Synthesis of Arylpiperazines as Perspective Toxoplasma gondii Dihydrofolate Reductase Inhibitors

Type: 
Sell
Cooperation
Short description of advertisement: 
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.

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

Contact person: 
Nadiia Kachaput
Contact languages: 
English
Russian
Ukrainian
Country: 
Ukraine
Address: 
150a Zabolotnogo St., Suite 32
Phone: 
+380-989914813
E-mail: 
ukraine [at] otavachemicals [dot] com
Proposal valid till: 
Monday, 29 June, 2020