✦ LIBER ✦
The Partition Coefficient of Protonated Antihistamines. Its calculation and interpretation in terms of hydrophobic fragmental constants
✍ Scribed by Bernard Testa; Livia Murset-Rossetti
- Publisher
- John Wiley and Sons
- Year
- 1978
- Tongue
- German
- Weight
- 452 KB
- Volume
- 61
- Category
- Article
- ISSN
- 0018-019X
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✦ Synopsis
Abstract
The octanol/water partition coefficient (P~+~) of nineteen monoprotonated antihistaminic drugs has been measured. These values are compared with the partition coefficient (P) of the neutral molecules, suggesting the variations in partition coefficient seen upon protonation to obey simple rules. Indeed, the (log P–log P~+~) values are multiples of a constant term 0.28 (Rekker's ‘magic constant’ c~M~[6]), each functional group contributing with a fixed incremental value. The incremental values are confirmed by multiple linear regression analysis, and their physical significance is discussed.