Penicillanic acid derivs. of formula (I) (where R is phenyl, tolyl, chlorophenyl hydroxyphenyl or 2, 5-dihydroxyphenyl; A is alkylamino, dialkylamino, opt. substd. arylamino, aralkylamino, heterocyclylamino, heterocyclylalkylamino, heterocyclyl, or a gp. -NR1-COOR1, -NH-CHR1-COOR1, -NR1-COR1, -N-CO-Y-(CR1R1)m, -NR2-CX-N(R2)2, or -N=CR2-NR4R5 in which each R1 (same or different) is H or opt. substd. alkyl each R2 (same or different) is H. opt. substd. alkyl, alkoxy or phenyl, R3 is R2, -COR2 -SO2R2, -CONR4R5, -N(R1)2 or -OR1, R4 and R5 are H, opt. substd. alkyl or aryl, or R4 + R5 is -(CR1R1)n- or -CR1R1-CR1R1-Z-CR1R1-CR1R1- m is 3,4 or 5, n is 4,5 or 6; Zis O,S or SO2, X is O or S and Y is O or a direct C-C bond; and B is H, Na, K, Ca or di or tri- (lower alkyl) ammonium; the asterisk indicating that the cpd. may have R and/or S configuration at this chiral centre) e.g. D-alpha-(4-benzyl-allophanylamido)-benzylpenicillin sodium, and their hydrates are new cpds. (I) are broad spectrum antimicrobial agents active against Gram-positive and negative bacteria and bacteria-like organisms, and can be used for the prophylaxis and treatment of local and systemic infections.
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