Chitin synthase inhibitor 2

Chitin synthase inhibitor 2 (compound 2b) is a potent inhibitor of chitin synthase with the IC50 value of 0.09 mM and the Ki value of 0.12 mM. Chitin synthase inhibitor 2 has antimicrobial activities in vitro and shows synergistic or additive effects with fluconazole or polyoxin B[1].

Signaling Pathways >> Anti-infection >> Fungal

Research Areas >> Inflammation/Immunology

IC50: 0.09 mM; Ki: 0.12 mM[1]

Chitin synthase inhibitor 2 (compound 2b) (0, 0.032, 0.126, and 0.25 mM) inhibits chitin synthase with inhibition constant Ki value of 0.12 mM and the inhibition percent (IP) of 78.3% at 0.3 mM[1]. Chitin synthase inhibitor 2 (1-4 μg/mL) has excellent antifungal activity with MIC (minimum inhibitory concentration) values of 2, 4, 1, and 2 μg/mL against C. albicans (ATCC 76615), A. fumigatus (GIMCC 3.19), C. albicans (ATCC 90023), and A. flavus (ATCC 16870), respectively[1]. Chitin synthase inhibitor 2 (128-512 g/mL) has no antibacterial activity against MRSA (N. 315), S. aureus (ATCC 25923), B. subtilis (ATCC 6633), C. coli (JM 109), P. aeruginosa (ATCC 9027), and B. proteus (ATCC 8427) [1].

[1]. Li B, Shen Y, Wu H, Wu X, Yuan L, Ji Q. Design, synthesis and biological evaluation of novel 3,4-dihydro-2(1H)-quinolinone derivatives as potential chitin synthase inhibitors and antifungal agents. Eur J Med Chem. 2020 Jun 1;195:112278.