Stereo-isomeric dissociation of the antibacterial and the neuroleptic effect of clopenthixol.

J E Kristiansen, I Mortensen
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Abstract

Measurement of the IC50 of cis(Z)-clopenthixol and trans(E)-clopenthixol on 188 bacterial strains from human clinical specimens shows that the antibacterial activity of clopenthixol is exerted by both isomerical components and trans(E)-clopenthixol is the most active antibiotic of the two drugs against the sensitive strains. It is known that the trans(E)-clopenthixol isomere is without neuroleptic effect. The possibility of creating new antibiotics by e.g. steric alteration of neuroleptical agents is stressed. These drugs have different antibiotic patterns from those of classical antibiotics. It seems particularly promising that Pseudomonas aeruginosa is sensitive to these drugs.

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氯戊硫醇的立体异构体解离抑菌及抗精神病作用。
测定了顺式(Z)-氯戊硫醇和反式(E)-氯戊硫醇对188株人类临床标本细菌的IC50,结果表明,氯戊硫醇的抑菌活性是由同分异构体组分共同发挥的,反式(E)-氯戊硫醇是两种药物中对敏感菌株最有效的抗生素。已知反式(E)-氯戊二醇异构体无抗精神病作用。强调了通过神经安定剂的立体改变来创造新抗生素的可能性。这些药物与传统抗生素具有不同的抗生素模式。铜绿假单胞菌对这些药物敏感似乎特别有希望。
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