36 results about "Antimalarial medication" patented technology

Methods of treating malaria comprising administration of compounds of Formula (I′) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. It also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin X, plasmepsin IX or plasmepsin X and IX activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

Provided are methods of treating malaria comprising administration of compounds of Formula (I) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. Also provided are uses of the compounds of Formula (I), as defined herein, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

The present invention provides methods of treating malaria comprising administration of compounds of Formula (I) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. The invention also provides uses of the compounds of Formula (I), as defined herein, for the possible inhibition of plasmepsin X, plasmepsin IX or plasmepsin X and IX activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

The invention relates to application of a mir-331-3p inhibitor in preparation of a medicine for inhibiting malaria mosquito transmission, and belongs to the technical field of biological medicine. Aiming at the technical problems that the existing anti-malarial drug mainly acts on the later stage of plasmodium development and is lack of an effective propagation blocker, the invention provides the miR-331-3p inhibitor which is used for blocking the formation of plasmodium oocysts by inhibiting the interaction between microRNA and a mosquito target gene spetzle. Experiments show that the inhibitor can reduce the mosquito infection rate by about 50%, and has the characteristics of high targeting property, simplicity in operation and the like. The invention provides a novel drug development target for blocking malaria transmission, can effectively supplement the prevention and control blind area of the existing anti-malarial drug, and has important application value in the field of mosquito-borne infectious disease control.

The present disclosure generally relates to substituted heteroaromatic compounds. The invention relates to novel substituted 4-heteroatom-isoquinolone compounds, and isomers, derivatives, analogues and / or salt forms thereof of formula I; and its process of preparation thereof. Furtherore, the present invention relates to a process of preparation of various drugs / APIs / alkaloids e.g. Ampikin APIs such as CX-614, CX-554, DRF-2655, ITF-296, ITF-1129, Raititrexed, Deoxyvasicinone family of quinazolinone alkaloids, etc. using said formula I compound as starting material. The compound of formula I acts as antimalarial agent, anticancer agent, neuroprotective agent and so on. Formula I

To provide a new antimalarial agent that achieves a balance between strong antimalarial activity and low cytotoxicity.SOLUTION: An antimalarial agent comprising an ethanol extract and / or a methanol extract of at least one plant selected from the group consisting of Ficus hispida, Streblus asper, Boerhavia repens, Clerodendrum viscosum, Amaranthus spinosus, and Mussaenda corymbosa.SELECTED DRAWING: None

This invention provides the application of Pulsatilla saponin B4 in the preparation of antimalarial drugs, which can significantly improve weight loss, peripheral blood parasitemia, and survival rate in mice infected with lethal Plasmodium. Its mechanism of action is not to directly kill Plasmodium, but to regulate the host immune system, including activating T / B cell immune responses, upregulating pro-inflammatory factors and interferon signaling pathways, and downregulating Arg1 expression. At the same time, Pulsatilla saponin B4 can alleviate immunopathological damage to organs such as the spleen and liver, restore the homeostasis of the spleen's immune microenvironment, and protect the normal structure of tissues. As a natural product, this compound has the characteristics of multiple targets and low toxicity, and has the dual advantages of anti-infection and immune homeostasis regulation, showing good prospects for clinical application and translation.

Disclosed herein are methods and compositions for treating and / or preventing Plasmodium falciparum malaria by administering a compound that mimics the binding of anti-Plasmodium falciparum Glutamic Acid Rich Protein (PfGARP).

The present application relates to a preparation of a 7,7'-epoxy lignan compound and its application in preparing anti-malaria products, and belongs to the field of traditional Chinese medicine and natural medicine pharmacy. The anti-malaria medicine with the compound as an active ingredient. The present application expands the medicinal value of 7,7'-epoxy lignan compounds in Rhodiola henryi.

The present invention discloses a functionalized isoquinolone and quinolone compounds and an efficient transition-metal-free approach for the synthesis of the same. The invention provides a highly functionalized isoquinolones from the reaction of dimethyl-2-((phenylamino)methylene) malonate with aryne precursors under mild. The reaction proceeds through insertion of aryne into the C−C σ-bond, which offers a novel and practical entry to access a wide range of isoquinolones with enhanced yields. The substrate scope is broad as the process can stands a variety of functional groups and the application of the developed process has been demonstrated in the total synthesis of antimalarial agent SJ000101247. Also, the highly functionalized quinolones are also useful in the synthesis of floxacins based compounds and derivatives e.g. ciprofloxacin, norfloxacin, G003967, etc.

