-
1
-
-
33846606086
-
-
Some of these data have been previously reported: Kochanny, M. J.; Adler, M.; Cheeseman, S.; Chou, Y. L.; Davey, D. D.; Eagen, K. A.; Ewing, J.; Fitch, R.; Griedel, B. D.; Karanjawala, R.; Lee, W.; Lentz, D.; Liang, A.; Morrissey, M. M.; Phillips, G. B.; Post, J.; Sacchi, K. L.; Sakata, S. T.; Shaw, K. J.; Snider, R. M.; Subramanyam, B.; Trinh, L.; Vergona, R.; Walters, J.; Wang, Y. X.; White, K. A.; Whitlow, M.; Wu, S. C.; Ye, B.; Zhao, Z. Abstracts of Papers, 221st American Chemical Society National Meeting, April 1-5, 2001, San Diego, CA; Abstract MEDI-16.
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2
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33846631934
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Lee, W.; Ewing, J.; Griedel, B. D.; Karanjawala, R.; Lentz, D.; Liang, A.; Morrissey, M. M.; Post, J.; Sacchi, K. L.; Sakata, S. T.; Shaw, K. J.; Ye, B.; Kochanny, M.J. Abstracts of Papers, 221st American Chemical Society National Meeting, April 1-5, 2001, San Diego, CA; Abstract MEDI-126.
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0034624694
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Several other laboratories have also reported on the investigation of anthranilamide-derived inhibitors of Factor Xa. See Ref. 7, as well as the following:
-
Several other laboratories have also reported on the investigation of anthranilamide-derived inhibitors of Factor Xa. See Ref. 7, as well as the following:. Yee Y.K., Tebbe A.L., Linebarger J.H., Beight D.W., Craft T.J., Gifford-Moore D., Goodson Jr. T., Herron D.K., Klimkowski V.J., Kyle J.A., Sawyer J.S., Smith G.F., Tinsley J.M., Towner R.D., Weir L., and Wiley M.R. J. Med. Chem. 43 (2000) 873
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33846562547
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note
-
In later stages of this work, the preparation of 28 was carried out by bromination of the methyl group of 18 to afford the dibromomethyl product. This was followed by conversion to the aldehyde with sodium acetate in acetic acid, reduction with sodium borohydride, and basic hydrolysis to give hydroxy acid 28.
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-
-
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25
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0037468474
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Crystallography results for compound 31 (this paper and reference 16) confirm that the chlorophenyl moiety binds in the S1 pocket of fXa. Others have also observed binding modes for fXa inhibitors wherein a neutral group preferentially occupies the S1 pocket and the S4 pocket may contain a basic group:
-
Crystallography results for compound 31 (this paper and reference 16) confirm that the chlorophenyl moiety binds in the S1 pocket of fXa. Others have also observed binding modes for fXa inhibitors wherein a neutral group preferentially occupies the S1 pocket and the S4 pocket may contain a basic group:. Choi-Sledeski Y.M., Kearney R., Poli G., Pauls H., Gardner C., Gong Y., Becker M., Davis R., Spada A., Liang G., Chu V., Brown K., Collussi D., Leadley Jr. R., Rebello S., Moxey P., Morgan S., Bentley R., Kasiewski C., Maignan S., Guilloteau J.P., and Mikol V. J. Med. Chem. 46 (2003) 681
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Kasiewski, C.19
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Mikol, V.22
more..
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26
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24944536065
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33746486222
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Watson N.S., Brown D., Campbell M., Chan C., Chaudry L., Convery M.A., Fenwick R., Hamblin J.N., Haslam C., Kelly H.A., King N.P., Kurtis C.L., Leach A.R., Manchee G.R., Mason A.M., Mitchell C., Patel C., Patel V.K., Senger S., Shah G.P., Weston H.E., Whitworth C., and Young R.J. Bioorg. Med. Chem. Lett. 16 (2006) 3784
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28
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33846610594
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note
-
a values were measured for selected analogs in this series, and demonstrated the same rank order of lipophilicity and basicity as predicted by the calculations.
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30
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0028269097
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Hara T., Yokoyama A., Ishihara H., Yokoyama Y., Nagahara T., and Iwamoto M. Thromb. Hemost. 71 (1994) 314
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31
-
-
0037207123
-
-
A detailed discussion of the crystal structure of compound 31 bound to fXa is described elsewhere pdb code 1MQ5
-
A detailed discussion of the crystal structure of compound 31 bound to fXa is described elsewhere. Adler M., Kochanny M.J., Ye B., Rumennik G., Light D.R., Biancalana S., and Whitlow M. Biochemistry 41 (2002) 15514 pdb code 1MQ5
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0037468471
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See Ref. 13b and the following:
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See Ref. 13b and the following:. Maignan S., Guilloteau J.P., Choi-Sledeski Y.M., Becker M.R., Ewing W.R., Pauls H.W., Spada A.P., and Mikol V. J. Med. Chem. 46 (2003) 685
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33644814132
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For another reference to intramolecular hydrogen bonding between a chlorine and an amide NH, please see the following paper
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For another reference to intramolecular hydrogen bonding between a chlorine and an amide NH, please see the following paper. Mollendal H., and Samdal S. J. Phys. Chem. A 110 (2006) 2139
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