| Che-Ming Teng |
------>authors3_c= ------>paper_class1=6 ------>Impact_Factor=None ------>paper_class3=0 ------>paper_class2=0 ------>vol= ------>confirm_bywho=amel ------>insert_bywho=hpw ------>Jurnal_Rank=None ------>authors4_c= ------>comm_author= ------>patent_EDate=2013-01-01 00:00:00 ------>authors5_c= ------>publish_day=1 ------>paper_class2Letter=None ------>page2= ------>medlineContent= ------>unit=G0100 ------>insert_date=20080508 ------>iam=1 ------>update_date=None ------>author=??? ------>change_event=4 ------>ISSN= ------>authors_c= ------>score=2 ------>journal_name=India-IN-PCT-2002-01192-DEL-patent-granted Notification ------>paper_name=Piperazine compounds ------>confirm_date=20080508 ------>tch_id=096021 ------>pmid=19882697 ------>page1= ------>fullAbstract=Novel compounds were prepared in fair to good yields as human beta(3)-adrenoceptor (beta(3)-AR) agonists. In particular, aryloxypropanolamines 7 a-d (EC(50)=0.57-2.1 nM) and arylethanolamines 12 a,b,e (EC(50)=6.38-19.4 nM) were designed to explore the effects of modifications at the right-hand side of these molecules on their activity as beta(3)-AR agonists. Piperidine sulfonamides 15 a-c, e-g (EC(50)=6.1-36.2 nM) and piperazine sulfonamide derivatives 20-29 (EC(50)=1.79-49.3 nM) were examined as compounds bearing a non-aromatic linker on the right- and left-hand sides of the molecules. Some piperazine sulfonamides were found to be potent and selective beta(3)-AR agonists, even if the amine nitrogen atom is tertiary and not secondary, as is the case for all beta(3)-AR agonists reported so far. (S)-3-{4-{N-{4-{2-[2-Hydroxy-3-(4-hydroxyphenoxy)propylamino]ethyl}phenyl} sulfamoyl}phenoxy}propanoic acid (7 d; EC(50)=0.57 nM), (R)-N-{4-[2-(2-hydroxy-2-phenylethylamino)ethyl]phenyl}-4-(3-octylureido)b enzenesulfonamide (12 e; EC(50)=6.38 nM), (R)-2-[1-(4-methoxyphenylsulfonyl)piperidin-4-ylamino]-1-phenylethanol (15 f; EC(50)=6.1 nM), and (S)-4-{2-hydroxy-3-[4-(4-methoxyphenylsulfonyl)piperazin-1-yl]propoxy}phen ol (25; EC(50)=1.79 nM) were found to be the most potent beta(3)-AR agonists of the aryloxypropanolamine, arylethanolamine, piperidine sulfonamide, and piperazine sulfonamide classes, respectively. The two most potent compounds were identified as possible candidates for further development of beta(3)-AR agonists useful in the treatment of beta(3)-AR-mediated pathological conditions. ------>tmu_sno=None ------>sno=18553 ------>authors2=Hui-po Wang ------>authors3=Eric I. C. Li ------>authors4=On Lee ------>authors5=Jih Hwa Guh ------>authors6=Hui-Ting Chen ------>authors6_c= ------>authors=Che-Ming Teng ------>delete_flag=0 ------>SCI_JNo=None ------>authors2_c= ------>publish_area=0 ------>updateTitle=The Tertiary Amine Nitrogen Atom of Piperazine Sulfonamides as a Novel Determinant of Potent and Selective beta(3)-Adrenoceptor Agonists. ------>language=2 ------>check_flag=None ------>submit_date=None ------>country=?? ------>no= ------>patent_SDate=2003-01-01 00:00:00 ------>update_bywho=None ------>publish_year=2008 ------>submit_flag=None ------>publish_month=1 |