Mussarat Tasleem, Julie Pelletier, Jean Sévigny, Zahid Hussain, Muhammad Ajmal, Ahmed Al-Harrasi, Attalla F El-Kott, Parham Taslimi, Sally Negm, Zahid Shafiq, Jamshed Iqbal
An extensive range of new biologically active morpholine based thiosemicarbazones derivatives 3a-r were synthesized, characterized by spectral techniques and evaluated as inhibitors of ENPP isozymes. Most of the novel thiosemicarbazones exhibit potent inhibition towards NPP1 and NPP3 isozymes. Compound 3 h was potent inhibitor of NPP1 with IC50 value of 0.55 ± 0.02. However, the most powerful inhibitor of NPP3 was 3e with an IC50 value of 0.24 ± 0.02. Furthermore, Lineweaver-Burk plot for compound 3 h against NPP1 and for compound 3e against NPP3 was devised through enzymes kinetics studies...
March 24, 2024: International Journal of Biological Macromolecules