New 2,5-diaryl tetrahydrothiophenes and analogs thereof as paf-antagonists.

摘要

2,5-Diaryl tetrahydrothiophene compounds of the general formula <CHEM> or a sulfoxide or sulfone thereof are disclosed wherein R and R<1> independently are (a) hydrogen; (b) lower alkyl of 1-6 carbon atoms; (c) haloloweralkyl; (d) halo; (e) COOH; (f) CONR<2>R<3> wherein R<2> and R<3> independently represent C1-6 alkyl and hydrogen; (g) COOR<2>; (h) loweralkenyl; (i) -COR<2>; (j) -CH2OR<2>; (k) loweralkynyl; (l) -CH2NR<2>R<3>; (m) -CH2SR<2>; (n) =O; or (o) -OR<2>; Ar and Ar<1> are the same or different from each other and are (a) phenyl or substituted phenyl of formula <CHEM> where R<4>-R<8> independently represent H, RO-, RS-, R<2>SO, R<2>-SO2-, CF3O-, CF3S-, R<2>R<3>N-, -OCH2CO2R<2>, -SO2NR<2>R<3>, -CO2R<2>, -NR<2>SO2R<3>, COR<2>, NO2, or CN or R<4>-R<5>, R<5>-R<6>, R<6>-R<7> and R<7>-R<8> are joined together forming a bridge; (b) pyrryl or substituted pyrryl; (c) furyl or substituted furyl; (d) pyridyl or substituted pyridyl; (e) thiophene or substituted thiophene; or (f) cyclohexyl or substituted cyclohexyl. These compounds are found to be leukotriene inhibitors and potent and specific PAF (Platelet Activating Factor) antagonists.