摘要:
20,23-disubstituted mycaminosyltylonolide derivatives and use of the same in the field of the prophylaxis and treatment of pasteurellosis are disclosed. The di-substituents are peperidino optionally substituted with one or two methyl groups. The derivatives have selective antibacterial activity against Pasteurella.
摘要:
Provided is a pharmaceutical composition for the prevention or treatment of a diarrhea, which comprises as an active ingredient, siastatin B or a siastatin B derivative having a β-glucuronidase inhibitory activity. Siastatin B or the siastatin B derivative is useful as a drug for the prevention or treatment of a diarrhea, which is capable of ameliorating the diarrhea disorders as induced as a side effect when a cancer-bearing patient received the administration of an anticancer chemotherapeutic agent, particularly an anticancer camptothecin derivative acting as a topoisomerase I inhibitor. This composition is effective to prevent or treat such diarrhea as induced by the administration of an anticancer camptothecin derivative to the cancer-bearing patient.
摘要:
A compound of the formula (I): and a compound of the formula (V): as well as a compound of the formula (X): which are each a novel siastatin B derivative having a potent inhibitory activity against a glycosidase, are now synthesized by new processes. The compound of the formula (I), the compound of the formula (V) and the compound of the formula (X) have a potent enzyme-inhibitory activity to a glycosidase, which is particularly N -acetyl-galactosaminidase, galactosidase, glucosidase and mannosidase.
摘要:
A process for producing D-chiro-inositol which comprises either mixing an aqueous solution of kasugamycin or a salt thereof with a strongly acidic ion-exchange resin (of H type) in a reactor or bringing the aqueous solution into contact with the resin in a column packed therewith, heating the aqueous solution and the resin under normal or applied pressure to effect hydrolysis of kasugamycin to thereby prepare an acidic reaction solution containing D-chiro-inositol, separating the acidic reaction solution from the resin, and recovering D-chiro-inositol from the solution. In this stage, it is possible to obtain efficiently high-purity D-chiro-inositol by passing the acidic reaction solution first through a column packed with a strongly acidic ion-exchange resin (of H type) and then through another column packed with a strongly basic ion-exchange resin (of OH type) to prepare a neutral eluate containing D-chiro-inositol, and concentrating the eluate to effect deposition of D-chiro-inositol crystals.
摘要:
A compound represented by general formula (1) which is useful for producing 3,4'-dideoxymycaminosyltylonolide useful as an antibacterial substance. In the said formula, A represents optionally protected carbonyl; B represents optionally protected formyl; R¹ represents optionally protected hydroxy; R² represents hydrogen or acyl; W represents hydrogen, hydroxy, lower alkanoyloxy or substituted sulfonyloxy; Y represents hydrogen, halogen, hydroxy or substituted sulfonyloxy; and symbol --- represents either a double or a single bond.
摘要翻译:由通式(1)表示的化合物,其可用于制备可用作抗菌物质的3,4'-二脱氧碳霉糖基太乐内酯。 在所述式中,A表示任选被保护的羰基; B代表任选保护的甲酰基; R 1代表任选保护的羟基; R 2代表氢或酰基; W代表氢,羟基,低级烷酰氧基或取代的磺酰氧基; Y代表氢,卤素,羟基或取代的磺酰氧基; 符号---代表双键或单键。
摘要:
The invention provides 5-deoxy-5,5-difluoro derivatives of aminoglycoside antibiotics of neamine, kanamycin A, kanamycin B, gentamicin and seldomycin, each synthesized as a novel compound, and also 1-N-(a-hydroxy- m-aminoalkanoyl) derivatives synthesized from the newly obtained 5-deoxy-5,5-difluorokanamycins A and B and analogs thereof. The 5-deoxy-5,5-difluoro derivatives thus obtained have antibacterial activities superior or substantially equivalent to those of the amino-glycoside antibiotics from which they are derived and further have a remarkably improved median lethal dose (LD so ) when intravenously administered to mice and a remarkably reduced toxicity on mammals.
摘要:
A compound represented by formula (I); a process for producing a compound (substance F-1490) of formula (I), wherein X represents -O- and R represents a hydroxyl group, by using a microorganism belonging to the genus Cunninghamella; and a Cunninghamella sp. F-1490 strain (FERM BP-8287) capable of producing the substance F-1490; and an osteoclast differentiation inhibitory agent containing as an active ingredient the compound represented by formula (I): wherein X represents -O- or -CH 2 -, and R represents a hydroxyl group when X represents -O-, or a hydrogen atom when X represents -CH 2 -.
摘要:
Compounds represented by formula (I) below; a process for producing the compounds by culturing a microorganism belonging to the genus Aspergillus and isolating the above-mentioned compounds from the culture; an angiogenesis inhibitory agent containing as an active ingredient the compounds; and an Aspergillus sp. F-1491 (FERM BP-8288) strain capable of producing the compounds. In formula (I), R represents a methyl group or an ethyl group, R 1 represents a hydrogen atom, a chlorine atom, a hydroxyl group or a methoxy group, R 2 represents a hydroxyl group, or R 1 and R 2 taken together form an epoxy ring structure.
摘要:
Sulphostin analogues characterized by being represented by general formula (IV'); or medicinally acceptable salts thereof wherein n is an integer of 0 to 3, with the proviso that the case wherein n is 2 and C* takes S-configuration and P* R-configuration is excepted.
摘要:
Salicylamide derivatives represented by formulae (1a) and (1b); intermediates in the production thereof; a process for producing the same; and drugs containing the same as the active ingredient. The salicylamide derivatives represented by formulae (1a) and (1b) are useful as anti-inflammatory agents and immunosuppressive agents which exert an effect of inhibiting the activation of NF-κB with little side effects.