摘要:
The present invention provides a cyclic lipopeptide acylase which may effectively deacylate the acyl side chain of a cyclic lipopeptide compound, specifically FR901379 Substance or its analog thereof shown by the following general formula [I], and a process for production of a cyclic peptide compound which comprises the use of said acylase. [wherein R 1 is acyl;
R 2 is hydroxy or acyloxy; R 3 is hydrogen or hydroxy; R 4 is hydrogen or hydroxy; R 5 is hydrogen or hydroxysulfonyloxy; and R 6 is hydrogen or carbamoyl]
摘要翻译:本发明提供了一种环状脂肽酰基转移酶,其可以有效地脱酰化环状脂肽化合物的酰基侧链,特别是FR901379由以下通式ⅪI所示的物质或其类似物,以及一种环肽化合物的制备方法, 使用所述酰基转移酶。 其中R 1是酰基; R 2是羟基或酰氧基; R 3是氢或羟基; R 4是氢或羟基; R 5是氢或羟基磺酰氧基; R 6是氢或氨基甲酰基
摘要:
There is provided a cyclic lipopeptide acylase which is capable of deacylating the acyl side chain of a cyclic lipopeptide compound, e.g. Substance FR901379 or its analog, of the following general formula [I] with effectiveness as well a method of producing a cyclic peptide compound which comprises using the acylase.
[wherein R 1 is acyl; R 2 is hydroxy or acyloxy; R 3 is hydrogen or hydroxy; R 4 is hydrogen or hydroxy; R 5 is hydrogen or hydroxysulfonyloxy; and R 6 is hydrogen or carbamoyl.]
摘要翻译:提供了环状脂肽酰基转移酶,其能够使环状脂肽化合物的酰基侧链脱酰化,例如, 具有以下通式的物质FR901379或其类似物,其有效性以及包含使用酰基转移酶的环肽化合物的制备方法。 其中R 1是酰基; R 2是羟基或酰氧基; R 3是氢或羟基; R 4是氢或羟基; R 5是氢或羟基磺酰氧基; 和R 6是氢或氨基甲酰基
摘要:
The invention relates to new polypeptide compounds represented by formula (I), wherein R1 is hydrogen, etc., R2 is hydrogen, etc., R3 is hydrogen, etc., and R4 is hydrogen, etc., or a salt thereof which have antimicrobial activities (especially antifungal activities), inhibitory activity on β-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for the prophylactic and/or therapeutic treatment of infectious diseases including Pneumocystis carinii infection (e.g. Pneumocystis carinii pneumonia in a human being or an animal.
摘要:
New peptide compounds of formula (I), wherein R1 is alkyl or aralkyl, R2 is amino(lower)alkyl or protected amino(lower)alkyl, R3 is hydroxy, protected hydroxy, amino or protected amino, R4 is hydroxy, or R?3 and R4¿ are linked together to form -Z- (in which -Z- is -O- or -NH-), and R5 is hydrogen or an amino protective group, R6 is hydroxy, or R?5 and R6¿ are linked together to form bond, with proviso that when R3 is hydroxy, protected hydroxy, amino or protected amino and R4 is hydroxy, then R?5 and R6¿ are linked together to form bond, and a pharmaceutically acceptable salt thereof, which is useful as a medicament.
摘要:
A process for preparing compounds represented by general formula (I), wherein R 1 represent hydrogen, a lower alkanoyl group or a lower alkyl group; and R 2 and R 3 represent each hydrogen or a lower alkanoyl group, characterized by reacting a culture of a strain belonging to the genus Fusarium or cells obtained by the filtration of the culture with a compound represented by general formula (II) wherein R 1 , R 2 , and R 3 are each as defined above.
摘要翻译:一种制备由通式(I)表示的化合物的方法,其中R 1表示氢,低级烷酰基或低级烷基; R 2和R 3代表每个氢或低级烷酰基,其特征在于使属于镰刀菌属的菌株的培养物或通过过滤培养物得到的细胞与通式(II)表示的化合物反应 )其中R 1,R 2和R 3各自如上所定义。
摘要:
This invention relates to new polypeptide compounds represented by formula (I), wherein R1 is as defined in the description or a salt thereof, which have antimicrobial activities (especially, antifungal activities), inhibitory activity on β-1,3-glucan synthase, to a process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for the prophylactic and/or therapeutic treatment of infectious diseases including Pneumocystis carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal.
摘要:
New peptide compounds of formula (I) wherein W is a group of formula (a) [in which R1 is hydrogen, halogen, lower alkyl, etc., Q is CH or N, L is a bivalent radical (b) (in which Y is CH or N, Z is NH, O or S, and --- is a single bond or a double bond), etc.,], etc., A1 is lower alkylene, -NHCO-, (c) (in which V is O or S), or -SO¿2?-, T is hydrogen, aryl which may have suitable substituent(s), heterocyclic group, hydroxy, etc., A?2¿ is lower alkylene, R8 is hydrogen or lower alkyl, etc., R3 is hydrogen, aryl which may have suitable substituent(s), hydroxy, protected hydroxy, etc., A3 is bond or lower alkylene, R9 is hydrogen or lower alkyl, etc., and R4 is carboxy, protected carboxy, heterocycliccarbonyl which may have suitable substituent(s), or a group of formula (d) (in which R5 is hydrogen or lower alkyl, and R6 is hydrogen, aryl, ar(lower)alkyl which may have suitable substituent(s), etc.), etc., and a pharmaceutically acceptable salt thereof which are useful as a medicament.