A compound having the formula ##STR348## or a pharmaceutically acceptable salt, ester or amide thereof, wherein R.sup.1 in formula (I) is selected from (a) loweralkyl, (b) loweralkenyl, (c) halo(loweralkyl), (d) loweralkoxy, (e) cycloalkyl of from three to eight carbon atoms, (f) phenyl, (g) substituted phenyl, (h) halo, (i) cyano, (j) nitro, (k) bicycloalkyl, (1) loweralkynyl, (m) loweralkoxycarbonyl, (n) nitrogen-containing aromatic heterocycle, selected from the group consisting of pyridine, pyrazine, pyrimidine, pyrrazole, imidazole, thiazole, oxazole, isoxazole, thiadiazole and oxadiazole, (o) halo-substituted nitrogen-containing aromatic heterocycle, where the nitrogen-containing aromatic heterocycle is as defined above, (p) a 4-, 5- or 6-membered cyclic ether, and (q) --NR.sup.7 R.sup.8 where R.sup.7 and R.sup.8 are independently selected from the group consisting of_hydrogen, loweralkyl and alkanoyl of from one to eight carbon atoms or, taken together with the nitrogen atom to which they are attached, R.sup.7 and R.sup.8 form a 5-, 6- or 7-membered heterocycle;
- R.sup.2 in formula (I) is selected from (a) halogen, (b) loweralkyl, (c) loweralkenyl, (d) cycloalkyl of from three to eight carbons, (e) cycloalkenyl of from four to eight carbons, (f) loweralkoxy, (g) aryloxy, (h) aryl(loweralkyl)oxy, (i) aryl(loweralkyl), (j) cycloalkyl(loweralkyl), (k) amino, (1) (loweralkyl)amino, (m) aryl(loweralkyl)amino, (n) hydroxy-substituted (loweralkyl)amino, (o) phenyl, (p) substituted phenyl, (q) bicyclic nitrogen-containing heterocycle, (r) nitrogen-containing aromatic heterocycle as defined above, (s) nitrogen-containing heterocycle having the formula ##STR349## (t) non-nitrogen-containing heterocycle having the formula ##STR350## where x is zero, one, two or three;
- R.sup.9 is selected from the group consisting of (i) --(CH.sub.2).sub.m - where m is one, two or three, and (ii) --(CH.sub.2).sub.n R.sup.13 (CH.sub.2).sub.p - where R.sup.13 is selected from --S--, --O-- and --NH--, R.sup.10 is CH.sub.2, or when R.sup.9 is selected from option (i) may be O, S or N, n is one or two, and p is one or two;
- and R.sup.31 is --(CH.sub.2).sub.q R.sup.32 - where R.sup.32 is selected from --S-- and --O--, and q is one, two or three;
- and Y is independently selected at each occurrence from the group consisting, of:
- (i) loweralkyl,
- (ii) hydroxy,
- (iii) halogen,
- (iv) halo(loweralkyl),
- (v) hydroxy-substituted loweralkyl,
- (vi) loweralkenylamino,
- (vii) loweralkylamino,
- (viii) loweralkoxy,
- (ix) (loweralkoxy)loweralkylamino,
- (x) loweralkoxy(loweralkyl),
- (xi) loweralkoxy(loweralkoxy)(loweralkyl),
- (xii) hydroxy-substituted loweralkyl,
- (xiii) imino,
- (xiv) alkoxycarbonyl,
- (xv) carbamoyl,
- (xvi) aryl(loweralkyl),
- (xvii) aminoxy
- (xviii) amino(loweralkyl),
- (xix) halo(loweralkyl)amino,
- (xx) halo(loweralkyl)amino(loweralkyl),
- (xxi) thioloweralkoxy(loweralkyl),
- (xxii) aminothioloweralkoxy,
- (xxiii) cycloalkyl of from three to six carbon atoms,
- (xxiv) cycloalkyl(loweralkyl),
- (xxv) cycloalkylamino,
- (xxvi) phenyl,
- (xxvii) substituted phenyl,
- (xxviii) substituted phenyl(loweralkyl)
- (xxix) nitrogen-containing aromatic heterocycle as defined above,
- (xxx) --NR.sup.11 R.sup.12 where R.sup.11 and R.sup.12 are independently selected from hydrogen and loweralkyl or, when one of R.sup.11 and R.sup.12 is hydrogen, the other is alkanoyl of from one to eight carbon atoms, an alpha-amino acid, or a polypeptide residue of from two to five amino acids, and
- (xxxi) --C(R.sup.21)(R.sup.22)NH.sub.2 where R.sup.21 and R.sup.22 are independently selected from among hydrogen, loweralkyl, hydroxy-substituted loweralkyl, amino(loweralkyl), loweralkoxy-(loweralkyl), thioloweralkoxy(loweralkyl), cycloalkyl of from three to six carbon atoms, and loweralkyl substituted with nitrogen-containing aromatic heterocycle as defined above or, taken together with the carbon atom to which they are attached, R.sup.21 and R.sup.22 form a ring structure selected from cycloalkyl of from three to six carbon atoms and nitrogen-containing heterocycle;
- R.sup.3 is selected from the group consisting of hydrogen, halogen and loweralkoxy;
- R.sup.4 is selected from the group consisting of hydrogen, loweralkyl, a pharmaceutically acceptable cation, and a prodrug ester group;
- R.sup.5 is selected from the group consisting of (a) hydrogen, (b) halogen, (c) hydroxy, (d) loweralkyl, (e) halo(loweralkyl), (f) loweralkoxy, and (g) --NR.sup.13 R.sup.14 where R.sup.13 and R.sup.14 are independently selected from the group consisting of hydrogen, loweralkyl, hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), and alkanoyl of from one to eight carbon atoms;
- and
- A is .dbd.CR.sup.6 -, where R.sup.6 is selected from the group consisting of (a) hydrogen, (b) halogen, (c) loweralkyl, (d) halo(loweralkyl), (e) hydroxy-substituted loweralkyl, (f) loweralkoxy(loweralkyl), (h) loweralkoxy, and (i) amino(loweralkyl);
- provided that, when R.sup.5 is hydrogen and A is .dbd.CH--, R.sup.1 is not unsubstituted phenyl.