A compound having Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein: A 1 is selected from the group consisting of optionally substituted phenyl, optionally substituted 5- or 6-membered heteroaryl, optionally substituted cycloalkyl, optionally substituted heterocyclo, and aralkyl; X is selected from the group consisting of -O-, -S-, -SO 2 -, -CH 2 -, -CH -, -C(=O)-, -C(=O)N -, and -SO 2 N-; A 2 is selected from the group consisting of optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclo, and optionally substituted cycloalkyl; G is selected from the group consisting of dihydroxyalkyl, -CH CH C(=O)E, and -C(=O)E; E is selected from the group consisting of hydroxy, alkoxy, hydroxyalkyl, and -NR 1a R 1b; R 1a is selected from the group consisting of hydrogen, alkyl, aralkyl, (heterocyclo)alkyl, (heteroaryl)alkyl, (amino)alkyl, (alkylamino)alkyl, (dialkylamino)alkyl, (carboxamido)alkyl, (cyano)alkyl, alkoxyalkyl, hydroxyalkyl, and heteroalkyl; R 1b is selected from the group consisting of hydrogen and alkyl; or R 1a and R 1b taken together with the nitrogen atom to which they are attached form a 3- to 8-membered optionally substituted heterocyclo; R 2a and R 2b are independently selected from the group consisting of hydrogen and alkyl; n is 1, 2, or 3; Y is selected from the group consisting of - OR 4a and -NR 4b R 5; R 3 selected from the group consisting of hydrogen, alkyl, halo, nitro, cyano, hydroxy, amino, alkylamino, dialkylamino, haloalkyl, hydroxyalkyl, alkoxy, haloalkoxy, and alkoxyalkyl; R 4a is selected from the group consisting of hydrogen, alkyl, (heterocyclo)alkyl, (heteroaryl)alkyl, (amino)alkyl, (alkylamino)alkyl, (dialkylamino)alkyl, (carboxamido)alkyl, (cyano)alkyl, alkoxyalkyl, hydroxyalkyl, heteroalkyl, R 4b is selected from the group consisting of hydrogen, alkyl, (heterocyclo)alkyl, (heteroaryl)alkyl, (amino)alkyl, (alkylamino)alkyl, (dialkylamino)alkyl, (carboxamido)alkyl, (cyano)alkyl, alkoxyalkyl, hydroxyalkyl, heteroalkyl, R 6 is selected from the group consisting of hydrogen, alkyl, and hydroxyalkyl; R 7 is selected from the group consisting of hydroxy, alkoxy, and -NR 8a R 8b; R 8a is selected from the group consisting of hydrogen, alkyl, aralkyl, (heterocyclo)alkyl, (heteroaryl)alkyl, (amino)alkyl, (alkylamino)alkyl, (dialkylamino)alkyl, (carboxamido)alkyl, (cyano)alkyl, alkoxyalkyl, hydroxyalkyl, and heteroalkyl; R 8b is selected from the group consisting of hydrogen and alkyl; or R 8a and R 8b taken together with the nitrogen atom to which they are attached form a 3- to 8-membered optionally substituted heterocyclo; and R 5 is selected from the group consisting of hydrogen and alkyl; or R 4b and R 5 taken together with the nitrogen atom to which they are attached form a 3- to 8-membered optionally substituted heterocyclo. A 1 is selected from the group consisting of optionally substituted phenyl, optionally substituted 5- or 6-membered heteroaryl, optionally substituted cycloalkyl, optionally substituted heterocyclo, and aralkyl; X is selected from the group consisting of -O-, -S-, -SO 2 -, -CH 2 -, -CH -, -C(=O)-, -C(=O)N -, and -SO 2 N-; A 2 is selected from the group consisting of optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclo, and optionally substituted cycloalkyl; G is selected from the group consisting of dihydroxyalkyl, -CH CH C(=O)E, and -C(=O)E; E is selected from the group consisting of hydroxy, alkoxy, hydroxyalkyl, and -NR 1a R 1b; R 1a is selected from the group consisting of hydrogen, alkyl, aralkyl, (heterocyclo)alkyl, (heteroaryl)alkyl, (amino)alkyl, (alkylamino)alkyl, (dialkylamino)alkyl, (carboxamido)alkyl, (cyano)alkyl, alkoxyalkyl, hydroxyalkyl, and heteroalkyl; R 1b is selected from the group consisting of hydrogen and alkyl; or R 1a and R 1b taken together with the nitrogen atom to which they are attached form a 3- to 8-membered optionally substituted heterocyclo; R 2a and R 2b are independently selected from the group consisting of hydrogen and alkyl; n is 1, 2, or 3; Y is selected from the group consisting of - OR 4a and -NR 4b R 5; R 3 selected from the group consisting of hydrogen, alkyl, halo, nitro, cyano, hydroxy, amino, alkylamino, dialkylamino, haloalkyl, hydroxyalkyl, alkoxy, haloalkoxy, and alkoxyalkyl; R 4a is selected from the group consisting of hydrogen, alkyl, (heterocyclo)alkyl, (heteroaryl)alkyl, (amino)alkyl, (alkylamino)alkyl, (dialkylamino)alkyl, (carboxamido)alkyl, (cyano)alkyl, alkoxyalkyl, hydroxyalkyl, heteroalkyl, R 4b is selected from the group consisting of hydrogen, alkyl, (heterocyclo)alkyl, (heteroaryl)alkyl, (amino)alkyl, (alkylamino)alkyl, (dialkylamino)alkyl, (carboxamido)alkyl, (cyano)alkyl, alkoxyalkyl, hydroxyalkyl, heteroalkyl, R 6 is selected from the group consisting of hydrogen, alkyl, and hydroxyalkyl; R 7 is selected from the group consisting of hydroxy, alkoxy, and -NR 8a R 8b; R 8a is selected from the group consisting of hydrogen, alkyl, aralkyl, (heterocyclo)alkyl, (heteroaryl)alkyl, (amino)alkyl, (alkylamino)alkyl, (dialkylamino)alkyl, (carboxamido)alkyl, (cyano)alkyl, alkoxyalkyl, hydroxyalkyl, and heteroalkyl; R 8b is selected from the group consisting of hydrogen and alkyl; or R 8a and R 8b taken together with the nitrogen atom to which they are attached form a 3- to 8-membered optionally substituted heterocyclo; and R 5 is selected from the group consisting of hydrogen and alkyl; or R 4b and R 5 taken together with the nitrogen atom to which they are attached form a 3- to 8-membered optionally substituted heterocyclo.