The present invention relates to the technical field of drug application. Disclosed are patchouli alcohol, a patchouli alcohol compound antimalarial composition, and a use in preparation of an anti-plasmodial drug. The antimalarial pharmaceutical composition is a composition of artesunate and patchouli alcohol. By compounding patchouli alcohol and artesunate, synergistic antimalarial activity can be produced; and by reducing the plasmodium infection rate in red blood cells, patchouli alcohol and the compound antimalarial composition alleviate edema and inflammation in the liver and the spleen caused by malaria, and decrease haemozoin deposition in the liver and the spleen, having minimal toxic and side effects on the liver while exerting the antimalarial activity. The antimalarial effect of patchouli alcohol is obviously superior to that of patchouli oil, the antimalarial effect of the composition of artesunate and patchouli alcohol is obviously superior to that of artesunate or patchouli alcohol used alone, and patchouli alcohol and the composition of artesunate and patchouli alcohol especially have a more obvious inhibitory effect on artesunate-resistant plasmodium.

The present invention belongs to the field of biomedical technology, and specifically relates to the application of Lactobacillus murinus driving GABA in the treatment of cerebral malaria in mice. The present invention found significantly enriched Lactobacillus murinus and confirmed that Lactobacillus murinus can produce GABA. Subsequently, in a mouse cerebral malaria model, the effects of Lactobacillus murinus and GABA on improving and treating mouse cerebral malaria were evaluated when Lactobacillus murinus and GABA were used alone or in conjunction with dihydroartemisinin. The results showed that whether used alone or in combination with dihydroartemisinin, the bacteria and its metabolite GABA can effectively improve mouse behavior, immune pathological damage to various organs, reduce parasitemia, and prolong mouse survival. Compared with the use of drugs alone, it can effectively treat mouse cerebral malaria. From the perspective of using probiotics to drive their metabolites to assist antimalarial drugs in the treatment of mouse cerebral malaria, the present invention provides a new solution for the treatment of severe malaria caused by falciparum malaria, especially human cerebral malaria.

The invention discloses an artemisinin compound containing a piperazine side chain or a pharmaceutical salt thereof, and the structural general formula is shown in the specification. The artemisinin compound containing the piperazine side chain and the pharmaceutical salt thereof provided by the invention have a brand-new skeleton structure and better anti-malaria and anti-tumor activity, can be used as an anti-tumor drug and an anti-malarial drug, and can be used as an anti-malarial drug. And more choices can be provided for clinical treatment.

The invention belongs to the field of compound synthesis, and discloses an epsilon-caprolactam compound containing a guanidyl structural unit and preparation and application of the epsilon-caprolactam compound, the chemical structure of the epsilon-caprolactam compound is shown in the specification, and the epsilon-caprolactam compound containing the guanidyl structural unit has good anti-malarial activity and is expected to become a novel drug intermediate. The compound is used for preparing antimalarial drugs. The invention also discloses a preparation method of the epsilon-caprolactam compound containing the guanidyl structural unit. The preparation method of the epsilon-caprolactam compound containing the guanidyl structural unit has the advantages that the raw materials and the catalyst are cheap and easy to obtain; reaction conditions are mild, and operation is simple and convenient; and the method has the advantages of wide substrate universality, high yield for a series of epsilon-caprolactam products containing guanidyl structural units, and the like.

The invention discloses application of a naturally-sourced small molecule compound and a pharmaceutical composition thereof in preparation of antimalarial drugs, and belongs to the technical field of biological medicines. The small molecule compound is PHPP, the CAS number of the small molecule compound is 252205-23-5, and the structure of the small molecule compound is shown in the specification. According to the invention, the small molecule compound PHPP, which is a specific monomer component, is screened from natural products for the first time and is proved to have remarkable anti-malarial activity, and the cognitive blank of the anti-malarial application of the small molecule compound is filled up; the compound not only has an excellent in-vitro anti-malarial effect, but also has no obvious cytotoxicity under an effective concentration and is high in safety; more importantly, when the compound is combined with artemisinin, a remarkable synergistic effect can be generated, a brand new solution is provided for solving the problem of severe artemisinin drug resistance, and candidate lead compounds and combination schemes with wide prospects are provided for developing new-generation antimalarial drugs.

