Medicinal Chemistry

Pintapa P Grongsaard

Publications

• Research Article
  Design, Synthesis and Calcium Channel Blocking Activity of Diltiazem- Verapamil Hybrid Molecules
  Author(s): Ahmed S Mehanna, Timothy J Maher and Pintapa P GrongsaardAhmed S Mehanna, Timothy J Maher and Pintapa P Grongsaard
  
  The current manuscript describes the design, synthesis, and in vitro testing of four thioacetanilides with diltiazemverapamil hybrid structural features as potential calcium channel blockers. The current hybrid strategy of drug design aimed to generate compounds that could span, with a single compound, the trans-membrane locales where the two drugs bind, with the ultimate goal of increasing the blocking activity. The latter, was assessed by measuring the inhibitory effects, expressed as IC50, on calcium-induced contractions of potassium depolarized isolated rat aorta strips. The assessment of the binding locales was determined by incubating the test compound with aortic strips for two different periods, 10-minutes and 2-hours, before adding the contractile calcium ions to the assay medium. Diltiazem IC50 values were 0.26 and 0.14 μ.. Read More»
  DOI: 10.4172/2161-0444.1000216

  Abstract PDF