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Synthesis of three rimantadine schiff bases and their biological effects on serum albumin.

Liu BM, Ma P, Wang X, Kong YM, Zhang LP, Liu B - Iran J Pharm Res (2014)

Bottom Line: The results showed that the three RSBs effectively quenched the intrinsic fluorescence of BSA via static quenching.According to the results of displacement experiments of site probes, it was considered that the binding sites were located in hydrophobic cavities in sub-domains IIA of BSA.What is more, synchronous fluorescence studies indicated that the hydrophobicity around tryptophan residues was increased with the addition of rimantadine-o-vanillin (ROV) and rimantadine-4-methoxy-salicylaldehyde (RMS), while there was no apparent change with the addition of rimantadine-salicylaldehyde (RS).

View Article: PubMed Central - PubMed

Affiliation: College of Pharmacy , Liaoning University, Shenyang 110036, P . R . China .

ABSTRACT
Three new rimantadine Schiff bases (RSBs) were prepared, and then the interaction of RSBs with bovine serum albumin (BSA) was investigated using fluorescence, synchronous fluorescence, UV-vis absorption spectroscopy under physiological conditions. The results showed that the three RSBs effectively quenched the intrinsic fluorescence of BSA via static quenching. Binding constant (K a), number of binding sites (n), and the binding distance (r) between three RSBs and BSA were calculated by Stern-Volmer equation and Förster's theory in this study. According to the results of displacement experiments of site probes, it was considered that the binding sites were located in hydrophobic cavities in sub-domains IIA of BSA. What is more, synchronous fluorescence studies indicated that the hydrophobicity around tryptophan residues was increased with the addition of rimantadine-o-vanillin (ROV) and rimantadine-4-methoxy-salicylaldehyde (RMS), while there was no apparent change with the addition of rimantadine-salicylaldehyde (RS).

No MeSH data available.


Related in: MedlinePlus

Molecular structures of rimantadine-salicylaldehyde (RS), rimantadine-o-vanillin (ROV) and rimantadine-4-methoxy- salicylaldehyde (RMS) Schiff bases
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Figure 1: Molecular structures of rimantadine-salicylaldehyde (RS), rimantadine-o-vanillin (ROV) and rimantadine-4-methoxy- salicylaldehyde (RMS) Schiff bases

Mentions: In recent years, the new pattern influenzal characteristic is often amphibianous. That is, the influenza is caused by viruses and germs at the same time (12, 13). Therefore, it is necessary to design the difunctional drugs, which have antiviral and antibacterial actions simultaneously (14). In this work, three new rimantadine Schiff bases (RSBs), rimantadine-salicylaldehyde (RS), rimantadine-o-vanillin (ROV) and rimantadine-4-methoxy-salicylaldehyde (RMS), were synthesized which would display the better biologic activities. The molecular structures of three RSBs are shown in Figure 1.


Synthesis of three rimantadine schiff bases and their biological effects on serum albumin.

Liu BM, Ma P, Wang X, Kong YM, Zhang LP, Liu B - Iran J Pharm Res (2014)

Molecular structures of rimantadine-salicylaldehyde (RS), rimantadine-o-vanillin (ROV) and rimantadine-4-methoxy- salicylaldehyde (RMS) Schiff bases
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4232783&req=5

Figure 1: Molecular structures of rimantadine-salicylaldehyde (RS), rimantadine-o-vanillin (ROV) and rimantadine-4-methoxy- salicylaldehyde (RMS) Schiff bases
Mentions: In recent years, the new pattern influenzal characteristic is often amphibianous. That is, the influenza is caused by viruses and germs at the same time (12, 13). Therefore, it is necessary to design the difunctional drugs, which have antiviral and antibacterial actions simultaneously (14). In this work, three new rimantadine Schiff bases (RSBs), rimantadine-salicylaldehyde (RS), rimantadine-o-vanillin (ROV) and rimantadine-4-methoxy-salicylaldehyde (RMS), were synthesized which would display the better biologic activities. The molecular structures of three RSBs are shown in Figure 1.

Bottom Line: The results showed that the three RSBs effectively quenched the intrinsic fluorescence of BSA via static quenching.According to the results of displacement experiments of site probes, it was considered that the binding sites were located in hydrophobic cavities in sub-domains IIA of BSA.What is more, synchronous fluorescence studies indicated that the hydrophobicity around tryptophan residues was increased with the addition of rimantadine-o-vanillin (ROV) and rimantadine-4-methoxy-salicylaldehyde (RMS), while there was no apparent change with the addition of rimantadine-salicylaldehyde (RS).

View Article: PubMed Central - PubMed

Affiliation: College of Pharmacy , Liaoning University, Shenyang 110036, P . R . China .

ABSTRACT
Three new rimantadine Schiff bases (RSBs) were prepared, and then the interaction of RSBs with bovine serum albumin (BSA) was investigated using fluorescence, synchronous fluorescence, UV-vis absorption spectroscopy under physiological conditions. The results showed that the three RSBs effectively quenched the intrinsic fluorescence of BSA via static quenching. Binding constant (K a), number of binding sites (n), and the binding distance (r) between three RSBs and BSA were calculated by Stern-Volmer equation and Förster's theory in this study. According to the results of displacement experiments of site probes, it was considered that the binding sites were located in hydrophobic cavities in sub-domains IIA of BSA. What is more, synchronous fluorescence studies indicated that the hydrophobicity around tryptophan residues was increased with the addition of rimantadine-o-vanillin (ROV) and rimantadine-4-methoxy-salicylaldehyde (RMS), while there was no apparent change with the addition of rimantadine-salicylaldehyde (RS).

No MeSH data available.


Related in: MedlinePlus