The invention provides a compound containing an artemisinin similar structure and a preparation method and application of the compound, the structural formula of the compound is shown in the formula I. The compound has excellent histone deacetylase inhibitory activity and anti-tumor and anti-malarial activity and can be used for preparing anti-tumor and anti-malarial drugs.

The present invention is related to the telotristat ethyl compound for use in the treatment of malaria and / or the prevention and treatment of the complications thereof. The present invention also concerns a combination of the telotristat ethyl compound and of at least one antimalarial drug conventionally used for treatment of the subject with malaria, and a kit comprising the telotristat ethyl compound inside a container, and one or more antimalarial drugs in one or more containers. Furthermore, the present invention is related to a process for the preparation of the telotristat ethyl.

The synthesis and characterization of a series of derivatives and analogs based on the 9-aminoacridine scaffold shared by antimalarial drugs quinacrine and pyronaridine are described. Also described is the structure-activity relationship of these compounds against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the virus that causes the coronavirus disease of 2019 (COVID-19). Several compounds displayed potent in vitro activity, with 50% inhibitory concentrations below 1 micromolar.

The invention discloses an artemisinin compound containing a 10-bit ether side chain or a pharmaceutical salt thereof, the structural general formula is one of the following structures: the artemisinin compound containing the 10-bit ether side chain provided by the invention has a relatively obvious proliferation inhibition effect on liver cancer HepG2, lung cancer A549, intestinal cancer HCT116, hematologic tumors MV-4-11 and HL-60; the anti-tumor activity of part of the compounds is higher than that of commercially available drugs SAHA and belinostat, and the compounds are expected to be developed into novel anti-tumor drugs. In addition, the performance of a plurality of compounds is superior to the in-vitro antimalarial activity of artemisinin, and the compounds are expected to be developed into novel antimalarial drugs.

The present invention recognizes that there is a need for the prophylaxis or treatment of COVID and COVID-19. A first aspect of the present invention generally relates to methods of prophylaxis or treatment of COVID or COVID-19 using various pharmaceutical compositions. A second aspect of the present invention generally relates to methods of prophylaxis or treatment of COVID or COVID-19 using combinations of antimalarial drugs and antiviral drugs. A third aspect of the present invention generally relates to methods of prophylaxis or treatment of COVID or COVID-19 using nanoparticle formulations that include pharmaceutical compositions. A fourth aspect of the present invention generally relates to methods of prophylaxis or treatment of COVID or COVID-19 using combinations of various pharmaceutical compositions. A fifth aspect of the present invention generally relates to methods of prophylaxis or treatment of COVID or COVID-19 using a polio vaccine and pharmaceutical compositions.

The present invention relates to dosing regimen of a new antimalarial drug, as monotherapy or combination therapy.

The invention discloses a method for inducing polarization of macrophages by AKK and / or outer membrane vesicles thereof and application of AKK and / or outer membrane vesicles thereof in preparation of drugs for promoting phagocytosis and infection of erythrocytes by macrophages, and belongs to the technical field of biological medicines. According to the invention, after macrophages are induced by AKK bacteria or OMVs thereof, an M1 polarization phenomenon occurs. Macrophages polarized by M1 generate proinflammatory factors, and meanwhile, erythrocytes infected by plasmodium are subjected to more phagocytosis. Compared with macrophages not polarized by M1, the macrophages polarized by M1 induced by AKK bacteria or AKK-OMVs can swallow more erythrocytes infected by plasmodium under the condition of not using the existing anti-malarial drugs, so that the resistance of plasmodium to the anti-malarial drugs due to long-term use of the anti-malarial drugs is effectively avoided; and a new scheme is provided for clinical malaria treatment.

