685904-18-1Relevant articles and documents
Metabolically stable 5-HMF derivatives for the treatment of hypoxia
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Page/Page column 21-23, (2020/11/23)
5-HMF derivative compounds that bind covalently with hemoglobin are provided. Methods of treating sickle cell disease and other hypoxia-related disorders by administering such compounds are also provided.
PRODRUG AND PROTECTED FORMS OF 5-HYDROXYMETHYLFURFURANAL (5-HMF) AND ITS DERIVATIVES
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Page/Page column 36, (2018/02/27)
Prodrugs and derivatives of 5-hydoxymethyl-2-furfural (5-HMF) with protected or modified aldehyde and/or alcohol moieties are provided. The prodrugs or derivatives exhibit increased bioavailability, e.g. due to having extended half-lives in circulation. The drugs are therefore administered i) at lower doses and/or ii) less frequently than 5-HMF, while still maintaining the beneficial therapeutic effects of 5-HMF.
Synthesis of the insecticide prothrin and its analogues from biomass-derived 5-(chloromethyl)furfural
Chang, Fei,Dutta, Saikat,Becnel, James J.,Estep, Alden S.,Mascal, Mark
, p. 476 - 480 (2014/02/14)
Prothrin, a synthetic pyrethroid insecticide, was synthesized from the biomass-derived platform chemical 5-(chloromethyl)furfural in six steps and overall 65% yield. Two structural analogues of prothrin were also prepared following the same synthetic approach. Preliminary testing of these furan-based pyrethroids against the yellow fever mosquito Aedes aegypti indicates promising insecticidal activities.
Synthesis of the insecticide prothrin and its analogues from biomass-derived 5-(Chloromethyl)furfural
Chang, Fei,Dutta, Saikat,Becnel, James J.,Estep, Alden S.,Mascal, Mark
, p. 476 - 480 (2015/04/22)
Prothrin, a synthetic pyrethroid insecticide, was synthesized from the biomass-derived platform chemical 5-(chloromethyl)furfural in six steps and overall 65% yield. Two structural analogues of prothrin were also prepared following the same synthetic approach. Preliminary testing of these furan-based pyrethroids against the yellow fever mosquito Aedes aegypti indicates promising insecticidal activities.
Synthesis of exo-3-ammo-7-azabicyclo[2.2.1]heptanes as a class of malarial aspartic protease inhibitors: Exploration of two binding pockets
Zuercher, Martina,Hof, Fraser,Barandun, Luzi,Schuetz, Andri,Schweizer, W. Bernd,Meyer, Solange,Bur, Daniel,Diederich, Francois
supporting information; experimental part, p. 1707 - 1719 (2009/08/09)
The increasing prevalence of drug-resisLant strains of malaria-causing Plasmodium parasites necessitates the development of therapeutic agents that inhibit new biochemical targets. We herein describe the design, synthesis, and in vitro evaluation of a class of inhibitors that target the malarial aspartic proteases known as the plasmepsins. The title compounds feature a 7-azanorbornane skeleton that bears an exo-amino function, which was designed to interact with the catalytic dyad of aspartic proteases while providing vectors for the attachment of binding elements that target the flap and S1/S3 binding pockets at. the enzyme active site. Their synthesis takes advantage of a solvent-free and highly diastereoselective conjugate addition of amines to bicyclic vinyl sulfones. Structural optimization based on a little-known conformational preference of aryl sulfones produced the most potent inhibitors of this new class. In vitro assays demonstrate that the title compounds are capable of potent (IC50 ≥ 1.0 nM) inhibition of plasmepsins, while remaining relatively weak inhibitors of the closely related human enzymes cathepsins D and E. The ideal occupation of the flap pocket is crucial for both potency and selectivity over the human proteases. Differently functionalized compounds were synthesized to gain new insights info the molecular recognition properties of this cavity. Wiley-VCH Verlag GmbH & Co. KGaA.
2 - SUBSTITUTED HETEROCYCLIC COMPOUNDS AND ANTITUMOR COMPOSITION COMPRISING THE SAME
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Page 13-14; 87-88, (2010/02/06)
The present invention relates with 2-substituted heterocyclic compounds and antitumor composition comprising the same. The compound according to the present invention exhibits superior effect as telomerase inhibitor based on new mechanism (terlomere-terlomerase) which can resolve the problems occurring at the time of using chemotherapeutics, i.e side effects and cross resistance between related mechanism on using chemotherapeutics. In addition, the antitumor composition comprising the compound of the present invention exhibits superior effect in inhibiting the growth of cancer cell.