160 results about "Anti hiv activity" patented technology

Betulin and dihydrobetulin acyl derivatives according to the present invention have been found to have potent anti-HIV activity. The compounds of the present invention have Formula I as described herein, or pharmaceutically acceptable salts thereof; wherein R1 is a C2-C20 substituted or unsubstituted carboxyacyl or ester thereof; R2 is hydrogen, halogen, hydroxyl or —OR3, R3 is C2-C20 substituted or unsubstituted carboxyacyl; and R4 is hydrogen or C(C6H5)3; wherein the dashed line represents an optional double bond between C20 and C29.

Pharmacophore models to be used in drug design and discovery are provided. An in silico protocol and in vitro assays are presented. Compounds and their pharmaceutically acceptable salts with HIV-1 integrase inhibitory and anti-HIV activity and use thereof in the treatment of HIV / AIDS and related infections either alone or in combination with all the known antiretroviral therapeutics are described.

Polypeptides of A1-Arg-A2-Cys-Tyr-A3-A4-X-A5-A6-Cit Cys-A7 (I) or their salts (wherein A1 is hydrogen or a residue of arginine, lysine, ornithine, citrulline, alanine, or the like; A2 is an aromatic amino acid residue; A3, A4 and A6 are each a residue of arginine, lysine, ornithine, citrulline, or alanine; A5 is a residue of tyrosine, phenylalanine, alanine, naphthylalanine, or citrulline; A7 is a lysine or arginine residue whose carboxyl group may be converted into amido; and X is a residue of D-ornithyl-proline, prolyl-D-ornithine, D-lysylproline, or the like, with the proviso that any one of A1, A3, A4, A5, A6 and A7 is a residue of alanine or the like or that X is citrulline or the like).

The present invention features antibodies and antibody fragments that specifically bind a CD4-inducible HIV gp120 epitope that is enhanced by binding a co-receptor for HIV, such as CCR5 or CXCR4, and pharmaceutical compositions comprising the antibodies or antibody fragments. The invention also features nucleic acids encoding the antibodies or antibody fragments, pharmaceutical compositions comprising the nucleic acids encoding the antibodies or antibody fragments, vectors comprising the nucleic acids, and cells comprising the vectors. The invention further features methods of identifying antibodies or antibody fragments with broadly neutralizing activity against HIV. The invention also features methods of inhibiting HIV entry into cells and methods of inhibiting replication of HIV in mammals, using the antibodies and nucleic acids of the invention.

The present invention relates to inhibition of viruses, e.g., HIV using oxindoles and compounds related to oxindoles. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhibit HIV in a cell; as well as to methods of prophylaxis, and therapy related to HIV infection and related disease states such as AIDS.

The present invention relates to a polypeptide represented by the formula: A1-Arg-A2-Cys-Tyr-A3-A4-X-A5-A6-Cit-Cys-A7  (I) (wherein A1 represents a hydrogen atom or an arginine, lysine, ornithine, citrulline, alanine residue, etc.; A2 represents an aromatic amino acid residue; A3, A4 and A6 represent an arginine, lysine, ornithine, citrulline or alanine residue, A5 represents a tyrosine, phenylalanine, alanine, naphthylalanine or citrulline residue; A7 represents a lysine or arginine residue in which a carboxyl group may be amidated; X represents a D-ornithyl-proline, prolyl-D-ornithine, D-lysyl-proline residue, etc.; provided that either of A1, A3, A4, A5, A6 and A7 is an alanine residue, etc., or X is citrulline, etc.) or a salt thereof.

The present invention is to provide a multiple-agents-binding compound comprising a compound having anti-HIV activity and having no affinity for cell surface protein bound together with a same or different kind of at least one compound having anti-HIV activity and having no affinity for cell surface protein, or a salt thereof, and a pharmaceutical composition for the prevention or treatment of infectious diseases of HIV or AIDS comprising said multiple-agents-binding compound.

RANTES-derived peptides and the use thereof in the treatment of diseases in which RANTES receptor is involved, such as viral infections, particularly HIV infections, and inflammatory, allergic, degenerative, neoplastic or metastatic diseases.

The present invention provides methods and formulations for optimizing the anti-cancer and anti-HIV activities of a camptothecin drug, including camptothecin and its related analogs including 9-aminocamptothecin and 9-nitrocamptothecin. The invention involves methodologies and formulations that limit human serum albumin-mediated reduction of the anti-cancer and anti-HIV effects of the camptothecins, and the methods and formulations provide combination therapies in which binding of the camptothecin agent to human serum albumin can be modulated by the administration of a competing agent such as ibuprofen, clofibrate or clofibric acid that also binds human serum albumin. Reduced camptothecin drug binding to human serum albumin can result in elevated camptothecin free drug levels and thus improve the effectiveness of treatment regimens involving these drugs. Further agents such as methotrexate and AZT can also be used in cancer and HIV-positive patients employing camptothecin drugs.

