Schiff bases of tryptamine as potent inhibitors of nucleoside triphosphate diphosphohydrolases (NTPDases): Structure-activity relationship.

  title={Schiff bases of tryptamine as potent inhibitors of nucleoside triphosphate diphosphohydrolases (NTPDases): Structure-activity relationship.},
  author={Kanwal and Khalid Mohammed Khan and Uzma Salar and Saira Afzal and Abdul Wadood and Muhammad Taha and Shahnaz Perveen and Huma Khan and Joanna Lecka and Jean S{\'e}vigny and Jamshed Iqbal},
  journal={Bioorganic chemistry},

Development of Anthraquinone Derivatives as Ectonucleoside Triphosphate Diphosphohydrolase (NTPDase) Inhibitors With Selectivity for NTPDase2 and NTPDase3

Two potent compounds were found to be selective vs. other NTPDases and will be useful tools for studying the roles of NTPDase2 and -3 in physiology and under pathological conditions.

Highly potent and selective ectonucleoside triphosphate diphosphohydrolases (ENTPDase1, 2, 3 and 8) inhibitors having 2-substituted-7-trifluoromethyl-thiadiazolopyrimidones scaffold.

Molecular docking studies of the most potent inhibitors were conducted into the homology models of NTPDases and the putative binding analysis confirmed that selective and potent compounds bind deep inside the active pocket of the respective enzymes.

Computational investigation of Schiff bases from tryptamine as COX-2 inhibitors with potential anti-inflammatory activity

  • R. S. Porto
  • Chemistry, Biology
  • 2022
The results of this study indicate that tryptamine Schiff bases are promising candidates to treat inflammatory disorders, with the potential to be used as suitable medicines for pain and inflammation treatment.

New Barbiturate Derivatives as potent in vitro α-Glucosidase Inhibitors

Abstract: A series of new Schiff base derivatives were synthesized by reaction barbiturate derivatives (barbital and phenobarbital) with some aromatic aldehydes. Barbital and phenobarbital were

Nucleotide Analog ARL67156 as a Lead Structure for the Development of CD39 and Dual CD39/CD73 Ectonucleotidase Inhibitors

The present study provides a full characterization of the frequently applied CD39 inhibitor ARL67156, presents structure-activity relationships, and provides a basis for future optimization towards selective CD39 and dual CD39/CD73 inhibitors.

2‐Substituted thienotetrahydropyridine derivatives: Allosteric ectonucleotidase inhibitors

2‐substituted thienotetrahydropyridine derivatives, structurally related to ticlopidine, are investigated as CD39 inhibitors due to their substituent on the 2‐position, they will not be metabolically transformed into reactive thiols and can be expected to be devoid of P2Y12 receptor‐antagonistic activity in vivo.

E-NTPDases: Possible Roles on Host-Parasite Interactions and Therapeutic Opportunities

A comprehensive review showing the involvement of the nucleotidases/NTPDases in parasites infectivity and virulence, and how inhibition of NTPDases contributes to parasite clearance and the development of new antiparasitic drugs is provided.



Selective nucleoside triphosphate diphosphohydrolase-2 (NTPDase2) inhibitors: nucleotide mimetics derived from uridine-5'-carboxamide.

The present study synthesized adenine and uracil nucleotide mimetics, in which the phosphate residues were replaced by phosphonic acid esters attached to the nucleoside at the 5'-position by amide linkers, and identified the first potent and selective inhibitors of human NTPDase2.

Nucleoside triphosphate diphosphohydrolases (NTPDase) inhibitory activity of some medicinal plants.

Data shows that only 6 plants exhibited anti-NTPDase activity above 50% with crude enzyme preparation of chicken liver at 125 μg plant extract, and further work is required to explore these plants using purified enzyme preparations.

The structure of the nucleoside triphosphate diphosphohydrolases (NTPDases) as revealed by mutagenic and computational modeling analyses

A speculative cartoon model of the enzymatic mechanism of the membrane-bound NTPDases that integrates movements of the extracellular region required for catalysis with movements ofThe N- and C-terminal transmembrane helices that are important for control and modulation of enzyme activity are presented.

Is Ecto-nucleoside Triphosphate Diphosphohydrolase (NTPDase)-based Therapy of Central Nervous System Disorders Possible?

The application of genetically engineered stem cells as carrier vehicles offers a promising strategy for the efficient delivery of the NTPDase-based treatment of CNS disorders, and seems a good therapeutic method.

Purine signaling and potential new therapeutic approach: possible outcomes of NTPDase inhibition.

The development of specific molecules targeting purinergic signaling, more specifically the inhibition of NTPDase and their impact on the different physiological systems are covered.

Polyoxometalates--a new class of potent ecto-nucleoside triphosphate diphosphohydrolase (NTPDase) inhibitors.

Therapeutic Potentials of Ecto‐Nucleoside Triphosphate Diphosphohydrolase, Ecto‐Nucleotide Pyrophosphatase/Phosphodiesterase, Ecto‐5′‐Nucleotidase, and Alkaline Phosphatase Inhibitors

Most recent and significant advances in field of NTPDase, NPP, AP, and e5NT inhibitors is being discussed in detail in anticipation of providing prolific leads and relevant background for research groups interested in synthesis of selective ecto‐nucleotidase inhibitors.

The E-NTPDase family of ectonucleotidases: Structure function relationships and pathophysiological significance

It appears that the spatial and temporal expression of NTPDases by various cell types within the vasculature, the nervous tissues and other tissues impacts on several patho-physiological processes.