scholarly journals Total Synthesis of (+)-Spiroindimicin A via Asymmetric Palladium-Catalyzed Spirocyclization

2021 ◽  
Author(s):  
Zhen Zhang ◽  
Sneha Ray ◽  
Leah Imlay ◽  
Lauren Callaghan ◽  
Hanspeter Niederstrasser ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Human Health ◽  
Neglected Tropical Diseases ◽  
Indole Alkaloids ◽  
Sleeping Sickness ◽  
Tropical Diseases ◽  
African Sleeping Sickness ◽  
Palladium Catalyzed ◽  
Natural Precursor

<p>The spiroindimicins are a unique class of chlorinated indole alkaloids characterized by three heteroaromatic rings structured around a congested spirocyclic stereocenter. Here, we report the first total synthesis of (+)-spiroindimicin A, which bears a challenging C-3’/C-5’’-linked spiroindolenine. We detail our initial efforts to effect a biomimetic oxidative spirocyclization from its proposed natural precursor, lynamicin D, and describe how these studies shaped our final abiotic 9-step solution to this complex alkaloid built around a key asymmetric Pd-catalyzed spirocyclization. Scalable access to spiroindimicins A, H, and their congeners has enabled discovery of their activity against several parasites relevant to human health, providing potential starting points for new therapeutics for the neglected tropical diseases leishmaniasis and African sleeping sickness.</p>

scholarly journals Total Synthesis of (+)-Spiroindimicin A via Asymmetric Palladium-Catalyzed Spirocyclization

2021 ◽  
Author(s):  
Zhen Zhang ◽  
Sneha Ray ◽  
Leah Imlay ◽  
Lauren Callaghan ◽  
Hanspeter Niederstrasser ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Human Health ◽  
Neglected Tropical Diseases ◽  
Indole Alkaloids ◽  
Sleeping Sickness ◽  
Tropical Diseases ◽  
African Sleeping Sickness ◽  
Palladium Catalyzed ◽  
Natural Precursor

<p>The spiroindimicins are a unique class of chlorinated indole alkaloids characterized by three heteroaromatic rings structured around a congested spirocyclic stereocenter. Here, we report the first total synthesis of (+)-spiroindimicin A, which bears a challenging C-3’/C-5’’-linked spiroindolenine. We detail our initial efforts to effect a biomimetic oxidative spirocyclization from its proposed natural precursor, lynamicin D, and describe how these studies shaped our final abiotic 9-step solution to this complex alkaloid built around a key asymmetric Pd-catalyzed spirocyclization. Scalable access to spiroindimicins A, H, and their congeners has enabled discovery of their activity against several parasites relevant to human health, providing potential starting points for new therapeutics for the neglected tropical diseases leishmaniasis and African sleeping sickness.</p>

scholarly journals Glasgow encounters with tropical diseases

Parasitology ◽  
2017 ◽  
Vol 144 (12) ◽  
pp. 1561-1566
Author(s):  
FRANCIS E. G. COX
Keyword(s):  
Wide Spectrum ◽  
Life Cycles ◽  
Sleeping Sickness ◽  
Parasitic Diseases ◽  
Tropical Diseases ◽  
Special Issue ◽  
African Sleeping Sickness ◽  
History Of ◽  
The University ◽  
The Tropics

SUMMARYThe period 1875–1925 was remarkable in the history of parasitology mainly for the elucidation of the life cycles of parasites causing important parasitic diseases and the incrimination of vectors in their transmission. These discoveries were made by a small number of scientists working in the tropics a number of whom were Scots. Sir Patrick Manson, the discoverer of the mosquito transmission of filarial worms, was instrumental in directly or indirectly encouraging other Scots including Douglas Argyll-Robertson, David Blacklock, David Bruce, David Cunningham, Robert Leiper, William Leishman, George Low, Muriel Robertson and Ronald Ross, who all made significant discoveries across a wide spectrum of tropical diseases. Among these, William Leishman, Robert Leiper and Muriel Robertson were all graduates of the University of Glasgow and their achievements in the fields of leishmaniasis, schistosomiasis, dracunculiasis and African sleeping sickness, together with subsequent developments in these fields, are the subjects of the ten papers in this Special Issue of Parasitology.

scholarly journals From Colonial Research Spirit to Global Commitment: Bayer and African Sleeping Sickness in the Mirror of History

2020 ◽  
Vol 5 (1) ◽  
pp. 42
Author(s):  
Ulrich-Dietmar Madeja ◽  
Ulrike Schroeder
Keyword(s):  
Life Cycle ◽  
Trypanosoma Brucei ◽  
Human African Trypanosomiasis ◽  
Sleeping Sickness ◽  
Early 20Th Century ◽  
Tropical Diseases ◽  
Brand Name ◽  
African Sleeping Sickness ◽  
Medical Progress ◽  
Equatorial Africa

In the early 20th century, a series of epidemics across equatorial Africa brought African sleeping sickness (human African trypanosomiasis, HAT) to the attention of the European colonial administrations. This disease presented an exciting challenge for microbiologists across Europe to study the disease, discover the pathogen and search for an effective treatment. In 1923, the first “remedy for tropical diseases”—Suramin—manufactured by Bayer AG came onto the market under the brand name “Germanin.” The development and life cycle of this product—which today is still the medicine of choice for Trypanosoma brucei (T.b), hodesiense infections—reflect medical progress as well as the successes and failures in fighting the disease in the context of historic political changes over the last 100 years.

THE ROLE OF EBM AND CLINICAL PRACTICE GUIDELINES IN GENERATING RESEARCH AND INTERVENTIONS IN NEGLECTED TROPICAL DISEASES: A RATIONAL MODEL FOR DEVELOPING COUNTRIES

2020 ◽  
Author(s):  
Cristhian David Morales-Plaza
Keyword(s):  
Developing Countries ◽  
Clinical Practice ◽  
Clinical Practice Guidelines ◽  
Practice Guidelines ◽  
Neglected Tropical Diseases ◽  
Tropical Diseases ◽  
Rational Model ◽  
Clinical Practices ◽  
Vulnerable Communities

Guarantee better clinical practices among clinicians who attend NTDs in developing countries as well as provide education in vector control in hotspot vulnerable communities

Sign in / Sign up

Export Citation Format

Share Document