The present invention relates to one kind of phenolic acid compound and its preparation process and use in treating AIDS. Red sage material is treated through solvent extraction, macroporous adsorbing resin purification, conventional drying and other steps to obtain total phenolic acid. The total phenolic acid is dissolved in water via heating, chromatographic column separation and repeated purification to obtain new compound salvianolic acid N. Enzyme and cell activity experiments show that the new compound has HIV resisting activity and is hopeful in being developed into one new kind of AIDS treating medicine.

The invention belongs to the field of traditional Chinese medicine production, and relates to 1-alkylated daphnane diterpene and application thereof to preparation of anti-HIV drugs. 1-alkylated daphnane diterpene is a compound extracted from S. chamaejasme of the Stellera genus; tests prove that 1-alkylated daphnane diterpene is remarkable in anti-HIV activity, and the EC50 value is lower than 0.001 [mu]M; 1-alkylated daphnane diterpene is relatively low in cytotoxicity, and the CC50 value is higher than 11 [mu]M; compared with a positive control drug zidovudine, 1-alkylated daphnane diterpene has more obvious advantages; the 1-alkylated daphnane diterpene compound can serve as an active ingredient for preparation of the anti-HIV drugs.

The invention discloses a di(7-hydroxy-2,3-dihydro-1H-inden-1-yl) ether and analogue, synthesizing method and application in the pharmacy, which is characterized by the following: the structure of the ether possesses formula I and formula II, which improves anti-HCV activity and better anti-HIV activity; the product can be used to study and develop new drug with obvious scientific meaning and using prospect.

The invention relates to a series of novel compounds and a preparation method thereof, particularly to a series of benzoxazolone derivatives and a preparation method thereof, and solves the problem that the prior benzoxazolone compounds have no 4-substituted derivatives and have anti-HBV activity and anti-HIV activity. The general structural formula of the derivatives is shown in the figure, wherein R is C3-C6 fatty acid ester group, benzoate group / substituted benzoate group, benzene sulfonate group / substituted benzene sulfonate group, amino acid ester group, or heterocyclic acid ester group / substituted heterocyclic acid ester group. The invention obtains a series of 4-substituted benzoxazolone derivatives with proven anti-HBV activity and anti-HIV activity, opens new preparation paths of the above three drugs, and brings new breakthrough in pharmaceutical and pesticide fields. In addition, the synthetic method has the advantages of easy operation, mild reaction conditions, single reaction product, and applicability to large scale production.

The present invention relates to the use of Indian Green Mussel (Perna viridis) as a source of anti-HIV activity. More particularly, the present invention relates to the use of an extract of Indian Green Mussel (Perna viridis) as a source of anti-HIV activity in vitro.

The invention relates to a building method of a 3-dimensional quantitative structure-activity relationship (3D-QSAR) model, in particular to building of the 3D-QSAR model based on HIV-1 inhibitor molecules and consistency model building, and belongs to the technical field of biological information. The HIV-1 inhibitor molecules are selected to perform 3D-QSAR and consistency model research so as to mine the relationship between the structure of an inhibitor and the anti-HIV activity of the inhibitor. According to the method, the bioactivities of compounds with similar structures are predicted through building of a mathematical model based on the chemical characteristics (such as hydrophilcity, hydrophobicity, electrostatic property, polarity and three-dimensional structure) of the inhibitor. A consistency model is built with a statistics method on the basis of three 3D-QSAR models, and the aim is to further enhance the prediction capability of the model. The obtained model can better predict the anti-HIV activities of compounds, and the prediction accuracy of the anti-HIV activity of a brand new compound is increased. Compared with other methods, the method has the advantages that the medicament discovery efficiency is increased, and the medicament discovery cost is reduced.

The invention relates to 2-(4-substituted phenylamino group) polysubstitution paradoximes as HIV reverse transcriptase inhibitors, and a preparation method and purpose thereof, in particular to I type compounds or medicinal salt thereof, wherein the definitions of the R1, R2, R3, R4, R5, R6, R7 and X are stated as the specification. The I type compounds of the invention are anti-HIV activity compounds having a novel framework structure.

