Search Results - "Gowravaram, Madhusudhan"

Potent and selective inhibitors of Helicobacter pylori glutamate racemase (MurI): Pyridodiazepine amines by Geng, Bolin, Basarab, Gregory, Comita-Prevoir, Janelle, Gowravaram, Madhusudhan, Hill, Pamela, Kiely, Andrew, Loch, James, MacPherson, Lawrence, Morningstar, Marshall, Mullen, George, Osimboni, Ekundayo, Satz, Alexander, Eyermann, Charles, Lundqvist, Tomas

“…An SAR study of a screening hit generated a series of pyridodiazepine amines as inhibitors of Helicobacter pylori glutamate racemase (MurI) showing highly…”
Get full text

Antibacterial Spiropyrimidinetriones with N‑Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase by Basarab, Gregory S, Doig, Peter, Eyermann, Charles J, Galullo, Vincent, Kern, Gunther, Kimzey, Amy, Kutschke, Amy, Morningstar, Marshall, Schuck, Virna, Vishwanathan, Karthick, Zhou, Fei, Gowravaram, Madhusudhan, Hauck, Sheila

“…Herein, we report spiropyrimidinetriones (SPTs) incorporating N-linked azole substituents on a benzisoxazole scaffold with improved Gram-positive antibacterial…”
Get full text

Discovery of Novel DNA Gyrase Inhibiting Spiropyrimidinetriones: Benzisoxazole Fusion with N‑Linked Oxazolidinone Substituents Leading to a Clinical Candidate (ETX0914) by Basarab, Gregory S, Doig, Peter, Galullo, Vincent, Kern, Gunther, Kimzey, Amy, Kutschke, Amy, Newman, Joseph P, Morningstar, Marshall, Mueller, John, Otterson, Linda, Vishwanathan, Karthick, Zhou, Fei, Gowravaram, Madhusudhan

“…A novel class of bacterial type-II topoisomerase inhibitor displaying a spiropyrimidinetrione architecture fused to a benzisoxazole scaffold shows potent…”
Get full text

Responding to the challenge of untreatable gonorrhea: ETX0914, a first-in-class agent with a distinct mechanism-of-action against bacterial Type II topoisomerases by Basarab, Gregory S., Kern, Gunther H., McNulty, John, Mueller, John P., Lawrence, Kenneth, Vishwanathan, Karthick, Alm, Richard A., Barvian, Kevin, Doig, Peter, Galullo, Vincent, Gardner, Humphrey, Gowravaram, Madhusudhan, Huband, Michael, Kimzey, Amy, Morningstar, Marshall, Kutschke, Amy, Lahiri, Sushmita D., Perros, Manos, Singh, Renu, Schuck, Virna J. A., Tommasi, Ruben, Walkup, Grant, Newman, Joseph V.

“…With the diminishing effectiveness of current antibacterial therapies, it is critically important to discover agents that operate by a mechanism that…”
Get full text

Inhibition of Matrix Metalloproteinases by Hydroxamates Containing Heteroatom-Based Modifications of the P1' Group by Gowravaram, Madhusudhan R, Johnson, Jeffrey S, Delecki, Daniel, Cook, Ewell R, Tomczuk, Bruce E, Ghose, Arup K, Mathiowetz, Alan M, Spurlino, John C, Rubin, Byron, Smith, Douglas L, Pulvino, Tricia, Wahl, Robert C

“…In this study, structure-based drug design of matrix metalloproteinase inhibitors [human fibroblast collagenase (HFC), human fibroblast stromelysin (HFS), and…”
Get full text

Novel DNA Gyrase Inhibiting Spiropyrimidinetriones with a Benzisoxazole Scaffold: SAR and in Vivo Characterization by Basarab, Gregory S, Brassil, Patrick, Doig, Peter, Galullo, Vincent, Haimes, Howard B, Kern, Gunther, Kutschke, Amy, McNulty, John, Schuck, Virna J. A, Stone, Gregory, Gowravaram, Madhusudhan

“…The compounds described herein with a spirocyclic architecture fused to a benzisoxazole ring represent a new class of antibacterial agents that operate by…”
Get full text

Determination of Pharmacophoric Geometry for Collagenase Inhibitors Using a Novel Computational Method and Its Verification Using Molecular Dynamics, NMR, and X-ray Crystallography by Ghose, Arup K, Logan, Margaret E, Treasurywala, Adi M, Wang, Hsin, Wahl, Robert C, Tomczuk, Bruce E, Gowravaram, Madhusudhan R, Jaeger, Edward P, Wendoloski, John J

Get full text

From fragments to leads: novel bacterial NAD+-dependent DNA ligase inhibitors by Hale, Michael R., Brassington, Claire, Carcanague, Dan, Embrey, Kevin, Eyermann, Charles J., Giacobbe, Robert A., Gingipalli, Lakshmaiah, Gowravaram, Madhusudhan, Harang, Jenna, Howard, Tina, Ioannidis, Georgine, Jahic, Haris, Kutschke, Amy, Laganas, Valerie A., Loch, James, Miller, Matthew D., Murphy-Benenato, Kerry E., Oguto, Herbert, Otterbein, Ludovic, Patel, Sahil Joe, Shapiro, Adam B., Boriack-Sjodin, P. Ann

“…[Display omitted] Bacterial NAD+-dependent DNA ligase (LigA) is an essential enzyme involved in the repair, replication, and recombination of DNA in all…”
Get full text

Discovery of bacterial NAD +-dependent DNA ligase inhibitors: Optimization of antibacterial activity by Stokes, Suzanne S., Huynh, Hoan, Gowravaram, Madhusudhan, Albert, Robert, Cavero-Tomas, Marta, Chen, Brendan, Harang, Jenna, Loch, James T., Lu, Min, Mullen, George B., Zhao, Shannon, Liu, Ce-Feng, Mills, Scott D.

