ChemInform Abstract: 2,3‐DIHYDRO‐6,8‐DIMETHYLTHIAZOLO(3,2‐F)XANTHIN‐3‐ONE AND ITS DERIVATIVES AT THE METHYLENE GROUP

Красовский, А. Н.; Turkevich, N. M.; Yurchenko, M. I.; Кочергин, П. М.; Soroka, I. I.

doi:10.1002/chin.198246219

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“…Yield: 6.2 g (87%), mp: 215-216 o C as reported (Karsovskii et al, 1982 1,3-Dimethyl-2,6-dioxo-2,3,6,7-tetrahydro-1H-purine-8-yl thioacetohydrazide (5)…”

Section: H-purin-8-yl)thio]acetate (4)mentioning

confidence: 99%

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

2011

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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.

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“…Yield: 6.2 g (87%), mp: 215-216 o C as reported (Karsovskii et al, 1982 1,3-Dimethyl-2,6-dioxo-2,3,6,7-tetrahydro-1H-purine-8-yl thioacetohydrazide (5)…”

Section: H-purin-8-yl)thio]acetate (4)mentioning

confidence: 99%

“…4. Compounds 4 and 5 were previously published with no 1 H NMR data (Karsovskii et al, 1982) and (Strokin et al, 1990), respectively. In the present work, we have characterized them by determining their mp, IR, as well as 1 H NMR spectra.…”

Section: Chemistrymentioning

confidence: 99%

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

2011

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ChemInform Abstract: 2,3‐DIHYDRO‐6,8‐DIMETHYLTHIAZOLO(3,2‐F)XANTHIN‐3‐ONE AND ITS DERIVATIVES AT THE METHYLENE GROUP

Abstract: 8‐Thio‐theophyllin (I) reagiert mit Brom‐carbonsäuren bzw. ihren Estern (II) zu den Carboxy‐alkyl‐ bzw. Carbometho xy‐methyl‐Derivaten (III).

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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

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