Design, Synthesis And Antidiabetic, Cardiomyopathy Studies Of Cinnamic Acid-amino Acid Hybrid Analogs | 10517
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Diabetes mellitus, chronic metabolism disorder is characterized by hypergycemia due to insulin deficiency or insulin resistance.
Taking into consideration the high cost of modern treatment we have employed a newer approach of design, synthesis and
antidiabetic screening of cinnamic acid and amino acid hybrid compounds. The advent of biotechnology and molecular biology
has made the role of peptides and amino acids more significant to influence virtually all body functions. Associated complications
include myocardial infarction, cardiomyopathy, retinopathy, neuropathy, and nephropathy.
Cinnamic acid analogs (SSPC0-SSPC21) containing different amino acids were designed, docked into crystal structure of
AMPK and PPARs. Among the 22 compounds SSPC5, SSPC8, SSPC11, SSPC14, SSPC15 showed good docking scores using
Glide 5.0 maestro program and subjected to ADME prediction by using software Quickprop version 3.1.
Five best docked compounds were synthesis, characterized and antidiabetic activity carried out using alloxan induced
diabetic mice model by measuring blood glucose levels using glucometer at 0, 1, 2, 4, 6, 8 and 24 hrs. SSPC5, SSPC8, SSPC11,
SSPC14 showed % reduction of blood glucose of 23.02%, 37.02%, 14.04 and 15.96% as compared to standard glibenclamide
with 33.53% reduction. SSPC14 was subjected for the diabetic cardiomyopathy studies by recording the electrocardiogram using
Biopac Student Lab PRO System of both diabetic and control rat, analyzed using acknowledge 4 and was found to be very efficient
at low dose with a prolong duration of action of the heart (Up to 54 hrs). Thus this study indicated that such hybrid antidiabetic
drugs will serve as novel future medicines.
S. Samanta is Professor in the Department of Pharmaceutical Sciences, Birla Institute of Technology, and Mesra, India, with 27 years of teaching
and research experience. He is at present guiding 7 Ph.D. students, established the CADD lab for the rational designing and molecular modeling
and has been funded by the UCG for UGC-MRP project on antidiabetics. He has 12 international publications to his credit and also received patent
for process and product on peptide based antidiabetic compounds.
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