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Synthesis And Bioactivity Of PAMAM,PAMAM-salicylaldehyde Schiff Base And Diamine-salicylaldehyde Schiff Base

Posted on:2013-05-08Degree:MasterType:Thesis
Country:ChinaCandidate:J J ZhuFull Text:PDF
GTID:2231330371975855Subject:Physical chemistry
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In this paper, the progress on the biological and medical application of dendrimer and schiff base was reviewed in detail. Based on the reference survey, study on synthesis and biological activity about PAMAM, PAMAM-salicylaldehyde schiff base and diamine-salicylaldehyde schiff base was put forward. The research contents and results are as follows:1. Synthesis and biological activity of1.0-5.0G PAMAM1.0-5.0G PAMAM have been synthesized successfully by divergent approach with ethylenediamine as core. The half generation PAMAM (0.5G PAMAM was purified by the vacuum distillation) was separated and purified by the method of colum chromatography, and the whole generation PAMAM was purified by the vacuum distillation.1.0-5.0G PAMAM were confirmed by FT-IR,1H NMR and13C NMR. In vitro biological activity of1.0-5.0G PAMAM against bacterial strain and fungal strain was tested.The results of biological activity show that1.0-5.0G PAMAM are broad-spectrum biological activity to Gram-positive bacteria, Gram-negative bacteria and fungi.For the same bacteria or fungi, the different PAMAM has the different bacteriostatic activity and bactericidal activity. For E. coli,3.0G and4.0G PAMAM have the same and the best bacteriostatic activity and bactericidal activity, MIC is0.45mg/mL and MBC is0.9mg/mL. For S. aureus,4.0G and5.0G PAMAM have the same and the best bacteriostatic activity, MIC is0.23mg/mL, but4.0G PAMAM has the best bactericidal activity, MBC is0.23mg/mL. For C. albicans,4.0G PAMAM has the same and the best bacteriostatic activity and bactericidal activity, MIC and MBC are both0.12mg/mL. For B. thuringiensis,3.0G PAMAM has the best bacteriostatic activity and bactericidal activity, MIC and MBC are both0.23mg/mL. For C. neoforman,2.0G and3.0G PAMAM have the same and the best bacteriostatic activity and bactericidal activity, MIC and MBC are both0.12mg/mL. For S. enteritidis,3.0G PAMAM has the best bacteriostatic activity and bactericidal activity, MIC is0.45mg/mL and MBC is0.9mg/mL. For P. aeruginosa,1.0G,2.0G,3.0G and4.0G PAMAM have the same and the best bacteriostatic activity, MIC is1.8mg/mL, but2.0G,3.0G and4.0G PAMAM have the same and the best bactericidal activity, MBC is1.8mg/mL.To the different bacteria or fungi, the same generation PAMAM has different bacteriostatic activity and bactericidal activity.1.0G PAMAM has the same and the best bacteriostatic activity against E. coli, B. thuringiensis, P. aeruginosa, C. neoforman, and S. enteritidis, MIC is1.8mg/mL, but it has the best and the same bactericidal activity against E. coli and B. thuringiensis, MBC is1.8mg/mL.2.0G and3.0G PAMAMs have the same and the best bacteriostatic activity and bactericidal activity against C. neoforman, MIC and MBC are both0.12mg/mL.4.0G PAMAM has the best bacteriostatic activity and bactericidal activity against C. albicans, MIC and MBC are both0.12mg/mL.5.0G PAMAM has the best bacteriostatic activity and bactericidal activity against S. aureus, MIC is0.23mg/mL, MBC is0.45mg/mL.2. Synthesis and biological activity of1.0-5.0G PAMAMSA1.0-5.0G PAMAM salicylaldehyde schiff bases were synthesized. Their structures were confirmed by FT-IR,1H NMR and13C NMR et al. In vitro biological activity of1.0-5.0G PAMAMSA were tested. The results of biological activity show that1.0-5.0G PAMAMSA are broad-spectrum biological activity to Gram-positive bacteria, Gram-negative bacteria and fungi.To the different bacteria or fungi, the same PAMAMSA has the different bacteriostatic activity and bactericidal activity.1.0G,2.0G,3.0G,4.0G and5.0G PAMAMSA have the best bacteriostatic activity and bactericidal activity against C. neoforman in the tested micro-organisms, but MIC and MBC are different. For1.0G and2.0G PAMAMSA, MIC is0.032mg/mL, and MBC is0.125mg/mL. For3.0G and4.0G PAMAMSA, MIC is0.063mg/mL, and MBC is0.125mg/mL. For5.0G PAMAMSA, MIC is0.063mg/mL, and MBC is0.25mg/mL.For the same bacteria or fungi, the different PAMAMSA has the different bacteriostatic activity and bactericidal activity. For E. coli,1.0-5.0G PAMAMSA have the same bacteriostatic activity and bactericidal activity, MIC and MBC are both1.0mg/mL. For