Spiro Compounds

Publication Title: 
Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America

BACKGROUND: Artemisinin-based combination therapy is the first-line treatment for uncomplicated falciparum malaria. This study assessed the antimalarial efficacy and safety of a combination of 150 mg of arterolane maleate and 750 mg of piperaquine phosphate (AM-PQP) in comparison to Coartem (artemether and lumefantrine) in patients with acute uncomplicated P. falciparum malaria. METHODS: In this open-label, randomized, multicentric, parallel group clinical trial, 240 patients were randomized to receive AM-PQP (160 patients) or Coartem (80 patients). Patients with P.

Author(s): 
Valecha, Neena
Krudsood, Srivicha
Tangpukdee, Noppadon
Mohanty, Sanjib
Sharma, S. K.
Tyagi, P. K.
Anvikar, Anupkumar
Mohanty, Rajesh
Rao, B. S.
Jha, A. C.
Shahi, B.
Singh, Jai Prakash Narayan
Roy, Arjun
Kaur, Pawandeep
Kothari, Monica
Mehta, Shantanu
Gautam, Anirudh
Paliwal, Jyoti K.
Arora, Sudershan
Saha, Nilanjan
Publication Title: 
Molecular Medicine (Cambridge, Mass.)

Semisynthetic artemisinin-based therapies are the first-line treatment for P. falciparum malaria, but next-generation synthetic drug candidates are urgently required to improve availability and respond to the emergence of artemisinin-resistant parasites. Artemisinins are embryotoxic in animal models and induce apoptosis in sensitive mammalian cells. Understanding the cytotoxic propensities of antimalarial drug candidates is crucial to their successful development and utilization.

Author(s): 
Copple, Ian M.
Mercer, Amy E.
Firman, James
Donegan, Gail
Herpers, Bram
Wong, Michael Hl
Chadwick, James
Bringela, Andreia D.
Cristiano, Maria L. S.
van de Water, Bob
Ward, Stephen A.
O'Neill, Paul M.
Park, B. Kevin
Publication Title: 
Antimicrobial Agents and Chemotherapy

The declining efficacy of artemisinin derivatives against Plasmodium falciparum highlights the urgent need to identify alternative highly potent compounds for the treatment of malaria. In Papua Indonesia, where multidrug resistance has been documented against both P. falciparum and P.

Author(s): 
Marfurt, Jutta
Chalfein, Ferryanto
Prayoga, Pak
Wabiser, Frans
Wirjanata, Grennady
Sebayang, Boni
Piera, Kim A.
Wittlin, Sergio
Haynes, Richard K.
Möhrle, Jörg J.
Anstey, Nicholas M.
Kenangalem, Enny
Price, Ric N.
Publication Title: 
Malaria Journal

BACKGROUND: Semi-synthetic artemisinin derivatives are powerful peroxidic drugs in artemisinin-based combination therapy (ACT) recommended as first-line treatment of Plasmodium falciparum malaria in disease-endemic countries. Studies by Eckstein-Ludwig and co-workers showed both thapsigargin and artemisinin specifically inhibit the sarcoplasmic reticulum Ca²?-ATPase of Plasmodium falciparum (PfATP6). In the present study the type of interaction between thapsigargin and artemisinin derivatives as well as the ozonide OZ277 (RBx11160 or arterolane) was evaluated in parasite cultures.

Author(s): 
Abiodun, Oyindamola O.
Brun, Reto
Wittlin, Sergio
Publication Title: 
Antimicrobial Agents and Chemotherapy

Novel synthetic endoperoxides are being evaluated as new components of artemisinin combination therapies (ACTs) to treat artemisinin-resistant Plasmodium falciparum malaria. We conducted blinded ex vivo activity testing of fully synthetic (OZ78 and OZ277) and semisynthetic (artemisone, artemiside, artesunate, and dihydroartemisinin) endoperoxides in the histidine-rich protein 2 enzyme-linked immunosorbent assay against 200 P. falciparum isolates from areas of artemisinin-resistant malaria in western and northern Cambodia in 2009 and 2010.

Author(s): 
Lanteri, Charlotte A.
Chaorattanakawee, Suwanna
Lon, Chanthap
Saunders, David L.
Rutvisuttinunt, Wiriya
Yingyuen, Kritsanai
Bathurst, Ian
Ding, Xavier C.
Tyner, Stuart D.
Publication Title: 
Molecular Pharmacology

Germander, a plant used in folk medicine, caused an epidemic of cytolytic hepatitis in France. In about half of these patients, a rechallenge caused early recurrence, suggesting an immunoallergic type of hepatitis. Teucrin A (TA) was found responsible for the hepatotoxicity via metabolic activation by CYP3A. In this study, we describe the presence of anti-microsomal epoxide hydrolase (EH) autoantibodies in the sera of patients who drank germander teas for a long period of time.

Author(s): 
De Berardinis, V.
Moulis, C.
Maurice, M.
Beaune, P.
Pessayre, D.
Pompon, D.
Loeper, J.
Publication Title: 
Chemical & Pharmaceutical Bulletin

Two new steroidal saponins were isolated from the Chinese folk medicine called Gualou-xiebai-baijiu-tang. The structures were determined to be spirost 25(27)-ene-2beta,3beta-diol-3-O-beta-D-glucopyranosyl(1-->2)-beta-D-galactopyranoside and 26-O-beta-D-glucopyranosyl-22alpha-hydroxy-5beta-furost-25(27)-ene-1beta,3beta,6beta,26-tetraol-3-O-beta-D-galactopyranoside, respectively, based on chemical evidences and spectral analysis.

Author(s): 
He, Xiangjiu
Qiu, Feng
Shoyama, Yukihiro
Tanaka, Hiroyoki
Yao, Xinsheng
Publication Title: 
Chemistry & Biology

Natural products endowed with neuromodulatory activity and their underlying structural scaffolds may inspire the synthesis of novel neurotrophic compound classes. The spirocyclic secoyohimbane alkaloid rhynchophylline is the major component of the extracts of Uncaria species used in Chinese traditional medicine for treatment of disorders of the central nervous system.

Author(s): 
Antonchick, Andrey P.
López-Tosco, Sara
Parga, Juan
Sievers, Sonja
Schürmann, Markus
Preut, Hans
Höing, Susanne
Schöler, Hans R.
Sterneckert, Jared
Rauh, Daniel
Waldmann, Herbert

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