The invention provides a nano preparation acting on plasmodium in a targeting manner and a preparation method of the nano preparation. The preparation comprises a hydrophobic antimalarial drug dihydroartemisinin and a high-selectivity PI3K inhibitor delalisib, and the nano carrier comprises polyethylene glycol-polycaprolactone (mPEG2000-PCL1140), a high molecular polymer (polydopamine), and glucosamine. The preparation method comprises the following steps: co-entrapping dihydroartemisinin and delalisib in a cavity of a polyethylene glycol-polycaprolactone copolymer, forming polydopamine from a dopamine monomer through a self-polymerization reaction under an alkaline condition, and uniformly coating the surfaces of nanoparticles with the polydopamine; the glucosamine and catecholamine of the polydopamine are subjected to a Michael addition and / or Schiff base reaction and are covalently coupled with the nanoparticles to be adsorbed on the surface of a polydopamine shell layer, and finally the anti-malarial nano-drug is obtained. The pharmaceutical composition can greatly enhance the anti-malarial effect and realize reverse drug resistance. Meanwhile, glucosamine on the surfaces of the nanoparticles has targeting property and can be specifically combined with an erythrocyte membrane glucose transporter 1 and a plasmodium hexose transporter, so that a better treatment effect is achieved.

Provided are methods of treating malaria comprising administration of compounds of Formula (I), or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. Also provided are uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin X, plasmepsin IX or plasmepsin X and IX activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

This invention belongs to the field of drug synthesis and relates to a highly efficient hydrogen-borrowing reaction strategy for the preparation of ferroquinone (FQ). This strategy uses commercially available ferrocene as a starting material, constructs the key precursor ferrocene diol through two-step conversion, and then proceeds through two hydrogen-borrowing reactions, successfully inventing a highly efficient method for the preparation of FQ in four steps with an overall yield of 69%. Compared with previously reported routes, this method shortens the reaction steps, increases the reaction yield (the overall yield of the existing ferroquinone synthesis route in the background art is 39%), is simpler to operate, and is environmentally friendly (the only byproduct in the hydrogen-borrowing reaction is water). It can be widely used, laying a solid foundation for in-depth pharmacological and physiological activity research of FQ, and providing a novel and universal strategy for developing new scaffolds for candidate drug molecules with high activity and high selectivity of FQ derivatives.

The invention discloses a plasmodium falciparum proliferation inhibitor based on raw milk or pasteurized milk source exosomes (RM-EVs / CM-EVs), and the IC50 value of the plasmodium falciparum proliferation inhibitor is as low as 22.91 + / -2.7 mu g / mL and is obviously superior to that of ultrahigh-temperature sterilized milk and milk powder source EVs. The invention provides an extraction method of the EVs and application of the EVs in antimalarial drugs and functional foods, and provides a new natural and efficient choice for malaria prevention and treatment.

The invention shows that a P. falciparum-specific interaction between a PfEMP1 adhesin and the endothelial receptor CD36 modulates sporozoite infectivity. Using a synthetic peptide to leverage this interaction, a robust high-throughput screening method has been developed to identify next-generation prophylactics against this deadly malaria parasite. The synthetic peptide is also used as a prophylactic medicament to prevent P. falciparum infection in a subject.

This invention relates to a 6- O -L-arabinopyranosyl- β The preparation of β-D-glucopyranoside and its application in the preparation of antimalarial products belong to the field of traditional Chinese medicine and natural drug pharmaceuticals. Compound 6- of this invention... O -L-arabinopyranosyl- β This invention relates to an antimalarial drug with β-D-glucopyranoside as the active ingredient. It expands the application of aromatic disaccharide compounds 6- from *Hydrangea macrophylla*. O -L-arabinopyranosyl- β The medicinal value of D-glucopyranoside.

The invention discloses a long-chain non-coding RNA (lncRNA) lnc30 target spot of plasmodium falciparum in an erythrogenous stage and application of the long-chain non-coding RNA (lncRNA) lnc30 target spot, and relates to the technical field of biological medicines. The lnc30 nucleotide sequence is as shown in SEQ ID NO: 1, has the full length of 705nt, is positioned in a plasmodium falciparum cell nucleus, and is specifically and highly expressed in a schizosome stage. Researches find that lnc30 overexpression can significantly enhance the growth advantage of plasmodium falciparum and the ability of merozoite to invade erythrocytes, and participates in regulation of the erythroid stage development process of plasmodium, but after lnc30 is knocked down, plasmodium death may be caused. The key effect of the lnc30 in plasmodium falciparum development is disclosed for the first time, a new molecular tool is provided for antimalarial drug target screening, malaria diagnosis and pathogenesis research, and remarkable scientific value and application prospects are achieved.