S. aureus,3.0G and4.0G PAMAMSA have the same and the best bacteriostatic activity, MIC is0.5mg/mL, but3.0G,4.0G and5.0G PAMAMSA have the best and the same bactericidal activity, MBC is1.0mg/mL. For S. enteritidis,2.0G PAMAMSA has the best bacteriostatic activity and bactericidal activity, MIC is0.063mg/mL, and MBC is0.25mg/mL. For P. aeruginosa,2.0G PAMAMSA has the best bacteriostatic activity and bactericidal activity, MIC is0.125mg/mL, and MBC is0.5mg/mL. For C. albicans,2.0G,3.0G,4.0G and5.0G PAMAMSA have the same and the best bacteriostatic activity, MIC is0.5mg/mL,2.0G,3.0G and4.0G PAMAMSA have the same and the best bactericidal activity, MBC is0.5mg/mL. For C. neoforman,1.0G and2.0G PAMAM have the same and the best bacteriostatic activity, MIC is0.032mg/mL, but1.0-4.0G PAMAMSA have the same and the best bactericidal activity, MBC is0.125mg/mL. For C. glabrata,1.0G3.0G,4.0G and5.0G PAMAMSA have the same and the best bacteriostatic activity, MIC is0.25mg/mL, but3.0G,4.0G and5.0G PAMAMSA have the same and the best bactericidal activity, MBC is0.25mg/mL.3. Synthesis and biological activity of diamine salicylaldehyde schiff baseA series of diamine salicylaldehyde schiff bases were synthesized. Their structures were confirmed by FT-IR,1H NMR and13C NMR et al. In vitro biological activity of these diamine salicylaldehyde schiff bases were tested. The results of biological activity show that diamine salicylaldehyde schiff bases are broad-spectrum biological activity to Gram-positive bacteria, Gram-negative bacteria and fungi.To the different bacteria and fungi, the same diamine salicylaldehyde schiff base has the different bacteriostatic activity and bactericidal activity. Ethylenediamine salicylaldehyde schiff base has the same and the best bacteriostatic activity and bactericidal activity against C. albicans and C. neoforman, MIC and MBC are both0.032mg/mL.1,4-dutanediamine salicylaldehyde schiff base has the best bacteriostatic activity and bactericidal activity against C. neoforman, MIC and MBC are both0.032mg/mL.1,6-hexamethylenediamine salicylaldehyde schiff base has the best bacteriostatic activity and bactericidal activity against C. neoforman, MIC and MBC are both0.032mg/mL.1,8-diaminooctane salicylaldehyde schiff base has the best bacteriostatic activity and bactericidal activity against C. neoforman, MIC and MBC are both0.032mg/mL.1,10-diaminodecane salicylaldehyde schiff base has the same and the best bacteriostatic activity against S. aureus and C. neoforman, MIC is0.032mg/mL, but1,10-diaminodecane salicylaldehyde schiff base has the best bactericidal activity against C. neoforman, MBC is0.032mg/mLFor the same bacteria or fungi, diamine salicylaldehyde schiff bases have the different bacteriostatic activity and bactericidal activity. For E. coli,1,10-diaminodecane salicylaldehyde schiff base has the best bacteriostatic activity and bactericidal activity, MIC is0.063mg/mL, and MBC is0.125mg/mL. For S. aureus,1,10-diaminodecane salicylaldehyde schiff base has the best bacteriostatic activity and bactericidal activity, MIC is0.032mg/mL, MBC is0.063mg/mL. For S. enteritidis, ethylenediamine,1,6-hexamethylenediamine and1,8-diaminooctane salicylaldehyde schiff bases have the same and best bacteriostatic activity and bactericidal activity, MIC is0.125mg/mL, MBC is0.5mg/mL. For P. aeruginosa, ethylenediamine,1,4-dutanediamine and1,6-hexamethylenediamine salicylaldehyde schiff bases have the same and the best bacteriostatic activity, MIC is0.125mg/mL, but1,4-dutanediamine and1,6-hexamethylenediamine salicylaldehyde schiff bases have the same and best bactericidal activity, MBC is0.125mg/mL. For C. albicans, ethylenediamine salicylaldehyde schiff base has the best bacteriostatic activity and bactericidal activity, MIC and MBC are both0.032mg/mL. For C. neoforman, ethylenediamine,1,4-dutanediamine,1,6-hexamethylenediamine1,8-diaminooctane and1,10-diaminodecane salicylaldehyde schiff bases have the best bacteriostatic activity and bactericidal activity, MIC and MBC are both0.032mg/mL. For C. glabrata, ethylenediamine schiff base has the best bacteriostatic activity, MIC is0.063mg/mL; ethylenediamine,1,4-dutanediamine,1,6-hexamethylenediamine and1,10-diaminodecane salicylaldehyde schiff bases have the same and the best bactericidal activity, MBC is0.125mg/mL.
Keywords/Search Tags:PAMAM, PAMAMSA, Diamine-salicylaldehyde schiff baseBacteriostatic activity, Bactericidal activity
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