[From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist.]
>>Bioorg Med Chem Lett. 2006 Oct 1;16(19):5217-21. Epub 2006 Jul 25.
From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist.
Zheng X, Hodgetts KJ, Brielmann H, Hutchison A, Burkamp F, Brian Jones A,
Blurton P, Clarkson R, Chandrasekhar J, Bakthavatchalam R, De Lombaert S,
Crandall M, Cortright D, Blum CA.
Neurogen Corporation, 35 N. E. Industrial Road, Branford, CT 06405, USA.
Bioisosteric replacement of piperazine with an aryl ring in lead VR1 antagonist 1 led to the biarylamide series. The development of B-ring SAR led to the conformationally constrained analog 70. The resulting aminoquinazoline 70 represents a novel VR1 antagonist with improved in vitro potency and oral bioavailability vs the analogous compounds from the lead series.<<
Figuring that even three sentences of chemistry might be too much for Rick, I posted this for you -- though I have no idea if you care about NRGN. I also have no idea if the current lead compound would be this analog 70, or if analog 70 is a back-up, farther behind.
Bought a small position a couple of weeks ago for $5.80, which is looking good at the moment.
Cheers, Tuck |
