Tuesday , 1 December 2020

Synthesis and Evaluation of Sulfonylureas for Anti Diabetic Activity

Anurag Singh*1, Abhishek Agrawal1, Dr. Shantaram U2
1Nargund College of Pharmacy, Bangalore, Karnataka, India
2Deparment of Chemistry, Government College of Pharmacy, Bangalore, Karnataka

Drug ,synthesis and development multidisciplinary, creative, complex and highly regulated process New drug synthesis not only done loping new chemical entities but also important for therapeutic need Diabetes mellitus (DM) is one of the most daunting challenges posed by chronic diseases resulting from insulin deficiency or insulin resistance. Sulfonylureas have been used as hypoglycemic agents since the mid-1950s. Compounds in the first generation of this class such as chlorpropamide, tolbutamide etc. are still in use, but are less potent than the more recently introduced second generation drugs like glipizide, glibenclamide etc. The aim of our present study is to synthesize sulfonylureas derivatives with suitable substituents on Nitrogen and Sulfur and evaluate the antidiabetic activity of the synthesized compounds using albino wistar rats. Substituted sulfonylurea compounds were synthesized in three steps. In first step, oxidation of p-toluene sulfonamide (19) was carried out with KMnO4 to form p-Aminosulfonyl-benzoic Acid (22). This was then, in second step, reacted with aniline in presence of EDCI, HOBt and triethylamine to form p-Aminosulfonyl-N-(phenyl) benzamide (23). In third step, p-Aminosulfonyl-N-(phenyl)benzamide was reacted with triphosgene and various types of anilines (24(a-j)) to form different substituted sulfonylurea derivatives (25(a-j)). The synthesized compounds were screened for antidiabetic activity by GOD/POD method and anti-oxidant activity by DPPH method. A total of 10 novel sulfonylureas were synthesized (25(a-j)) which was characterized by m.p., TLC, elemental analysis, IR and 1H NMR.  Data pertaining to the effect of compound on blood glucose levels for all 10 molecules was obtained. Anti-oxidant activity data for 25c, 25f and 25g was also obtained. Of the ten compounds (25(a-j)) which were tested for blood glucose lowering effect, 25g and 25i were found to be very active. Other compounds were also showed good activity. The molecules that were tested for anti-oxidant activity were found to be very weak. Further work is proposed for blood glucose monitoring on diabetes induced rats.
Keywords: Diabetes mellitus, hypoglycemic agent, Sulfonylurea derivatives.

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