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Full-Text Articles in Physical Sciences and Mathematics
Inhibition Of Aminoglycoside 6’-N-Acetyltransferase Type Ib [Aac(6′)-Ib]: Structure-Activity Relationship Of Substituted Pyrrolidine Pentamine Derivatives As Inhibitors, Kenneth Rocha, Jesus Magallon, Craig Reeves, Kimberly Phan, Peter Vu, Crista L. Oakley-Havens, Stella Kwan, Maria S. Ramirez, Travis Lavoi, Haley Donow, Prem Chapagain, Radleigh Santos, Clemencia Pinilla, Marc A. Giulianotti, Marcelo E. Tolmasky
Inhibition Of Aminoglycoside 6’-N-Acetyltransferase Type Ib [Aac(6′)-Ib]: Structure-Activity Relationship Of Substituted Pyrrolidine Pentamine Derivatives As Inhibitors, Kenneth Rocha, Jesus Magallon, Craig Reeves, Kimberly Phan, Peter Vu, Crista L. Oakley-Havens, Stella Kwan, Maria S. Ramirez, Travis Lavoi, Haley Donow, Prem Chapagain, Radleigh Santos, Clemencia Pinilla, Marc A. Giulianotti, Marcelo E. Tolmasky
Mathematics Faculty Articles
The aminoglycoside 6′-N-acetyltransferase type Ib [AAC(6′)-Ib] is a common cause of resistance to amikacin and other aminoglycosides in Gram-negatives. Utilization of mixture-based combinatorial libraries and application of the positional scanning strategy identified an inhibitor of AAC(6′)-Ib. This inhibitor’s chemical structure consists of a pyrrolidine pentamine scaffold substituted at four locations (R1, R3, R4, and R5). The substituents are two S-phenyl (R1 and R4), an S-hydroxymethyl (R3), and a 3-phenylbutyl (R5) groups. Another location, R2, does not have a substitution, but it is named because its stereochemistry was modified in some compounds utilized in this study. Structure-activity …