521290-74-4Relevant academic research and scientific papers
Discovery and SAR of hydrazide antagonists of the pituitary adenylate cyclase-activating polypeptide (PACAP) receptor type 1 (PAC1-R)
Beebe, Xenia,Darczak, Daria,Davis-Taber, Rachel A.,Uchic, Marie E.,Scott, Victoria E.,Jarvis, Michael F.,Stewart, Andrew O.
, p. 2162 - 2166 (2008/09/20)
Potent small molecule antagonists for the PAC1-R have been discovered. Previously known antagonists for the PAC1-R were slightly truncated peptide ligands. The hydrazides reported here are the first small molecule antagonists ever reported for this class B GPCR.
NON-NUCLEOTIDE REVERSE TRANSCRIPTASE INHIBITORS
-
Page/Page column 39, (2008/06/13)
Compounds of the formula Z: where; A is CH or N; R1 is a substituent to a carbon atom in the ring containing A selected from -S(=O)pRa, where Ra is -C1-C4 alkyl, -ORx, -NRxRx, -NHNRxRx, - NHNHC(=O)ORx, -NRxOH; -C(=O)-Rb, where Rb is -CT-C4-alkyl, ORx, -NRxRx, -NHNRxRx, -NHC1-C3-alkyl-C(=O)Orx -NRxRc, where Rc is H, C1-C4 alkyl, -NRxRx; -C(=0)Rd, -CN, S(=O)pRx where Rd is Rd is C1-C4-alkyl, -ORx, -NRxRx C1-C3-alkyl-O-Cl-C3alkylC(=O)ORx, -C1-C3-alkyl-COORx; -C1-C3alkyl-OH or C1-C4 alkyl ethers or esters thereof (O-Cl-C3alkyl)q-O-Rx a 5 or 6 membered aromatic ring having 1-3 hetero atoms p is 1 or 2; Rx is independently selected from H, C1-C4 alkyl or acetyl; or a pair of Rx can together with the adjacent N atom form a ring; L is -0-, -S(=O),- or -CH2-, where r is 0, 1 or 2; R3-R7 are substituents as defined in the specification; X is -(CR8R8')n-D-(CR8R8')m-; D is a bond, -NR9-, -0-, -S-, -S(=0)- or -S(=0)2-; and pharmaceutically acceptable salts and prodrugs thereof, have utility as HIV antivirals.
