Synthesis and antimicrobial activity of 3-methyl-substituted 6,8-dimethylthiazolo-[2,3-f]xanthines

Dianov, V. M.; Булгаков, А. К.

doi:10.1007/s11094-006-0191-7

Cited by 2 publications

(2 citation statements)

References 4 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…1), under the name of laprafylline, is in Phase II clinical trials as a bronchodilator (Regnier et al, 1987;Baraldi et al, 2007). Furthermore, there are some reports studied the antibacterial action of xanthines and xanthine derivatives on various microorganisms, and proved that some compounds showed significant activity (Raj and Dhala, 1965;Ashour et al, 1993;Romanenko et al, 1997;Dianov and Bulgakov, 2006).…”

Section: Introductionmentioning

confidence: 99%

Design and synthesis of some new theophylline derivatives with bronchodilator and antibacterial activities

2011

View full text Add to dashboard Cite

Methylxanthines especially theophylline have been recognized as potent bronchodilators for the relief of acute asthma for over 65 years. Recently, it was found that bacterial infection plays a role in asthma pathogenesis. Accordingly, the present work involves the synthesis of 6-(4-(un)substituted phenyl)thiazolo[2,3-f]theophyllines 2a-g and different series of 8-(1,2,4-triazol-3-ylmethylthio)theophyllines 6-9. The chemical structures of the target compounds were proved by IR, (1)H NMR, (13)C NMR, EI-MS and HRMS spectroscopic techniques along with elemental analyses. The bronchodilator activity of fifteen compounds was determined in vivo by acetylcholine induced bronchospasm in anaesthetized guinea pigs. Results revealed that all compounds showed moderate to good activity; in addition, five compounds exhibited a bronchodilator activity nearly similar to that of aminophylline as a standard. The antibacterial activity of all the target compounds was investigated in vitro against both Gram-positive and Gram-negative bacterial strains. Results revealed that some compounds showed more potent antibacterial activity than ampicillin as a standard. Acute toxicity study for four target compounds revealed that none of these derivatives showed significant toxicity up to 300 mg/kg. It was found that compound 8c combined both promising bronchodilator and antibacterial activities. This compound could be subjected for further investigations as a new possible candidate in the treatment of bronchial asthma.

show abstract

Section: Introductionmentioning

confidence: 99%

Design and synthesis of some new theophylline derivatives with bronchodilator and antibacterial activities

2011

View full text Add to dashboard Cite

show abstract

“…Several 8-substituted theophylline derivatives were synthesized, and showed a potent bronchodilator activity [19][20][21] . Furthermore, there are some reports studied the antibacterial effect of xanthines and xanthine derivatives on various microorganisms, and stated that some compounds showed significant degree of activity [22][23][24][25][26] . Other studies reported that methylxanthines had a synergistic effect on antibacterial agents 27&28 .…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Anti-Bronchoconstrictive, and Antibacterial Activities of Some New 8- Substituted-1,3-Dimethylxanthine Derivatives

Elgaher

Hayallah

Alim

2009

Bulletin of Pharmaceutical Sciences. Assiut

View full text Add to dashboard Cite

Synthesis and antimicrobial activity of 3-methyl-substituted 6,8-dimethylthiazolo-[2,3-f]xanthines

Cited by 2 publications

References 4 publications

Design and synthesis of some new theophylline derivatives with bronchodilator and antibacterial activities

Design and synthesis of some new theophylline derivatives with bronchodilator and antibacterial activities

Synthesis, Anti-Bronchoconstrictive, and Antibacterial Activities of Some New 8- Substituted-1,3-Dimethylxanthine Derivatives

Contact Info

Product

Resources

About