Haskell T H, Woo P W, Nicolaides E D, Hutt M P, Huang G G, Sanchez J P, DeJohn D, Heifetz C L, Krolls U, Lunney E, Mich T F
J Antibiot (Tokyo). 1981 Jul;34(7):862-8. doi: 10.7164/antibiotics.34.862.
The synthesis and biological activities of a series of 12 new semisynthetic penicillins is described. These compounds consisted of acylated amino acid analogs of 6-substituted-1,2-dihydro-2-oxonicotinic acid and 2-substituted-3,4-dihydro-4-oxo-5-pyrimidinecarboxylic acid attached to amoxicillin. The effect of the amino acid substituent, chirality of amino acid and acyl function on biological properties is discussed.
描述了一系列12种新的半合成青霉素的合成及生物活性。这些化合物由连接到阿莫西林上的6-取代-1,2-二氢-2-氧代烟酸和2-取代-3,4-二氢-4-氧代-5-嘧啶羧酸的酰化氨基酸类似物组成。讨论了氨基酸取代基、氨基酸的手性和酰基功能对生物学性质的影响。