Certain phosphinic acid derivatives having antibacterial activity
申请人:Merck & Co., Inc.
公开号:US05099063A1
公开(公告)日:1992-03-24
New 3-(1-aminoalkylphosphinyl)-(2-substituted)propionic acids are described which display antibacterial activity and potentiate carbapenem antibiotics.
Antibacterial agents and potentiators of carbapenem antibiotics
申请人:Merck & Co., Inc.
公开号:US05143908A1
公开(公告)日:1992-09-01
New 3-(1-aminoalkylphosphinyl)-(2-substituted)propionic acids are described which display antibacterial activity and potentiate carbapenem antibiotics.
Peptides of the formula A-B-D-E-G are disclosed wherein
A is, e.g., benzyloxycarbonyl, t-butoxycarbonyl, 1-naphthyloxyacetyl or 1-naphthylacetyl;
B is, e.g., phenylalanine, 3-(1-naphthyl)alanine, tryptophan or homophenylalanine;
D is, e.g., histidine, lysine or phenylalanine;
E is, e.g., one of the following formulae:
or
and G is, e.g., -OH, -OEt, -NH2.
Those compounds inhibit enzymes and can be used as pharmaceutical agents.
公开了式 A-B-D-E-G 的多肽,其中
A 是苄氧羰基、叔丁氧羰基、1-萘氧乙酰基或 1-萘乙酰基;
B 是,例如,苯丙氨酸、3-(1-萘基)丙氨酸、色氨酸或均苯丙氨酸;
D 是组氨酸、赖氨酸或苯丙氨酸;
例如,E 是下式中的一种:
或
G为-OH、-OEt、-NH2 等。
这些化合物对酶有抑制作用,可用作药剂。