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TETRAMETHOPRIM and PENTAMETHOPRIM: Synthesis, Antibacterial Properties and X-Ray Structures

✍ Scribed by Arnold Brossi; Padam N. Sharma; Kimio Takahashi; Joseph F. Chiang; Isabella L. Karle; Gerhard Seibert

Publisher
John Wiley and Sons
Year
1983
Tongue
German
Weight
384 KB
Volume
66
Category
Article
ISSN
0018-019X

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✦ Synopsis

Abstract

TETRAMETHOPRIM (9) and PENTAMETHOPRIM (10), both prepared from the corresponding benzaldehydes 3 and 6 by conventional procedures, did not exhibit noteworthy antibacterial activity in vitro. A single crystal X‐ray analysis of 9 and 10 provided evidence that the out‐of‐plane methoxy groups in the two compounds created a completely different topographical situation to that present in TRIMETHOPRIM, and less ideal for the binding to bacterial dihydrofolate reductase.

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