“…Optimization of adenosine analog inhibitors of bacterial NAD +-dependent DNA ligase is discussed. Antibacterial activity against Streptococcus pneumoniae and…”
Get full text

Discovery of bacterial NAD+-dependent DNA ligase inhibitors: Improvements in clearance of adenosine series by Stokes, Suzanne S., Gowravaram, Madhusudhan, Huynh, Hoan, Lu, Min, Mullen, George B., Chen, Brendan, Albert, Robert, O’Shea, Thomas J., Rooney, Michael T., Hu, Haiqing, Newman, Joseph V., Mills, Scott D.

“…Optimization of clearance of adenosine inhibitors of bacterial NAD+-dependent DNA ligase is discussed. To reduce Cytochrome P-450-mediated metabolic clearance,…”
Get full text

Correction: Corrigendum: Responding to the challenge of untreatable gonorrhea: ETX0914, a first-in-class agent with a distinct mechanism-of-action against bacterial Type II topoisomerases by Basarab, Gregory S., Kern, Gunther H., McNulty, John, Mueller, John P., Lawrence, Kenneth, Vishwanathan, Karthick, Alm, Richard A., Barvian, Kevin, Doig, Peter, Galullo, Vincent, Gardner, Humphrey, Gowravaram, Madhusudhan, Huband, Michael, Kimzey, Amy, Morningstar, Marshall, Kutschke, Amy, Lahiri, Sushmita D., Perros, Manos, Singh, Renu, Schuck, Virna J. A., Tommasi, Ruben, Walkup, Grant, Newman, Joseph V.

“…With the diminishing effectiveness of current antibacterial therapies, it is critically important to discover agents that operate by a mechanism that…”
Get full text

Discovery of bacterial NAD super(+-dependent DNA ligase inhibitors: Optimization of antibacterial activity) by Stokes, Suzanne S, Huynh, Hoan, Gowravaram, Madhusudhan, Albert, Robert, Cavero-Tomas, Marta, Chen, Brendan, Harang, Jenna, Loch, James T, Lu, Min, Mullen, George B, Zhao, Shannon, Liu, Ce-Feng, Mills, Scott D

“…Optimization of adenosine analog inhibitors of bacterial NAD super(+-dependent DNA ligase is discussed. Antibacterial activity against Streptococcus pneumoniae…”
Get full text

“Traceless” solid-phase synthesis of furans via 1,3-dipolar cycloaddition reactions of isomünchnones by Gowravaram, Madhusudhan R., Gallop, Mark A.

“…The generation and cycloaddition reactions of polymer-supported mesoionic isomünchnones derived from α-diazocarbonyl intermediates is described in this report…”
Get full text

Corrigendum: Responding to the challenge of untreatable gonorrhea: ETX0914, a first-in-class agent with a distinct mechanism-of-action against bacterial Type II topoisomerases by Basarab, Gregory S, Kern, Gunther H, McNulty, John, Mueller, John P, Lawrence, Kenneth, Vishwanathan, Karthick, Alm, Richard A, Barvian, Kevin, Doig, Peter, Galullo, Vincent, Gardner, Humphrey, Gowravaram, Madhusudhan, Huband, Michael, Kimzey, Amy, Morningstar, Marshall, Kutschke, Amy, Lahiri, Sushmita D, Perros, Manos, Singh, Renu, Schuck, Virna J A, Tommasi, Ruben, Walkup, Grant, Newman, Joseph V

Get full text

Hydroxamate inhibitors of the matrix metallo-proteinases (MMPs) containing novel P1′ heteroatom based modifications by Tomczuk, Bruce E., Gowravaram, Madhusudhan R., Johnson, Jeffrey S., Delecki, Daniel, Cook, Ewell R., Ghose, Arup K., Mathiowetz, Alan M., Spurlino, John C., Rubin, Byron, Smith, Douglas L., Pulvino, Tricia, Wahl, Robert C.

Get full text

Hydroxamate inhibitors of human gelatinase B (92 kDa) by Wahl, Robert C., Pulvino, Tricia A., Mathiowetz, Alan M., Ghose, Arup K., Johnson, Jeffrey S., Delecki, Daniel, Cook, Ewell R., Gainor, James A., Gowravaram, Madhusudhan R., Tomczuk, Bruce E.

“…Gelatinase B is potently inhibited by peptide hydroxamates, including molecules that have a R 1′ group which is larger than the side chains of the natural…”
Get full text

Hydroxamate inhibitors of the matrix metallo-proteinases (MMPs) containing novel P 1′ heteroatom based modifications by Tomczuk, Bruce E., Gowravaram, Madhusudhan R., Johnson, Jeffrey S., Delecki, Daniel, Cook, Ewell R., Ghose, Arup K., Mathiowetz, Alan M., Spurlino, John C., Rubin, Byron, Smith, Douglas L., Pulvino, Tricia, Wahl, Robert C.

“…Structure-based drug design (SBDD) and traditional SAR have guided the development of potent and selective hydroxamate inhibitors which contain…”
Get full text