m-chlorophenylguanidine and 1-(3-chlorophenyl)biguanide

m-chlorophenylguanidine has been researched along with 1-(3-chlorophenyl)biguanide* in 1 studies

Other Studies

1 other study(ies) available for m-chlorophenylguanidine and 1-(3-chlorophenyl)biguanide

Article	Year
Conformationally-restricted analogues and partition coefficients of the 5-HT3 serotonin receptor ligands meta-chlorophenylbiguanide (mCPBG) and meta-chlorophenylguanidine (mCPG). Bioorganic & medicinal chemistry letters, 2003, Mar-24, Volume: 13, Issue:6 The present investigation examined two features of arylbiguanide and arylguanidine 5-HT(3) ligands: conformation and partition coefficients. Several conformationally-constrained analogues of mCPBG (2) and mCPG (11; K(i)=32 nM) were prepared and of these only 2-amino-5-chloro-3,4-dihydroquinazoline (14; K(i)=34 nM) retained high affinity. The partition coefficient of compound 11 (LogP(app)=-0.64) was less than that of its corresponding arylbiguanide 2 (LogP(app)=-0.38). The quinazoline structure may represent a pharmacologically-active conformation of these agents, and the arylbiguanides were found more lipid soluble than their arylguanidine counterparts at physiological pH. Topics: Biguanides; Chemical Phenomena; Chemistry, Physical; Guanidine; Ligands; Magnetic Resonance Spectroscopy; Molecular Conformation; Radioligand Assay; Receptors, Serotonin; Receptors, Serotonin, 5-HT3; Solubility; Structure-Activity Relationship	2003

Article

Year

Conformationally-restricted analogues and partition coefficients of the 5-HT3 serotonin receptor ligands meta-chlorophenylbiguanide (mCPBG) and meta-chlorophenylguanidine (mCPG).

Bioorganic & medicinal chemistry letters, 2003, Mar-24, Volume: 13, Issue:6

The present investigation examined two features of arylbiguanide and arylguanidine 5-HT(3) ligands: conformation and partition coefficients. Several conformationally-constrained analogues of mCPBG (2) and mCPG (11; K(i)=32 nM) were prepared and of these only 2-amino-5-chloro-3,4-dihydroquinazoline (14; K(i)=34 nM) retained high affinity. The partition coefficient of compound 11 (LogP(app)=-0.64) was less than that of its corresponding arylbiguanide 2 (LogP(app)=-0.38). The quinazoline structure may represent a pharmacologically-active conformation of these agents, and the arylbiguanides were found more lipid soluble than their arylguanidine counterparts at physiological pH.

Topics: Biguanides; Chemical Phenomena; Chemistry, Physical; Guanidine; Ligands; Magnetic Resonance Spectroscopy; Molecular Conformation; Radioligand Assay; Receptors, Serotonin; Receptors, Serotonin, 5-HT3; Solubility; Structure-Activity Relationship

2003