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New ureido-substituted dihydropyrimidinone derivatives, useful as broad-spectrum antibacterial agents with strong activity against Gram positive bacteria

机译:新的脲基取代的二氢嘧啶酮衍生物,可用作广谱抗菌剂,对革兰氏阳性细菌具有强活性

摘要

5-(Diaminoalkanoylamino)-3,4,5,6-tetrahydro-2-(aryl-, aroyl-, alkyl- or alkoxycarbonyl-ureido)-pyrimidin-4-one derivatives (I) are new. Dihydropyrimidinones of formula (I) and their salts, solvates, hydrates and hydrated salts are new. R1 = H or T; A = -NR4R5, -NR5-C(Q)-NR6R7 or -N(R5)-C(R8)=NR9; R4 - R7, R9 = H, T, COT, benzyl or pyridylmethyl; R8 = H or T; Q = O, S or NR9; D = 2-6C alkanediyl (optionally substituted by 1 or 2 of OH, OT, OCOT or =O); E = direct bond or CH2; R2 = H or T; R3 = 6-10C aryl or (6-10C) aroyl (both optionally ring-substituted by 1 or 2 of halo, CF3 or T); 1-10C alkyl (optionally having one or more C replaced by O and optionally substituted by 1-3 of 6-10C aryl, COOT or COOH); or COOT; T = 1-6C alkyl. An Independent claim is included for the preparation of (I).
机译:5-(二氨基链烷酰基氨基)-3,4,5,6-四氢-2-(芳基,芳酰基,烷基或烷氧基羰基-脲基)-嘧啶-4-酮衍生物(I)是新的。式(I)的二氢嘧啶酮及其盐,溶剂化物,水合物和水合盐是新的。 R1 = H或T; A = -NR4R5,-NR5-C(Q)-NR6R7或-N(R5)-C(R8)= NR9; R4-R7,R9 = H,T,COT,苄基或吡啶基甲基; R8 = H或T; Q = O,S或NR9; D = 2-6C链烷二基(任选地被OH,OT,OCOT或= O的1或2个取代); E =直接键或CH2; R2 = H或T; R3 = 6-10C芳基或(6-10C)芳酰基(均任选被1或2个卤素,CF3或T环取代); 1-10C烷基(任选具有一个或多个C被O取代并且任选被6-10C芳基,COOT或COOH中的1-3取代);或COOT; T = 1-6C烷基。准备(I)包括独立权利要求。

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