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Benzoxaboroles: A New Potential Drug for African Sleeping Sickness



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Life cycle of the Trypanosoma brucei parasites, source: CDC

Human African trypanosomiasis, caused by the kinetoplastid parasite Trypanosoma brucei, affects thousands of people across sub-Saharan Africa, and is fatal if left untreated. Treatment options for this disease, particularly stage 2 disease, which occurs after parasites have infected brain tissue, are limited due to inadequate efficacy, toxicity, and the complexity of treatment regimens.

We have discovered and optimized a series of benzoxaborole- 6-carboxamides to provide trypanocidal compounds that are orally active in murine models of human African trypanosomiasis. A key feature of this series is the presence of a boron atom in the heterocyclic core structure, which is essential to the observed trypanocidal activity. We also report the in vivo pharmacokinetic properties of lead compounds from the series and selection of SCYX-7158 as a preclinical candidate.

Human African trypanosomiasis (HAT), more commonly known as African sleeping sickness, is caused by two subspecies of the kinetoplastid parasite Trypanosoma brucei, Trypanosoma brucei gambiense and Trypanosoma brucei rhodesiense, which are introduced into the victim through the bite of the tse-tse fly. Endemic across sub-Saharan Africa, tens of thousands of people are infected each year, with millions at risk of contracting the disease. If not treated early in the progression of the disease, the T. brucei parasites migrate across the blood–brain barrier and reside in brain tissue, ultimately causing neuronal death leading to a multitude of neurological symptoms including hallucinations, sleep disorders, coma and, ultimately, death.

Current treatment options for HAT are inadequate due to lack of efficacy, particularly once the parasites have migrated to the brain (stage 2 HAT), toxicity and the complexity of treatment regimens. The most commonly used treatment for stage 2 HAT, melarsoprol is highly toxic, with an estimated 5–10% drug-related mortality. A more recent drug, eflornithine, while effective against T.b. gambiense, is not effective against T.b. rhodesiense, and must be administered in a complex intravenous regime that is impractical in disease-endemic areas.

Consequently, there is an urgent need for new drugs to treat HAT and, in particular, a need for a safe, orally active drug that is effective against all known strains of T. brucei and is effective in stage 2 HAT


  1. haresh bavadiya says:

    hats good info…

  2. medchemnintabelle says:

    Reblogged this on MedCheminAustralia.

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DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with GLENMARK PHARMACEUTICALS LTD, Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 30 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, Dr T.V. Radhakrishnan and Dr B. K. Kulkarni, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 30 year tenure till date Dec 2017, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 9 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 50 Lakh plus views on dozen plus blogs, He makes himself available to all, contact him on +91 9323115463, email, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 19 lakh plus views on New Drug Approvals Blog in 216 countries...... , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc

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