Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Sandeep R, Ghorpade"'
Publikováno v:
RSC Medicinal Chemistry. 14:644-657
Here, we critically review anti-TB compounds of the imidazo[1,2-a]pyridine class by discussing their development based on the structure–activity relationship, mode-of-action, and various scaffold hopping strategies over the last decade.
Autor:
Vinayak Singh, Anna E. Grzegorzewicz, Stephen Fienberg, Rudolf Müller, Lutete Peguy Khonde, Olalla Sanz, Salvatore Alfonso, Beatriz Urones, Gerard Drewes, Marcus Bantscheff, Sonja Ghidelli-Disse, Thomas R. Ioerger, Bhanupriya Angala, Jiuyu Liu, Richard E. Lee, James C. Sacchettini, Inna V. Krieger, Mary Jackson, Kelly Chibale, Sandeep R. Ghorpade
Publikováno v:
ACS Infectious Diseases. 8:2315-2326
Autor:
Preshendren Govender, Rudolf Müller, Kawaljit Singh, Virsinha Reddy, Charles J. Eyermann, Stephen Fienberg, Sandeep R. Ghorpade, Lizbé Koekemoer, Alissa Myrick, Dirk Schnappinger, Curtis Engelhart, Jaclynn Meshanni, Jo Ann W. Byl, Neil Osheroff, Vinayak Singh, Kelly Chibale, Gregory S. Basarab
Publikováno v:
J Med Chem
This is the accepted manuscript version of the work published in its final form as Govender, P., Müller, R., Singh, K., Reddy, V., Eyermann, C. J., Fienberg, S., Ghorpade, S. R., Koekemoer, L., Myrick, A., Schnappinger, D., Engelhart, C., Meshanni,
Autor:
Vinayak, Singh, Anna E, Grzegorzewicz, Stephen, Fienberg, Rudolf, Müller, Lutete Peguy, