Synthesis of Arylpiperazines as Perspective Toxoplasma gondii Dihydrofolate Reductase Inhibitors

Summary of the technology

Our company offers the chemical optimization service - synthesis of a unique DHFR targeted set of novel arylpiperazine derivatives for your biological projects, related to developing of anti-toxoplasmosis drugs.

Otava Research Institute

Details of the Technology Offer

Toxoplasmosis is a parasitic disease caused by Toxoplasma gondii. Approximately one-third of the population worldwide is chronically infected with T. gondii. First-line treatment of toxoplasmosis is a therapy based on dihydrofolate reductase (DHFR, DHFRP1, DYR)inhibitors which act on the folate metabolic pathway, thereby inhibiting T. gondii proliferation and survival.

Our company offers the chemical optimization service - synthesis of a unique DHFR targeted set of novel arylpiperazine derivatives for your biological projects, related to developing of anti-toxoplasmosis drugs. These novel compounds could be selected from a set of 1,000+ exclusive virtual arylpiperazines using our company’s proprietary molecular modeling platform ODDA™.

This target-specific set of novel arylpiperazine derivatives will be synthesized exclusively upon your request.

A recent paper from the Journal of Medicinal Chemistry* showed that authors synthesized a series of arylpiperazines through structural modification of TRC-19 (a lead compound from their previous study, IC50 = 8.76 nM). Among them, compound 3 (5-(4-(3-(2-methoxypyrimidin-5-yl)phenyl)piperazin-1-yl)pyrimidine-2,4-diamine) showed activity against dihydrofolate reductase of T. gondii (IC50 = 1.57 nM) and good selectivity ratio between Human DHFR and Toxoplasma DHFR

Related Keywords

  • Biological Sciences
  • Medicine, Human Health
  • Medical Technology / Biomedical Engineering
  • Genetic Engineering / Molecular Biology
  • Medical Health related
  • toxoplasma gondii

About Otava Research Institute

Otava Institute is a global provider of one-stop integrated research solutions for business and life science. Our team includes chemists, biologists, physicists whose combined efforts contribute to the complex contract research projects for pharmaceutical, agro, cosmetic and material science industries.We are dedicated to providing clients with outstanding service in these key areas and will continue to push boundaries to remain an industry front-runner. Each day we expand our core competencies delivering of new technologies to meet all the customer’s needs.

Our location in Toronto Ontario, Canada provides our clients with the added advantage of North American IP rules and regulations and secure communication and logistics. Our Ukraine – based R&D facilities represented with the Ukrainian Laboratories, that is cooperating with leading Ukrainian research institutions and carries out research work in the format of outsourcing.

We work as a preferred partner to many of the world’s top 10 pharma firms, and hundreds of other companies, providing support with creative solutions for complex technical compound issues. Our scientific knowledge, combined with our research and manufacturing capability, enables us to support chemical processing and production without ever compromising on quality.

Our experience, dedication, and commitment to quality make us an ideal partner for discovery stage research.

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