| 摘要 |
The guanidine, urea and thiourea derivatives have the formula I R2-N(R4)-A-n(R3)-R1 or salts thereof wherein: A is -C(Zi)- or -S(O)n-; Z1 is O, Se, NRa or -C(Ra)2-; n is 1 or 2; Ra is H, ORb, CN, NO2, N(Rb)2, S(O)mRb, CORb, CO2Rb, PO(ORb)2, or PO(NRb)2; m is 0 to 2; R1 is an optionally saturated, optionally substituted 3 to 8 membered monocyclic ring having 0 to 4 heteratoms selected from S, O and N or R1 is an optionally saturated, optionally substituted 7 to 10 membered bicyclic ring having 0 to 5 heteratoms selected from S, O and N; R2 is R5-C(R6)(R8)-C(R7)(R9)-; R5 is as defined for R1 above or is (R10)y-X-; R6 to R9 are independently H, cycloalkyl, optionally substituted alkyl, alkenyl, alkynyl or alkoxy, halo, amino, nitro, cyano, hydroxy, carboxy, hydroxymethyl, aminomethyl, carboxymethyl, alkylthio, alkanoyloxy or carbamoyl or two of R6 to R9 together with the carbons to which they are attached can form an optionally saturated, optionally substituted 3 to 7 membered monocyclic ring having 0 to 4 heteratoms selected from S, O and N; Rb, R10, y and X are as defined in the specification and R3 and R4 are independently H, OH, optionally substituted alkyl, alkenyl, alkynyl or alkoxy, amino, nitro, cyano, carboxy, hydroxymethyl, aminomethyl, carboxymethyl, alkylthio, alkanoyloxy or carbamoyl; limited by the provisos as defined in the specification. Carboxyl, carboxymethyl and/or carbamoyl include the corresponding acceptable alkyl and aryl esters. A medicament thereof is for inhibiting the replication of HIV. The use of the above compounds not limited by the above provisos in the manufacture of a medicament is for inhibiting the replication of HIV.
|
