ライフサイエンスコーパス: bithiazole

1 les with improved hydrophilicity compared to bithiazoles.

2 d bithiazole CF corrector 1 and s-cis-locked bithiazole 2.

3 o)-5,6-dihydro-4 H-cyclohepta[1,2- d:3,4- d']bithiazole-2'-yl)pivalamide 33.

4 o)-7,8-dihydro-6 H-cyclohepta[1,2- d:3,4- d']bithiazole-2'-yl)pivalamide, 29] results in improved cor

5 novel series of 4'-methyl-N(2)-phenyl-[4,5'-bithiazole]-2,2'-diamine inhibitors of gyrase B with a l

6 ed maximum efficacy (Vmax), with constrained bithiazoles 9e and 10c increasing Vmax by 1.5-fold compa

7 Eight C4'-C5 C,C-bond-controlling bithiazole analogues of 1 were designed, synthesized, an

8 Certain 4,4'-alkyl substituted 2,2'-bithiazole and bithiazole-thiophene oligomers display an

9 The solid-state structures of a series of bithiazole and thiophene oligomers, as well as a series

10 The importance of the bithiazoles and the partial intercalative mode of bindin

11 that the 7- and 8-membered constrained ring bithiazoles are similar in their ability to accommodate

12 orted here should be adaptable to many other bithiazole-based building blocks.

13 tant enzymes in vitro for their roles in BLM bithiazole biosynthesis.

14 ng block for HH linkages, 4,4'-dialkoxy-5,5'-bithiazole (BTzOR), and its incorporation into polymers

15 consistent with a binding model in which the bithiazole + C-terminal substituent of bleomycin bind to

16 modified metal-binding domain connected to a bithiazole/C-terminal tail via a methylvalerate-Thr link

17 We previously identified and characterized bithiazole CF corrector 1 and s-cis-locked bithiazole 2.

18 P of 4.1, which is 1.2 log units lower than bithiazole CF corrector 1.

19 were comparable with those conferred by the bithiazole Corr-4a and the flavone genistein, respective

20 asing Vmax by 1.5-fold compared to benchmark bithiazole corr4a.

21 othiazole 29 was found to be the most potent bithiazole corrector, with an IC50 of approximately 450

22 en 7- versus 8-membered in these constrained bithiazole correctors did not significantly enhance thei

23 o have improved efficacy over nonconstrained bithiazoles for correction of defective cellular process

24 they both adopt compact structures with the bithiazole group folded back over the N-terminus.

25 e TpA steps, and by the upfield shift of the bithiazole H-H5 and H-H5' proton resonances.

26 The bithiazole intercalates between base pairs involving eit

27 First, we report that the bithiazole intercalates in two distinct modes and can do

28 ons of recently proposed models in which the bithiazole is intercalated immediately 3' to the cleavag

29 es have indicated that the metal-binding and bithiazole moieties of BLM are both involved in the bind

30 Intercalation of the bithiazole moiety unfolds the CodPEP molecule and expose

31 ut it has been shown that replacement of the bithiazole moiety with a strong DNA binder can alter the

32 responsible for the biosynthesis of the BLM bithiazole moiety.

33 theses are reported of new 4,4'-dialkyl-2,2'-bithiazole oligomers that have alkenoxy side chains that

34 es, according to NOE connections between the bithiazole protons and protons from these bases and chan

35 als that the predominant conformation of the bithiazole protons is trans.

36 age occurs by partial intercalation of BLM's bithiazole tail 3' to the first cleavage site that facil

37 g the metal binding domain, threading of the bithiazole tail between base pairs, and finally position

38 Intercalation of the bithiazole tail between these base pairs is indicated by

39 CoBLM (HOO-CoBLM) have demonstrated that its bithiazole tail binds by partial intercalation to duplex

40 Studies with ZnBLM demonstrate that the bithiazole tail binds in the minor groove.

41 fects on the FeII site; intercalation of the bithiazole tail into the double helix likely brings the

42 The model reveals that the bithiazole tail is partially intercalated between the T1

43 which the penultimate thiazolium ring of the bithiazole tail is reduced.

44 For example, constraining the C4'-C5 bithiazole tether in the s-cis conformation [N-(2-(5-chl

45 tablish that constraining rotation about the bithiazole-tethering has a significant effect on correct

46 n 4,4'-alkyl substituted 2,2'-bithiazole and bithiazole-thiophene oligomers display an endothermic tr

47 In this study, two sets of constrained bithiazoles were designed, synthesized, and tested in vi

48 Conformationally constrained bithiazoles were previously found to have improved effic