The metabolic fingerprint and anti-inflammatory activity and anti-HIV activity of H. gentianoides is disclosed. High performance liquid chromatography (HPLC) analysis shows that H. gentianoides contains a family of compounds, including some not previously observed in other Hypericum species. H. gentianoides extracts and fractions from these extracts reduce prostaglandin E2 synthesis in mammalian macrophages and inhibit HIV in infected HeLa cells. The present invention provides extracts and fractions thereof from H. gentianoides for use in pharmaceutical compositions and methods for the treatment or inhibition of inflammation, prostaglandin E-mediated disease, disorder or condition, a cyclooxygenase-mediated disease, disorder or condition, or an HIV infection.

Betulin and dihydrobetulin acyl derivatives according to the present invention have been found to have potent anti-HIV activity. The compounds of the present invention have Formula I as described herein, or pharmaceutically acceptable salts thereof; wherein R1 is a C2-C20 substituted or unsubstituted carboxyacyl or ester thereof; R2 is hydrogen, halogen, hydroxyl or —OR3, R3 is C2-C20 substituted or unsubstituted carboxyacyl; and R4 is hydrogen or C(C6H5)3; wherein the dashed line represents an optional double bond between C20 and C29.

The invention discloses a method for preparing and applying tea extract with anti-HIV activity. The preparation method comprises the following steps: firstly, crushing tea to obtain coarse tea powder; secondly, using water or a water-soluble organic solvent to leach out the coarse tea powder to obtain an extracting solution; thirdly, filtrating the extracting solution, and using an organic solvent to extract and separate filtrate; and fourthly, performing vacuum concentration on extractive matters to obtain a clear paste, and performing vacuum freeze drying to obtain the tea extract. The application method comprises the following steps: adding a medicine carrier into the extract with the anti-HIV activity, performing mixing, granulation and drying, and preparing the obtained product into granules, capsules, tablets, oral liquid or injection according to a general medicament preparation method; or adding a carrier into the extract, and preparing the mixture into health-care drinks or health-care foods by a general method. Experiments prove that the suppression ratio of the tea extract with the anti-HIV activity to the activity of HIV-LTR sequences activity can reach more than 80 percent, so that the tea extract can be used for preparing anti-HIV medicaments. The extraction method provided by the invention is simple and easy, and is quite suitable for popularization and application.

The invention discloses a thiazole (piperazine) azululanone azasugar derivative, and provides a synthesis method of the derivative and application of the derivative to preparation of an anti-HIV (Human Immunodeficiency Virus) medicinal preparation. A compound has high anti-HIV activity, and more administration options can be provided for clinical treatment of AIDS.

The invention discloses a synthetic method of sulfo bagasse xylan phthalate. The synthetic method comprises the following steps: by taking bagasse xylan as a starting material, taking phthalic anhydride as a carboxylic acid esterification agent and taking triethylamine as a catalyst, synthesizing bagasse xylan phthalate in a dimethylformamide solvent; and then further synthesizing a sulfo bagasse xylan phthalate double esterification derivative in an alkaline water solvent by taking sodium trisulfamate as a second esterification agent. The bagasse xylan double esterification derivative namely sulfo bagasse xylan phthalate prepared by using the synthetic method disclosed by the invention integrates the properties of bagasse xylan carboxylic ester and bagasse xylan sulfate, and is easy to control synthesis process conditions; products have relatively high biological activity and good water solubility and surface activity; and modified double-active bagasse xylan has certain effects on the aspects of anti-HIV activity, anti-coagulation activity and platelet aggregation inhibition, and has relatively high application values in the fields of fine chemicals, foods and medicines.

The invention discloses an aspergillus sp. for producing an anti-HIV active substance and application of the aspergillus sp.. The strain number of the aspergillus sp. is CPCC400735, and the registration number of the aspergillus sp. in Center of General Microbiology of China Committee for Culture Collection of Microorganisms is CGMCC No.12376. The inhibition ratio of methyl alcohol extractive of fermentation culture of the aspergillus sp. CPCC400735 to HIV-1 is 99.9% when the concentration is 4 mg / mL. The inhibition ratio of a compound in a formula 1, the inhibition ratio of a compound in a formula 2, the inhibition ratio of a compound in a formula 3 and the inhibition ratio of a compound in a formula 4 to HIV-1 are 96% or above when the concentration is 100 micromol / L, and the IC50 value is 2.4-32.6 micromol / L. The methyl alcohol extractive of the fermentation culture of the aspergillus sp. CPCC400735, the compound in the formula 1, the compound in the formula 2, the compound in the formula 3 and the compound in the formula 4 have high inhibitory activity to HIV-1 and have less toxicity.

