Bredinin in .NET framework

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Bredinin
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O N N HO O OH OH 9 NH2 OH HO O OH OH H N N O O NH2
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The natural product bredinin (9) or mizoribine (4-carbamoyl-1-b-Dribofuranosylimidazolium-5-olate) is a derivative of AICAR.62 X-ray analysis of this compound con rmed its chemical structure and its zwitterionic nature. It can be synthesized by standard Vorbruggen coupling methods.72 Bredinin can be synthesized also by enzymatic coupling of 4-carbamoylimidazolium-5-olate through a transferase reaction catalyzed by purine nucleoside phoshporylases.62 Bredinin 50 -monophosphate is a potent inhibitor of IMPDH (Ki 0.5 nM).15
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INHIBITORS OF IMPDH WITH ACTIVITY AGAINST VIRUSES
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FIGURE 8.11 Human type II IMPDH: crystal structure of tetramer.54 (Reproduced with permission of Proceedings of the National Academy of Sciences of the United States of America.) (See insert for color representation.)
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Bredinin exhibits potent immunosuppressive activity. It also exhibits broadspectrum antiviral activity including activity against three strains of RSV, one strain each of the in uenza virus (FluV) types A and B, parain uenza virus (PFluV) types 2 and 3, mumps virus (MPSV), and measles virus (MLSV).73 It has also been reported to be active against the vaccinia virus.74 The mechanism of viral inhibition appears to be associated with the inhibition of IMPDH by the monophosphate of this compound. As in the case of ribavirin, other mechanisms may also be possible.
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2-[2(Z )-Fluorovinyl]inosine
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2-Fluorovinylinosine (2-FVIMP, 10), an analogue of the broad-spectrum antiviral compound 2-vinylinosine (discussed is Section 8.4.6) has been synthesized recently by us75 through a multistep route, which is described in detail in Scheme 8.2.
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IMPDH INHIBITORS: DISCOVERY OF ANTIVIRAL AGENTS AGAINST EMERGING DISEASES
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O N N HO O OH OH N NH NH2
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(1) Ac2O, DMAP Et3N, CH3CN
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Cl N N AcO
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(2) POCl3, N,N-diethylaniline
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N N NH2
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O OAc OAc
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n-C5H11ONO, CH2I2, CH3CN
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Cl N N AcO O OAc OAc
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OsO4, N-Methylmorpholine N-oxide NaIO4-H2O/ CH2Cl2
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Cl N N
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(Bu)3SnCH=CH2 Pd (CH3CN)2Cl2/ DMF
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N N I
N AcO O OAc OAc
Cl N N AcO O OAc OAc N N
(i) Bu3P, CFCl3, CH2Cl2
Cl N CHO
(ii) 10% NaOH
N AcO O OAc OAc
NH3, MeOH
O N N HO O OH OH
(ii) HPLC (i) POCl3 triethylphosphate
Cl NH F H
Adenosine deaminase
N N HO O OH OH N
O N NH N F H
O O P O O
N O OH OH
SCHEME 8.2 Synthesis of 2- uorovinylinosine and its 50 -monophosphate.
INHIBITORS OF IMPDH WITH ACTIVITY AGAINST VIRUSES
O N N HO O OH OH 10 N N H F H
We have carried out detailed studies of the inhibition of bacterial IMPDH by 2 uorovinylinosine 50 -monophosphate.76 The inhibition reaction was monitored by following the increase in absorbance at 340 nm due to the formation of NADH. The data were tted into the following equation [1]: ln Vt =V0 kobs t 1
where Vt is the activity at time t and V0 is the activity at time t 0. The kobs values obtained for inactivation of IMPDH were then tted into the equation [2]: kobs kinact I = Ki I 2
where kinact is the inactivation rate constant, Ki is the apparent dissociation constant, and [I] is the inhibitor (2-FVIMP) concentration. Incubation of IMPDH with 2-FVIMP exhibited a time-dependent decrease in Vt =V0 as shown in Figure 8.12. This is an indication that 2-FVIMP inactivates the enzyme. For further understanding of the mechanism of inhibition, the kobs values obtained by using equation [1] were plotted against inhibitor concentration. The hyperbolic relationship observed between kobs and 2-FVIMP concentration (Figure 8.13) suggests that 2-FVIMP interacts with IMPDH through a two-step mechanism as follows: E I E:I ! E I
k 1 k1 Kinact
where Ki k1 =k 1 , E is IMPDH, E.I is the reversibly bound enzyme inhibitor complex, and E I is the irreversibly inactivated enzyme. Thus, it appears that the mechanism of inactivation of IMPDH by 2-FVIMP involves the initial reversible formation of an E.I complex followed by the inactivation step. The values of kinact and Ki were determined using equation [2] by plotting the reciprocal of kobs versus the reciprocal of inhibitor concentration. The values of kinact and Ki were 0.0269 s 1 and 1.11 mM, respectively, whereas the well-known IMPDH inhibitor 6-chloropurine ribonucleoside monophosphate in these studies
IMPDH INHIBITORS: DISCOVERY OF ANTIVIRAL AGENTS AGAINST EMERGING DISEASES
FIGURE 8.12 Inhibition of E. coli IMPDH by 2-FVIMP with respect to time.76 (*, 0.25 mM; *, 0.50 mM; 3, 0.75 mM; 4, 1.0 mM; &, 1.5 mM.)
gave values of 0.076 min 1 and 62.0 mM. The type of inactivation of IMPDH shown by 2-FVIMP is related to that exhibited by ethynylimidazole carboxamide riboside monophosphate (EICARMP).37 Antiviral screening of 10 against the vaccinia and cowpox viruses (HFF cell line) showed moderate activity (T.I.$4).77 The mechanism of this antiviral activity is likely associated with the ability of the cellularly produced monophosphate to be an inhibitor of IMPDH.