Abstract：
:Alkyl 2-imidazolyl disulfide compounds are novel antitumor agents, one of which is currently being evaluated in Phase I clinical trials. These molecules contain an unsymmetrical disulfide fragment, the lipophilic and electronic contributions of which are still not defined in the literature. Lipophilicity, ionization, and solubility of a number of alkyl 2-imidazolyl disulfides were studied. Based on the additivity of lipophilicity and ionization properties, the contribution of the unsymmetrical disulfide fragment to lipophilicity and ionization was elucidated. The unsymmetrical disulfide fragment contributed a Rekker's hydrophobic constant of 0.761 to the lipophilicity of these compounds and an approximated Hammett constant (sigma) of 0.30 to their ionization. The applicability of the general solubility equation (GSE) proposed by Jain and Yalkowsky in predicting the aqueous solubility of these analogs was evaluated. The GSE correctly ranked the aqueous solubilities of these compounds and estimated their log molar solubilities with an average absolute error of 0.35.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Hashash A,Kirkpatrick DL,Lazo JS,Block LHdoi
10.1002/jps.10112subject
Has Abstractpub_date
2002-07-01 00:00:00pages
1686-92issue
7eissn
0022-3549issn
1520-6017pii
S0022-3549(16)31039-5journal_volume
91pub_type
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