464179-65-5Relevant academic research and scientific papers
SIALIDASE INHIBITORS AND PREPARATION THEREOF
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, (2018/11/22)
New 2-deoxy-2,3-dehydro-sialic acids and 2,7-anhydro-sialic acids, which are useful as sialidase inhibitors, and enzymatic methods for preparing them are disclosed. The methods include forming a reaction mixture comprising a glycoside acceptor, a sialic acid donor, and a sialyltransferase; maintaining the reaction mixture under conditions sufficient to form a sialoside; and contacting the sialoside with a Streptococcus pneumoniae sialidase to form the sialic acid product. Methods for the inhibition and sialidases and the treatment of cancer and infectious diseases are also disclosed.
Compounds useful for inhibiting paramyxovirus neuraminidase
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, (2008/06/13)
Compounds represented by the formula: wherein X is selected from the group consisting of: CHR, O, NR, N—OR, NR(O), S, S(O) and S(O)O X1 is selected from the group consisting of CR, N, and N(O); R is selected from the group consisting of: H, alkyl, alkene, alkyne, CN, NO2, N3, halo and NHR10; R1 is selected from the group consisting of: H, (CH2)nCO2R10, (CH2)n-tetrazol, (CH2)nSO3H, (CH2)nSO2H, (CH2)nPO3H2, (CH2)nCONR10, (CH2)nNO2, and (CH2)nCHO; R1a is selected from the group consisting of: H, (CH2)nOR10, (CH2)nCN, (CH2)nNR10R10a, (CH2)nNHC(O)R10, (CH2)nC(O)NR10R10a, and (CH2)nOC(O)R10; R1 and R1a both cannot be H each of R2 and R2a is independently selected from the group consisting of H, halo, CN, (CH2)nCO2R10, (CH2)nNR10R10a and (CH2)n—OR10; each of R3 and R3a is independently selected from the group consisting of: H, NHSO2R10, N(O)—SO2R10, NR10SO2R10a, (CH2)mYR10, and (CH2)mR6; at least one of R3 and R3a should be other than H Y is selected from the group consisting of: O, NH, NHC(O), C(O)NH, S, S(O), S(O)O, NHS(O)O, S(O)ONH, NHC(O)NH and heterocycle; R3 and R3a together may be ═O, ═CHR6, ═CHR10, ═NR10, NR10 and ═N—OR10 R4 and R4a is independently selected from the group consisting of: H, (CH2)mYR10 and (CH2)mR6 R4 and R4a together may be: ═O, ═CHR6, ═CHR10, ═NR10 and ═N—OR10 each of R5 and R5a is independently selected from the group consisting of C(R7)(R7a), C(R7)(R7a)C(R8)(R8a), C(R7)(R7a)C(R8)(R8a)C(R9)(R9a), OC(R7)(R7a), OC(R7)(R7a)C(R8)(R8a), C(R7)(R7a)OC(R8)(R8a), N(R10)C(R7)(R7a), N(R10) C(R7)(R7a)C(R8)(R8a), C(R7)(R7a)N(R10)C(R8)(R8a), and C(O)NR10R10a; R6 is selected from the group consisting of H, halo, CN, NO2, N3, CO2R10, R10 and NR10R10a; R7, R7a, R8, R8a, R9 and R9a is selected from the group from the group consisting of: H, (CH2)mYR10 and (CH2)mR6 each of the R10 and R10a is individually selected from the groups consisting of: H, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heterocycle, substituted heterocycle, alkenyl, substituted alkenyl, alkynyl, and substituted alkynyl; Each of m and n is individually 0, 1, 2, 3, or 4; and pharmaceutically acceptable salt thereof; and prodrugs thereof, and uses thereof.
