Synthesis and hypoglycemic activity of some new theophylline derivatives

Abstract

Thirty-one new theophylline derivatives have been synthesized and evaluated for their hypoglycemic activity. Compounds 24 (56% reduction) and 31 (57% reduction) showed better hypoglycemic activity than the standard drug glibenclamide which showed 52% reduction in serum glucose level. Compound 27 remarkably reduced serum glucose level by 53%. Ten compounds showed varying degrees of hypoglycemic activity ranging from 20 to 37% reduction in serum glucose level compared to the standard drug. The aromatic amide functionality is the common feature of these theophylline hypoglycemic derivatives. However, anthranilamide and or aliphatic amides proved to be the least active compounds in the present series.

The hypoglycemic effect of extract/fractions from Fuzhuan Brick‐Tea in streptozotocin‐induced diabetic mice and their active components characterized by LC‐QTOF‐MS/MS

“…It was reported that low‐dose theophylline treatment possessed an anti‐inflammatory effect with a relatively low risk of toxicity (Allen, Wong, Vassallo, & Kwan, 2016). In addition, a report suggested that thirteen new theophylline derivatives were found to be able to ameliorate the symptoms of diabetes mellitus (Alafeefy et al., 2014). In this study, the tentatively identified compounds consist of the same theophylline skeleton.…”

Phytochemical Screening, Gas Chromatography-mass Spectrometry Analysis, and Antidiabetic Effects of Corchorus olitorius Leaves in Rats

“…Adenosine 1 receptor antagonism improved glucose tolerance in Zucker rats through enhancing glucose uptake in skeletal muscle [23]. Derivatives of theophylline were accordingly synthesized and showed a hypoglycemic effect [24].…”

Recent Synthetic Approaches Towards Biologically Potent Derivatives/Analogues of Theophylline

“…Such collection of specificities has stimulated the desire to synthesize new theophylline derivatives and to achieve that desire into realization, Alafeefy et al . in 2014 synthesized theophylline derivatives substituted with acetohydrazide moiety at 7‐position. In their methodology, 7‐acetohydrazide derivative 156 was further utilized for the synthesis of number of theophylline derivatives by reacting with different reagents such as aldehydes/ketones, anhydrides, and acid chlorides.…”