2229043-42-7
Chemical Structure
NPD-008
- CAS No.: 2229043-42-7
- Formula:C31H36N4O4
- Molecular Weight:528.64
IUPAC Name: N-(2-amino-2-oxoethyl)-5'-((4aS,8aR)-3-cycloheptyl-4-oxo-3,4,4a,5,8,8a-hexahydrophthalazin-1-yl)-2'-methoxy-[1,1'-biphenyl]-4-carboxamide
InChIKey: VZKJWTFPORBEEH-RPBOFIJWSA-N
SMILES: O=C1[C@]2([H])[C@](CC=CC2)([H])C(C3=CC(C4=CC=C(C=C4)C(NCC(N)=O)=O)=C(C=C3)OC)=NN1C5CCCCCC5
Biological Activity: NPD-008 is a tetrahydrophthalazinone-based phosphodiesterase inhibitor. It exerts antiparasitic activity by binding to the active site of TbrPDEB1 to block cAMP degradation, increasing intracellular cAMP levels in trypanosomatid parasites, disrupting cellular structure, and inhibiting cytokinesis. NPD-008 is used in research on Chagas disease, leishmaniasis, and human African trypanosomiasis[1][2][3][4][5][6].
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NPD-008 | NPD-008 is a tetrahydrophthalazinone-based phosphodiesterase inhibitor. It exerts antiparasitic activity by binding to the active site of TbrPDEB1 to block cAMP degradation, increasing intracellular cAMP levels in trypanosomatid parasites, disrupting cellular structure, and inhibiting cytokinesis. NPD-008 is used in research on Chagas disease, leishmaniasis, and human African trypanosomiasis. | |||||||||||||||||||||
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References
- [1]. Eman Fathi Fadel, et al. Harnessing Conventional and Nanotechnology-Enabled Combination Therapies to Combat Kinetoplastid Neglected Tropical Diseases. ACS Infect. Dis. 2026
- [2]. Blaazer AR, et al. Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity. Journal of medicinal chemistry. 2018 May 10;61(9):3870-3888.
- [3]. de Araújo JS, et al. Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with Activity against Intracellular Trypanosomatids. Antimicrobial agents and chemotherapy. 2021 Feb 17;65(3):e00960-20.
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[4]. Huleani S. The identification of novel fragment leads by Biophysical methods for the inhibition of TbrPDEB1 as an anti-parasitic approach to Human African Trypanosomiasis[D]. University of Kent (United Kingdom), 2018.
- [5]. de Araújo JS, et al. Imidazole Derivatives as Promising Agents for the Treatment of Chagas Disease. Antimicrobial agents and chemotherapy. 2019 Apr;63(4):e02156-18.
- [6]. Soeiro MNC, et al. Perspectives for a new drug candidate for Chagas disease therapy. Memorias do Instituto Oswaldo Cruz. 2022;117:e220004.
