巴喹普林 | 102280-35-3

• 物质功能分类: 分析化学 - 标准品 - 分析标准品
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 中文名称: 巴喹普林
• 中文别名: 5-{[8-(二甲基氨基)-7-甲基-5-喹啉基]甲基}-2,4-嘧啶二胺
• 英文名称: Baquiloprim
• 英文别名: 5-[[8-(dimethylamino)-7-methylquinolin-5-yl]methyl]pyrimidine-2,4-diamine
• CAS: 102280-35-3
• 化学式: C₁₇H₂₀N₆
• mdl: MFCD00864859
• 分子量: 308.4
• InChiKey: AIOWJIMWVFWROP-UHFFFAOYSA-N

物化性质

• 熔点：
  >215 °C (dec.)
• 沸点：
  567.9±60.0 °C(Predicted)
• 密度：
  1.277±0.06 g/cm3(Predicted)
• 溶解度：
  可溶于DMSO（少许）、甲醇（少许）

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  23
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.235
• 拓扑面积：
  94
• 氢给体数：
  2
• 氢受体数：
  6

安全信息

• 危险品标志：
  Xn
• 安全说明：
  S26
• 危险类别码：
  R22,R36/37/38
• WGK Germany：
  3

制备方法与用途

概述

巴喹普林（Baquiloprim）具有与甲氧苄胺嘧啶相似的广谱抗菌活性，但其消除半衰期大大延长，能够克服甲氧苄胺嘧啶在协同性方面的不足。

用途

巴喹普林可用于治疗牛的肺炎及肠炎、腐蹄病、脐部感染、感染性外伤、感染性角膜结膜炎、非泌乳期牛的木舌病和放线菌下颌肿块；猪胃及肠道感染、胸膜肺炎、乳腺炎-子宫炎-无乳综合征等；狗的泌尿系统、呼吸系统、胃肠道及皮肤感染。

生物活性

巴喹普林是一种抗生素，是细菌二氢叶酸还原酶的选择性抑制剂。它对革兰氏阴性和革兰氏阳性细菌均具有体外抑菌活性。

文献信息

• Substituted pyrimidines, their synthesis and compositions containing them, their use in medicine and intermediates for making them
  申请人：THE WELLCOME FOUNDATION LIMITED

  公开号：EP0051879A2

  公开（公告）日：1982-05-19

  Compounds of the formula (1): or a salt, N-oxide or acyl derivative thereof, wherein is a six membered ring optionally containing a hetero atom double bonds, both the phenyl ring and the being optionally substituted except that when does not contain a hetero atom either or both the phenyl ring or must be substituted other than solely by a hydroxy group at the 4-position of the phenyl ring, and that there are no substituents attached to the atom of adjacent to the 6-position of the phenyl ring are useful in the treatment of bacterial infections. A process for preparing these compounds and novel chemical intermediates used in their preparation are disclosed as is the first medical use of the compounds of the formula (I) and pharmaceutical compositions containing them.

  式(1)化合物： 或其盐、N-氧化物或酰基衍生物，其中苯基环和苯基环均可被任选取代，但当不含有杂原子时，苯基环或苯基环均必须被取代，而不是仅被苯基环 4 位上的羟基取代，且与苯基环 6 位相邻的原子上不连接任何取代基。 本发明公开了制备这些化合物的工艺和用于制备这些化合物的新型化学中间体，以及式（I）化合物和含有这些化合物的药物组合物的首次医学用途。
• Bactericidal mixtures
  申请人：PITMAN-MOORE INC.

  公开号：EP0238207A1

  公开（公告）日：1987-09-23

  Compositions comprising the compounds 2,4-diamino-5-(8-dimethylamino-7-methyl-5-quinolylmethyl) pyrimidine and sulphadimidine, or salts thereof. The compositions are particularly useful for the treatment of bacterial infections in animals.

  由 2,4-二氨基-5-(8-二甲氨基-7-甲基-5-喹啉基甲基)嘧啶和磺胺二甲嘧啶或其盐组成的复合物。 这种复合物特别适用于治疗动物的细菌感染。
• Pharmaceutical compositions having differential drug release rate
  申请人：PITMAN-MOORE LIMITED

  公开号：EP0416722A2

  公开（公告）日：1991-03-13

  A solid pharmaceutical composition for release of a biologically active substance into a desired aqueous environment, containing a core and an outer layer, said core comprising between 17 and 93% by weight of the biologically active substance, between 0.01 and 7% by weight of a water swellable polymer material and between 0 and 83% of one or more accessory ingredients, relative to the total weight of the core; and the outer layer comprising between 25 and 75% by weight of the biologically active substance, between 25 and 75% by weight of a material for enabling rapid dispersion of the outer layer into the aqueous environment and 0 to 50% by weight of one or more accessory ingredients, relative to the total weight of the outer layer. The composition is preferably formulated as a bolus for veterinary use.

  一种用于将生物活性物质释放到所需水环境中的固体药物组合物，包含一个内核和一个外层，相对于内核总重量，所述内核由 17% 至 93% 的生物活性物质、0.相对于内核的总重量，外层包括 25% 至 75% 的生物活性物质、25% 至 75% 的可使外层快速分散到水环境中的材料以及 0% 至 50% 的一种或多种辅助成分。组合物最好配制成兽用栓剂。
• Baquiloprim for treating protozoal infections
  申请人：PITMAN-MOORE LIMITED

  公开号：EP0441475A2

  公开（公告）日：1991-08-14

  The antibacterial substance baquiloprim (2,4-diamino-5-[8-dimethylamino-7-methyl-5-quinolylmethyl] pyrimidine) is shown to be active against protozoal infections, e.g. toxoplasmosis. Preferably the baquiloprim is administered together with a sulphonamide.

  抗菌物质巴基洛普林（2,4-二氨基-5-[8-二甲氨基-7-甲基-5-喹啉基甲基]嘧啶）对原生动物感染（如弓形虫病）具有活性。巴基洛普林最好与磺胺一起使用。
• Pharmaceutical composition comprising a medicament and a water-swellable polymer
  申请人：MALLINCKRODT VETERINARY, INC.

  公开号：EP0236002B2

  公开（公告）日：1996-10-23