摘要 |
<p>PURPOSE:To obtain a new compound highly soluble in water, having potent antibacterial activity on Gram-positive bacteria including esp. methicillin- resistant Staphyloococcus aureus, thus useful as an antibacterial agent. CONSTITUTION:The compound of formula I {Q is CH or N; R<1> is carboxylate or carboxyl; R<2> is H, a lower alkyl, a lower alkenyl, etc.; R is of formula II or III [R<3> is (CH2)m-Y ((m) is 1-5; Y is quaternary ammonium), etc.; (n) is 0-4; B<-> is an anion; f is such that when R<1> is carboxylate, it is 0 or 1, when R<1> is carboxyl, it is 2; C-ring is a five-membered heterocycle with <=N4]}, e.g. 7-[2-hydroxyimino-2-(2-aminothiazol-4-yl)acetamido]-3-[2-(1-(3,4me thylmorpholino) propyl)-4-pyridino) thiovinyl]-3-cephem-4-carboxylate chloride. The compound of formula I is obtained by reaction of a compound of formula IV (R<4> is a protective group) with a compound of formula V [R<5> is (protected) amino; R<6> is a protective group, etc.].</p> |