Natural Science > Chemistry > DG CY2020 8130 1

Research Title Long-Term Outcomes of Diagnosed Tuberculosis Cases in the Philippines (Year 3 of 3)
Research Personnel Leader:
Staff:


Research Duration Start:
End:
1 July 2019
30 June 2022
Research Location UPD-IC
Research Description The goal of the study is to improve the lead compounds’ pharmacodynamics and pharmacokinetic properties, through evaluation on the criteria of Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADME-Tox). The first phase of the project was dedicated to the synthesis of bioactive hits and their derivatives and testing their inhibitory activity against the enzyme alpha-glucosidase. The Schiff bases group exhibited higher inhibitory activity against alphaglucosidase than acarbose, an alphaglucosidase drug currently in use for the treatment of type II diabetes mellitus. Four (4) Schiff bases were identified as lead compounds after passing the preliminary cytotoxicity and orthogonal assays.
Research Objectives a. To conduct in silico prediction and docking studies b. To synthesize, purify, and characterize target compounds c. To obtain IC50 values of target compounds for the alpha-glucosidase inhibition assay d. To test the target compounds with low IC50 values in an orthogonal assay (Glucose Uptake Assay) e. To test the target compounds with low IC50 values in a series of ADME-Tox Assays
Research Beneficiary(ies) a. Biotechnology, pharmaceutical companies, and other private investors who will commercialize the products after the technology transfer b. Scientists/researchers who will contribute to use the infrastructures and validated protocols c. Possible standards for herbal industries
Research Accoplishments [CY 2019] 1) At least 2 scientific journal publications after approval of patent applications for the synthesized compounds; 2) Proprietary information and patent applications for the synthesized compounds; 3) At least 1 clinical candidate that will have optimum efficacy and physico-chemical, biophysical, pharmacokinetic properties and toxicity profile; 4) Training of undergraduate and graduate students majoring in chemistry, biology or related fields; 5) Establishment of organic synthesis facilities.
Total Research Cost ₱3,058,050.84
Research Agencies Funding:
Implementing:
Cooperating:
Monitoring:

UPD-IC


Research Budget Breakdown Year:
Year Funded:
PS:
MOOE:
EO:
Total Cost
Date Released
Amount Released








Code DG CY2020 8130 1
KRA Code
Priority Thrust DOST
R&D


Sector Natural Sciences
Actual Sector Chemistry
Related sectors Medical Science
Entry revision: February 2021