The Experts below are selected from a list of 6 Experts worldwide ranked by ideXlab platform
Michio Kurosu - One of the best experts on this subject based on the ideXlab platform.
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Novel FR-900493 Analogues That Inhibit the Outgrowth of Clostridium difficile Spores
2018Co-Authors: Katsuhiko Mitachi, Hyun Gi Yun, Sara M. Kurosu, Shakiba Eslamimehr, Maddie R. Lemieux, Lada Klaić, William M. Clemons, Michio KurosuAbstract:The spectrum of antibacterial activity for the nucleoside antibiotic FR-900493 (1) can be extended by chemical modifications. We have generated a small focused library based on the structure of 1 and identified UT-17415 (9), UT-17455 (10), UT-17460 (11), and UT-17465 (12), which exhibit anti-Clostridium difficile growth Inhibitory activity. These analogues also inhibit the outgrowth of C. difficile spores at 2× minimum Inhibitory concentration. One of these analogues, 11, relative to 1 exhibits over 180-fold and 15-fold greater activity against the enzymes, phospho-MurNAc-pentapeptide translocase (MraY) and polyprenyl phosphate-GlcNAc-1-phosphate transferase (WecA), respectively. The Phosphotransferase Inhibitor 11 displays antimicrobial activity against several tested bacteria including Bacillus subtilis, Clostridium spp., and Mycobacterium smegmatis, but no growth Inhibitory activity is observed against the other Gram-positive and Gram-negative bacteria. The selectivity index (Vero cell cytotoxicity/C. difficileantimicrobial activity) of 11 is approximately 17, and 11 does not induce hemolysis even at a 100 μM concentration
Kurosu Michio - One of the best experts on this subject based on the ideXlab platform.
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Novel FR-900493 Analogues That Inhibit the Outgrowth of Clostridium difficile Spores
'American Chemical Society (ACS)', 2018Co-Authors: Mitachi Katsuhiko, Hyun Gi Yun, Kurosu, Sara M., Eslamimehr Shakiba, Lemieux, Maddie R., Klaić Lada, Clemons, William M., Kurosu MichioAbstract:The spectrum of antibacterial activity for the nucleoside antibiotic FR-900493 (1) can be extended by chemical modifications. We have generated a small focused library based on the structure of 1 and identified UT-17415 (9), UT-17455 (10), UT-17460 (11), and UT-17465 (12), which exhibit anti-Clostridium difficile growth Inhibitory activity. These analogues also inhibit the outgrowth of C. difficile spores at 2× minimum Inhibitory concentration. One of these analogues, 11, relative to 1 exhibits over 180-fold and 15-fold greater activity against the enzymes, phospho-MurNAc-pentapeptide translocase (MraY) and polyprenyl phosphate-GlcNAc-1-phosphate transferase (WecA), respectively. The Phosphotransferase Inhibitor 11 displays antimicrobial activity against several tested bacteria including Bacillus subtilis, Clostridium spp., and Mycobacterium smegmatis, but no growth Inhibitory activity is observed against the other Gram-positive and Gram-negative bacteria. The selectivity index (Vero cell cytotoxicity/C. difficileantimicrobial activity) of 11 is approximately 17, and 11 does not induce hemolysis even at a 100 μM concentration
Hyun Gi Yun - One of the best experts on this subject based on the ideXlab platform.
