Highly regioselective synthesis of N-3 organophosphorous derivatives of 3,4-dihydropyrimidin-2(1H)-ones and their calcium channel binding studies.
A series of novel N-3 substituted 3,4-dihydropyrimidin-2(1H)-ones derivatives bearing diaminophosphinyl, phosphonate and phosphorous containing heterocycles were obtained from 3,4-dihydropyrimidinones (DHPMs) in a regioselective manner through an efficient reaction protocol, tolerant to substitutional variation at the key diversity positions around the DHPM core. None of the representative compounds screened for calcium channel blocking activity was found to have significant activity compared to nifedipine.
Organic Synthesis Laboratory, Department of Applied Chemical Sciences and Technology, UGC SAP (DRS-1) Department, Guru Nanak Dev University, Amritsar 143005, India. kamaljit19in@yahoo.co.in
Kamaljit
K
Singh
Kawaljit
K
Singh
Danielle M
DM
Trappanese
Robert S
RS
Moreland
D002121:Calcium Channel Blockers / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism*; D015220:Calcium Channels / Q000378:metabolism*; D009943:Organophosphorus Compounds / Q000737:chemistry*; D011485:Protein Binding; D011744:Pyrimidinones / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism*; D013237:Stereoisomerism; D013379:Substrate Specificity
D002121:Calcium Channel Blockers; D015220:Calcium Channels; D009943:Organophosphorus Compounds; D011744:Pyrimidinones