Identification of antibacterial and antifungal pharmacophore sites for potent bacteria and fungi inhibition: Indolenyl sulfonamide derivatives
Identifieur interne : 000638 ( Main/Exploration ); précédent : 000637; suivant : 000639Identification of antibacterial and antifungal pharmacophore sites for potent bacteria and fungi inhibition: Indolenyl sulfonamide derivatives
Auteurs : Zahid H. Chohan [Pakistan] ; Moulay H. Youssoufi [Maroc] ; Aliasghar Jarrahpour [Iran] ; Taibi Ben Hadda [Maroc]Source :
- European journal of medicinal chemistry [ 0223-5234 ] ; 2010.
Descripteurs français
- Pascal (Inist)
- Antibactérien, Antifongique, Modèle moléculaire, Relation structure activité, Tautomère, Dérivé du benzène, Dérivé de l'isoxazole, Dérivé de la pyrimidine, Criblage virtuel, Bioinformatique, Composé aromatique, Synthèse chimique, Dérivé du thiazole, Aldimine, Antimicrobien, Toxicité, Artemia salina, Cytotoxicité, In vitro, Imine, Sulfonamide, Modélisation, Benzènesulfonamide(4-indol-3-ylméthylèneamino-N-thiazol-2-yl), Indole-3-carbaldéhyde dérivé, Benzènesulfonamide dérivé.
English descriptors
- KwdEn :
- Aldimine, Antibacterial agent, Antifungal agent, Antimicrobial agent, Aromatic compound, Artemia salina, Benzene derivatives, Bioinformatics, Chemical synthesis, Cytotoxicity, Imine, In vitro, Isoxazole derivatives, Modeling, Molecular model, Pyrimidine derivatives, Structure activity relation, Sulfonamide, Tautomer, Thiazole derivatives, Toxicity, Virtual screening.
Abstract
Synthesis of seven new indolenyl sulfonamides, have been prepared by the condensation reaction of indole-3-carboxaldehyde with different sulfonamides such as, sulphanilamide, sulfaguanidine, sulfathiazole, sulfamethoxazole, sulfisoxazole, sulfadiazine and sulfamethazine. These synthesized compounds have been used as potential ligands for complexation with some selective divalent transition metal ions (cobalt, copper, nickel & zinc). Structure of the synthesized ligands has been deduced from their physical, analytical (elemental analyses) and spectral (IR, 1H NMR and 13C NMR & UV-vis) data. All the compounds have also been assayed for their in vitro antibacterial and antifungal activities examining six species of pathogenic bacteria (Escherichia coli, Shigella flexneri, Pseudomonas aeruginosa, Salmonella typhi, Staphylococcus aureus and Bacillus subtilis) and six of fungi (Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium soloni and Candida glabrata). Antibacterial and antifungal results showed that all the compounds showed significant antibacterial activity whereas most of the compounds displayed good antifungal activity. Brine shrimp bioassay was also carried out for in vitro cytotoxic properties against Artemia salina.
Affiliations:
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Le document en format XML
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<term>Artemia salina</term>
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<front><div type="abstract" xml:lang="en">Synthesis of seven new indolenyl sulfonamides, have been prepared by the condensation reaction of indole-3-carboxaldehyde with different sulfonamides such as, sulphanilamide, sulfaguanidine, sulfathiazole, sulfamethoxazole, sulfisoxazole, sulfadiazine and sulfamethazine. These synthesized compounds have been used as potential ligands for complexation with some selective divalent transition metal ions (cobalt, copper, nickel & zinc). Structure of the synthesized ligands has been deduced from their physical, analytical (elemental analyses) and spectral (IR, <sup>1</sup>
H NMR and <sup>13</sup>
C NMR & UV-vis) data. All the compounds have also been assayed for their in vitro antibacterial and antifungal activities examining six species of pathogenic bacteria (Escherichia coli, Shigella flexneri, Pseudomonas aeruginosa, Salmonella typhi, Staphylococcus aureus and Bacillus subtilis) and six of fungi (Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium soloni and Candida glabrata). Antibacterial and antifungal results showed that all the compounds showed significant antibacterial activity whereas most of the compounds displayed good antifungal activity. Brine shrimp bioassay was also carried out for in vitro cytotoxic properties against Artemia salina.</div>
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