Albicidin derivatives, their use and synthesis

A compound having formula (23)

• a. with X1 being BA-D1 with BA being selected from
• with R2 and R3 being selected, where applicable, independently from each other from —H, —F, —CN, —OH, a substituted or unsubstituted C1-C3 alkyl, a substituted or unsubstituted C1-C3 alkoxy or a C1-C3 haloalkyl,
• with E being
• a substituted or unsubstituted C1-C16 alkyl, a substituted or unsubstituted C1-C16 alkoxy, a substituted or unsubstituted C1-C16 carboxy, a substituted or unsubstituted C2-C16 alkenyl, a substituted or unsubstituted C2-C16 alkynyl, or a C1-C16 haloalkyl, —
• a substituted or unsubstituted C3-C10 cycloalkyl or a substituted or unsubstituted C3-C10 halo cycloalkyl,
• a substituted or unsubstituted C3-C10 heterocycle or a substituted or unsubstituted C3-C10 halo heterocycle,
• a substituted or unsubstituted C5-C10 heteroaryl, or
• with n of R1n being 0, 1, 2, 3, 4, or 5, and
• with each R1 independently from any other R1 being selected from the group consisting of —OH, —F, —Cl, —Br, —I, —CCH, —CN, —N3, —OCH3, —OCF3, —NH2, —NHCH3, —N(CH3)2, —CH3, —CH2—CH3, —CF3, —OCONH2 or —NO2, B(ORa)(ORb), —(CH2)m—Ra, —(CH2)m—ORa, —(CH2)m—C(═O)Ra, —(CH2)m—C(═O)ORa, —(CH2)m—OC(═O)Ra, —(CH2)m—OC(═O)ORa, —(CH2)m—OC(═O)NRaRb, —(CH2)m—C(═O)NRaRb, —(CH2)m—C(═O)NRaRb, —(CH2)m—C(═O)NRb(ORa), —(CH2)m—C(═S)Ra, —(CH2)m—C(═S)ORa, —(CH2)m—OC(═S)Ra, —(CH2)m—OC(═S)ORa, —(CH2)m—OC(═S)NRaRb, —(CH2)m—C(═S)NRaRb, —(CH2)m—SRa, —(CH2)m—S(═O)Ra, —(CH2)m—S(O2)Ra, —(CH2)m—S(O2)ORa, —(CH2)m—OS(O2)Ra, —(CH2)m—OS(O2)ORa, —(CH2)m—NRaRb, —(CH2)m—NRcC(═O)Ra, —(CH2)m—NRcC(═O)NRaRb, —(CH2)m—NRcC(═O)ORa, —(CH2)m—NRcC(═S)Ra, —(CH2)m—NRcC(═S)NRaRb, —(CH2)m—NRcC(═S)ORa, —(CH2)m—NRcS(O2)Ra, —(CH2)m—P(═O)(ORb)(ORa), —(CH2)m—P(═O)(ORb)(Ra) or —(CH2)m—S(O2)NRbRa, —(CH2)m—O—C(═O)—(M)—C(═O)OH, —(CH2)m—O—C(═O)—(M)—C(═O)ORa, —(CH2)m—O—C(═O)—(M)—Ra, —(CH2)m—O—(CH2)q—P(═O)(Rba)(Raa), —(CH2)m—C(═O)O—(CH2)q—P(═O)(Rba)(Raa), —(CH2)m—C(═O)O—(CH2)q—S(O2)OH or —(CH2)m—C(═O)O—(CH2)q—S(O2)ORa,
• with Raa being selected independently from each other being —Ra or —ORa,
• with Rba being selected independently from each other being —Rb or —ORb,
• with M being a substituted or unsubstituted C1-C8 alkyl,
• with m being selected from 0, 1 or 2,
• with q being selected from 0, 1 or 2, and
• with each Ra, Rb or Rc being selected independently from each other from
• hydrogen, —CN,
• a substituted or unsubstituted C1-C16 alkyl, a substituted or unsubstituted C1-C16 alkoxy, a substituted or unsubstituted C1-C16 carboxy, a substituted or unsubstituted C2-C16 alkenyl, a substituted or unsubstituted C2-C16 alkynyl, or a C1-C16 haloalkyl, a substituted or unsubstituted C3-C10 cycloalkyl, or a substituted or unsubstituted C3-C10 halo cycloalkyl,
• a substituted or unsubstituted C3-C10 cycloalkyl or a substituted or unsubstituted C3-C10 halo cycloalkyl,
• a substituted or unsubstituted C3-C10 heterocycle or a substituted or unsubstituted C3-C10 halo heterocycle,
• a substituted or unsubstituted C5-C10 heteroaryl,
• a substituted or unsubstituted C6-C10 aryl;
• b. with BC being selected from
• with Y being selected from —CN, —C(═O)OH, —C(═O)OCH3, —C(═O)OCH2CH3, —C(═O)NHCH3, —C(═O)NHCH2CH3, —C(═O)N(CH3)2, —C(═O)N(CH2CH3)2, —C(═O)N(CH3)(CH2CH3), —CF3 or —C(═O)NH2, and
• with Z being selected from —H, —OH, —CH3, —CH2CH3, —OCH3, —NH2, —NHCH3, —N(CH3)2, —N(CH3)3+;
• c. with each R8 being
• —H, or, with each R8 being selected independently from each other from —H, —CH3, —CH2CH3;
• d. with n of R10n being 1 or 2;
• and
• with each R10 independently from any other R10 being selected from
• —OH, —F, —Cl, —Br, I, —CCH, —CN, —N3, —OCH3, —OCF3, —NH2, —NHCH3, —N(CH3)2, —CH3, —CH2—CH3, —CF3, or —NO2;
• e. with n of R11n being 0, 1, 2, 3 or 4,
• with each R11 being selected independently from any other from any other R11 from —OH, —F, —Cl, —Br, —I, —CCH, —CN, —N3, —OCH3, —OCF3, NH2, —NHCH3, —N(CH3)2, —CH3, —CH2CH3, —CH2OCH3, —CHCH2, —CH2OH, —SO2NH2, —SO2N(CH3)2, —SO2NHCH3, —CH3, —CF3, or —NO2;
• f. with T being selected from
• —OH, —F, —Cl, —Br, I, —CCH, —CN, —N3, —OCH3, —OCF3, —NH2, —NHCH3, —N(CH3)2, —CH3, —CH2—CH3, —CF3 or —NO2,
• —(CH2)m—C(═O)ORa, —(CH2)m—S(O2)ORa, with m being selected from 0, 1 or 2, with Ra being
• hydrogen,
• a substituted or unsubstituted C1-C16 alkyl, a substituted or unsubstituted C2-C16 alkenyl, a substituted or unsubstituted C2-C16 alkynyl, or a C1-C16 haloalkyl, or a substituted or unsubstituted C3-C10 cycloalkyl or a substituted or unsubstituted C3-C10 halo cycloalkyl;
• g. with D1, D4 and D5 being each independently from each other from
• wherein
• each R8 being —H, or with each R8 being selected independently from each other from —H, —CH3, —CH2CH3, and
• V being O;
• h. wherein the compounds of formulae (2a) is disclaimed:
• wherein R1 is H or CO(NH2), R2′ is CO(NH2) or CN, R3′ is H or OCH3.