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Novel FR-900493 Analogues That Inhibit the Outgrowth of Clostridium difficile Spores
'American Chemical Society (ACS)', 2018Co-Authors: Mitachi Katsuhiko, Hyun Gi Yun, Kurosu, Sara M., Eslamimehr Shakiba, Lemieux, Maddie R., Klaić Lada, Clemons, William M., Kurosu MichioAbstract:The spectrum of antibacterial activity for the nucleoside antibiotic FR-900493 (1) can be extended by chemical modifications. We have generated a small focused library based on the structure of 1 and identified UT-17415 (9), UT-17455 (10), UT-17460 (11), and UT-17465 (12), which exhibit anti-Clostridium difficile growth Inhibitory activity. These analogues also inhibit the outgrowth of C. difficile spores at 2× minimum Inhibitory concentration. One of these analogues, 11, relative to 1 exhibits over 180-fold and 15-fold greater activity against the enzymes, phospho-MurNAc-pentapeptide translocase (MraY) and polyprenyl phosphate-GlcNAc-1-phosphate transferase (WecA), respectively. The Phosphotransferase Inhibitor 11 displays antimicrobial activity against several tested bacteria including Bacillus subtilis, Clostridium spp., and Mycobacterium smegmatis, but no growth Inhibitory activity is observed against the other Gram-positive and Gram-negative bacteria. The selectivity index (Vero cell cytotoxicity/C. difficileantimicrobial activity) of 11 is approximately 17, and 11 does not induce hemolysis even at a 100 μM concentration
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Novel FR-900493 Analogues That Inhibit the Outgrowth of Clostridium difficile Spores
2018Co-Authors: Katsuhiko Mitachi, Hyun Gi Yun, Sara M. Kurosu, Shakiba Eslamimehr, Maddie R. Lemieux, Lada Klaić, William M. Clemons, Michio KurosuAbstract:The spectrum of antibacterial activity for the nucleoside antibiotic FR-900493 (1) can be extended by chemical modifications. We have generated a small focused library based on the structure of 1 and identified UT-17415 (9), UT-17455 (10), UT-17460 (11), and UT-17465 (12), which exhibit anti-Clostridium difficile growth Inhibitory activity. These analogues also inhibit the outgrowth of C. difficile spores at 2× minimum Inhibitory concentration. One of these analogues, 11, relative to 1 exhibits over 180-fold and 15-fold greater activity against the enzymes, phospho-MurNAc-pentapeptide translocase (MraY) and polyprenyl phosphate-GlcNAc-1-phosphate transferase (WecA), respectively. The Phosphotransferase Inhibitor 11 displays antimicrobial activity against several tested bacteria including Bacillus subtilis, Clostridium spp., and Mycobacterium smegmatis, but no growth Inhibitory activity is observed against the other Gram-positive and Gram-negative bacteria. The selectivity index (Vero cell cytotoxicity/C. difficileantimicrobial activity) of 11 is approximately 17, and 11 does not induce hemolysis even at a 100 μM concentration
Mitachi Katsuhiko - One of the best experts on this subject based on the ideXlab platform.
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Novel FR-900493 Analogues That Inhibit the Outgrowth of Clostridium difficile Spores
'American Chemical Society (ACS)', 2018Co-Authors: Mitachi Katsuhiko, Hyun Gi Yun, Kurosu, Sara M., Eslamimehr Shakiba, Lemieux, Maddie R., Klaić Lada, Clemons, William M., Kurosu MichioAbstract:The spectrum of antibacterial activity for the nucleoside antibiotic FR-900493 (1) can be extended by chemical modifications. We have generated a small focused library based on the structure of 1 and identified UT-17415 (9), UT-17455 (10), UT-17460 (11), and UT-17465 (12), which exhibit anti-Clostridium difficile growth Inhibitory activity. These analogues also inhibit the outgrowth of C. difficile spores at 2× minimum Inhibitory concentration. One of these analogues, 11, relative to 1 exhibits over 180-fold and 15-fold greater activity against the enzymes, phospho-MurNAc-pentapeptide translocase (MraY) and polyprenyl phosphate-GlcNAc-1-phosphate transferase (WecA), respectively. The Phosphotransferase Inhibitor 11 displays antimicrobial activity against several tested bacteria including Bacillus subtilis, Clostridium spp., and Mycobacterium smegmatis, but no growth Inhibitory activity is observed against the other Gram-positive and Gram-negative bacteria. The selectivity index (Vero cell cytotoxicity/C. difficileantimicrobial activity) of 11 is approximately 17, and 11 does not induce hemolysis even at a 100 μM concentration
Katsuhiko Mitachi - One of the best experts on this subject based on the ideXlab platform.
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Novel FR-900493 Analogues That Inhibit the Outgrowth of Clostridium difficile Spores
2018Co-Authors: Katsuhiko Mitachi, Hyun Gi Yun, Sara M. Kurosu, Shakiba Eslamimehr, Maddie R. Lemieux, Lada Klaić, William M. Clemons, Michio KurosuAbstract:The spectrum of antibacterial activity for the nucleoside antibiotic FR-900493 (1) can be extended by chemical modifications. We have generated a small focused library based on the structure of 1 and identified UT-17415 (9), UT-17455 (10), UT-17460 (11), and UT-17465 (12), which exhibit anti-Clostridium difficile growth Inhibitory activity. These analogues also inhibit the outgrowth of C. difficile spores at 2× minimum Inhibitory concentration. One of these analogues, 11, relative to 1 exhibits over 180-fold and 15-fold greater activity against the enzymes, phospho-MurNAc-pentapeptide translocase (MraY) and polyprenyl phosphate-GlcNAc-1-phosphate transferase (WecA), respectively. The Phosphotransferase Inhibitor 11 displays antimicrobial activity against several tested bacteria including Bacillus subtilis, Clostridium spp., and Mycobacterium smegmatis, but no growth Inhibitory activity is observed against the other Gram-positive and Gram-negative bacteria. The selectivity index (Vero cell cytotoxicity/C. difficileantimicrobial activity) of 11 is approximately 17, and 11 does not induce hemolysis even at a 100 μM concentration