Aryl phosphate derivatives of d4T with para-bromo substitution on the aryl group show markedly increased potency as anti-HIV agents without undesirable levels of cytotoxic activity. In particular, these derivatives are potent inhibitors of HIV reverse transcriptase. In a preferred aspect of the present invention, the phosphorus of the aryl phosphate group is further substituted with an amino acid residue that may be esterified or substituted, such as a methoxy alaninyl group.

The invention belongs to the field of drug synthesis, particularly discloses an artemisinin derivative as well as a preparation method and an application, and more particularly discloses an artemisinin derivative as well as a preparation method and an application thereof in anti-tumor drugs and anti-HIV drugs. The artemisinin derivative disclosed by the invention has a structure as shown in a formula I, wherein R is a residual radical of other compounds. The preparation method of the artemisinin derivative as shown in the formula I is simple and feasible, good in repeatability and small in environmental pollution, and can be used for massively preparing the compound as shown in the formula I. The compound as shown in the formula I has obvious anti-tumor activity and anti-HIV activity.

The present invention relates to fatty acid and fatty alcohol substituted nucleoside derivatives and nucleoside and nucleoside derivatives substituted on multivalent scaffolds (e.g., polymers, peptides, polycarboxylic acid substituted compounds, compounds containing polycycloSaligenyl groups) that display potent anti-HIV activity. Furthermore, they show enhanced activity against multi-drug resistant, R5, and cell-associated virus. Some of them also display activity against other sexually transmitted pathogens and sperm. The present invention provides their methods of synthesis, composition of matter, and methods of use. Emphasis is placed on their application as topical microbicides to treat or prevent sexual transmission of disease, especially HIV / AIDS.

The invention belongs to the field of biological medicines, in particular to a blue-green algal virus protein N mutant, a PEG modified derivative and application thereof. The blue-green algal virus protein N mutant comprises two sequences, one is connecting peptide with hydrophilic flexibility, and the other is a blue-green algal virus protein N sequence optimized by trinucleotide. The derivativeis obtained by PEG modification of the blue-green algal virus protein N mutant; the mutant and the derivative thereof show favorable anti-HIV activity. The invention is applied to preparing anti-HIV or other virus microorganisms.

The invention discloses a 1-(3-aminopropyl) piperazine-4-aminoamide compound as well as a preparation method and application thereof. The structural general formula of the compound is shown as a formula I, wherein R1 is the following groups unsubstituted or substituted by 1-3 substituents: phenyl groups, benzyl groups, naphthyl groups, C5-C10 aromatic heterocyclic groups or C4-C7 saturated heterocyclic groups; the heterocyclic groups comprises 1-3 (at least 1) heteroatoms selected from N, O and S; the substituents are selected from the following atoms or groups: halogen, sulfydryl groups, hydroxyl groups, CF3, CN, NO2 and SO2CH3; and X is methylene, carbonyl or does exist. Through cell activity screening of an HIV-1 infected Bal(R5) lymphoid tissue sample, the series of compound is found to have very strong anti-HIV (Human Immunodeficiency Virus) activity, wherein the compound with strongest activity has the IC50 value reaching 10nM and the selection index more than 14.545 and can be developed into anti-AIDs medicaments. The formula I is shown in the specification.

The invention relates to an azepine brazilin compound and a synthesis method thereof. By using the structure of a natural product brazilin as a simulation object, a series of brazilin structure compounds containing nitrogen atoms are designed; and substituted cinnamic acid is used as a raw material, and a series of azepine brazilin compounds is obtained through serial chemical conversion and synthesis. Partial azepine brazilin compounds have strong anti-cancer activity, partial compounds have anti-HIV (Human Immunodeficiency Virus) activity, and partial compounds have aldose reductase suppressive activity and obviously reduce the blood sugar level. Medical compositions prepared from the compounds and at least one pharmaceutically acceptable excipient or carrier can be used for treating cancer and resist virus infections.

Pharmacophore models to be used in drug design and discovery are provided. An in silico protocol and in vitro assays are presented. Compounds and their pharmaceutically acceptable salts with HIV-1 integrase inhibitory and anti-HIV activity and use thereof in the treatment of HIV / AIDS and related infections either alone or in combination with all the known antiretroviral therapeutics are described.

The invention discloses an indole compound extracted from radix isatidis shown in a general formula (I) and a derivative of the indole compound, as well as a salt acceptable on pharmacy, a preparation method of the compound, and a medicinal composite. The compound has apparent HIV-resisting activity and influenza virus-resisting activity, and can be used for preparing drugs or healthcare products for resisting HIV or influenza viruses. (The formula is shown in the description.).