substituted conjugates 17-19 show promising antibacterial properties against the tested Gram-positive (S. aureus and S. pyogenes) and Gram-negative bacteria (S. typhi) with potency higher than that of the parent antibiotics 1-3. 2D-QSAR modeling supports the observed biological properties.
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http://dx.doi.org/10.1016/j.ejmech.2017.10.042DOI Listing
January 2018

New Inducible Nitric Oxide Synthase and Cyclooxygenase-2 Inhibitors, Nalidixic Acid Linked to Isatin Schiff Bases via Certain l-Amino Acid Bridges.

Molecules 2016 Apr 15;21(4):498. Epub 2016 Apr 15.

Peptide Chemistry Department, National Research Centre, 12622-Dokki, Cairo 12311, Egypt.

A series of new Schiff bases were synthesized by condensation of isatins with the nalidixic acid-l-amino acid hydrazides. Prior to hydrazide formation, a peptide linkage has been prepared via coupling of nalidixic acid with appropriate l-amino acid methyl esters to yield 3a-c. The chemical structures of the new Schiff bases (5b and 5d-h) were confirmed by means of IR, NMR, mass spectroscopic, and elemental analyses. The anti-inflammatory activity of these Schiff bases was evaluated via measurement of the expressed inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in the lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage cells model. The Schiff bases exhibited significant dual inhibitory effect against the induction of the pro-inflammatory iNOS and COX-2 proteins with variable potencies. However, they strongly down-regulated the iNOS expression to the level of 16.5% ± 7.4%-42.2% ± 19.6% compared to the effect on COX-2 expression (<56.4% ± 3.1% inhibition) at the same concentration (10 μM). The higher iNOS inhibition activity of the tested Schiff bases, relative to that of COX-2, seems to be a reflection of the combined suppressive effects exerted by their nalidixic acid, isatins (4a-c), and l-amino acid moieties against iNOS expression. These synthesized nalidixic acid-l-amino acid-isatin conjugates can be regarded as a novel class of anti-inflammatory antibacterial agents.
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http://dx.doi.org/10.3390/molecules21040498DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273797PMC
April 2016

Synthesis and pharmacological activities of some new triazolo- and tetrazolopyrimidine derivatives.

Molecules 2013 Dec 6;18(12):15051-63. Epub 2013 Dec 6.

Pharmacology and Toxicology Department, College of Pharmacy, Taibah University, Al-Madinah Al-Munawara 3893, Saudi Arabia.

A new series of fused triazolo- and tetrazolopyrimidine derivatives 2-14 were synthesized and their anti-inflammatory and ulcerogenic activities were evaluated. The pharmacological screening showed that many of these obtained compounds have good anti-inflammatory activities, comparable to the reference drug. The toxicity of the compounds was also assayed via the determination of their LD50 values. The structures of newly synthesized compounds were confirmed by IR, 1H-NMR, MS spectral data and elemental analysis.
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http://dx.doi.org/10.3390/molecules181215051DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6269734PMC
December 2013

Synthesis of novel vasodilatory active nicotinate esters with amino acid function.

Bioorg Med Chem 2006 Dec 14;14(24):8488-94. Epub 2006 Sep 14.

Pesticide Chemistry Department, National Research Centre, Dokki, 12622 Cairo, Egypt.

A variety of N-[(ethyl-4,6-diaryl-3-pyridinecarboxylate)-2-yl]amino acid esters 6a-h were synthesized through the reaction of 2-bromonicotinates 4 with a number of primary amino acid ester hydrochlorides 5 in refluxing tetrahydrofuran in the presence of triethylamine as dehydrohalogenating agent. Similarly, reaction of 4 with N-glycylglycine ethyl ester hydrochloride 7 'as a representative example of dipeptide derivative' afforded smoothly the corresponding N-[(ethyl-4,6-diaryl-3-pyridinecarboxylate)-2-yl]-N'-glycylglycine ethyl ester analogues 8. However, reaction of 4 with 5 in refluxing pyridine yielded the unexpected 2-aminonicotinate esters 9. Vasodilation activity screening for the synthesized nicotinate esters was investigated in vitro on the contractile response of vascular thoracic aorta smooth muscle from Wistar rats, where all the tested compounds exhibit considerable vasodilatory properties. In addition, few prepared compounds especially, 6b, 6h and 9b reveal remarkable vasodilation potency (IC(50)).
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http://dx.doi.org/10.1016/j.bmc.2006.08.041DOI Listing
December 2006
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