Antiprotozoal Screening Compound Library

Parasitic diseases, usually found in tropical regions of the world, have serious health, social and economic impacts. Among all of the parasites, protozoan parasites, such as Trypanosomacruzi, Leishmania mexicana, Plasmodium falciparum, Giardia intestinalis, and Trichomonas vaginalis, are the main disease-causing organisms. Diseases caused by protozoan parasites can cause a considerable mortality and morbidity. Nowadays, the number of deaths caused by protozoan diseases is increasing every year and there is still a lack of effective drugs against parasitic diseases due to the resistance and toxicity of current antiprotozoal drugs. Many researchers and scientists are committed to searching for new drugs against protozoan parasites.

BOC Sciences’ well-developed Antiprotozoal Screening Compound Library contains over 8,200 small-molecule screening compounds with desired antiprotozoal activity against major protozoan diseases.

Antiprotozoal drugs. Figure 1. Antiprotozoal drugs. (Oster, N.; Lanzer, M. 2004)

Library Design

a. At BOC Sciences, a reference set of molecules with reported antiprotozoal activity are collected from a wide range of commercially available databases

b. Then, a 2D molecular fingerprints search has been employed against our HTS Compound Collection for compound selection.

Here is the targeted protozoa families:

  • Cryptosporidium parvum
  • Plasmodium (P.berghei, P.falciparum)
  • Entamoeba histolytica
  • Schistosoma mansoni
  • Giardia (G.intestinalis)
  • Toxoplasma gondii
  • Leishmania (L.amazonensis, L.braziliensis, L.chagasi, L.donovani, L.major)
  • Trichomonas vaginalis
  • Trypanosoma brucei (T.brucei(brucei & rhodesiense), T.cruzi (normal & strain CL Brener))

c. The 80% similarity threshold (Tanimoto) and selected compounds for the following molecular targets are selected to search the HTS compound collection for analogues of molecules with known activity against different protozoan targets:

  • Cannabinoid CB1 receptor
  • Falcipain 2 cysteine protease
  • Carbonic anhydrase I and II
  • Glutamate NMDA receptor
  • Cathepsin L endopeptidase
  • Glyceraldehyde-3-phosphate dehydrogenase
  • Cdc2-related kinase
  • Ser/thr-protein kinase Aurora-B
  • Cruzipain cysteine protease
  • Sterol 14-alpha demethylase

Antiprotozoal Screening Compound Library Characteristics

  • No PAINS or toxic substances/unwanted functions: filtered by strict ‘Ro5-like’ physicochemical and most stringent in-house structural filters
  • Confirmed bioactivity and safety via preclinical studies and clinical trials
  • This unique library is developed based on the most reliable inhibitor databases with the inhibitory activity data lower than 10 μM validated by bioassay
  • All of the compounds have potential antiprotozoal activity against major protozoan diseases such as giardiasis, leishmaniasis, malaria, trichomoniasis, and trypanosomiasis, etc.
  • Structural diversity, significant efficacy, and cellular penetration
  • Structural document, IC50, and other chemical and biological data are provided
  • Tanimoto index ≥ 0.80
  • All compounds are continually updated
  • Compound cherry-picking service is provided

What We Deliver

  • Delivered within 2 weeks in any customer-preferred format
  • Powders, dry films or DMSO solutions formatted in vials, 96 or 384-well plates
  • All compounds have a minimum purity of 90% assessed by 1H NMR and HPLC
  • Analytical data is provided

BOC Sciences provides professional, rapid and high-quality services of Antiprotozoal Screening Compound Library design at competitive prices for global customers. Personalized and customized services of Antiprotozoal Screening Compound Library design can satisfy any innovative scientific study demands. Our clients have direct access to our staff and prompt feedback to their inquiries. If you are interested in our services, please contact us immediately!

Reference

  1. Oster, N.; Lanzer, M. Antiprotozoal Drugs. Katzung & Trevor's Pharmacology: Examination & Board Review. 2004. 11e.
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Services Based on the Chemical Library Design Platform

Services Based on the Chemical Library Design Platform

BOC Sciences has rich experience in working with global customers in custom library synthesis of compounds and generating small to medium-sized libraries of target compounds. Our knowledge in generating a large number of target molecules in a remarkably shorter time enables quick biological screenings for affinities. With the target properties in mind, we deliver target molecules, by applying our extensive knowledge in drug discovery.

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