Abstract
PAF is a powerful phospholipid-derived autacoid involved in many physio-pathological mechanisms. Many PAF antagonists have been synthesized and assayed for therapeutic purposes. In this study, molecular electrostatic potential is used to compare the electronic properties of 48 ‘heterocyclic’ sp 2 nitrogen’ highly potent PAF antagonists, belonging to six series (nine hetrazepines, five pyrrolo[1,2- c]thiazoles, 14 carboxamides, nine dihydropyridines, nine pyridinylthiazolidines and two imidazo[4,5- c]pyridines). Their common features consist of three main electronegative zones (A, B 1, and B 2) describing the electronic pharmacophore of these ligands. The high affinity of these PAF antagonists seems to be related to this electronegative system A-B( x ), which is characterized by three distances A-B 1, (9.3 ± 1.0 Å), A-B 2 (13.4 ± 0.7 Å) and B 1–B 2 (4.9 ± 0.9 Å). Moreover, B 1 and B 2 may surround a common anchorage point in the binding site of the receptor.
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
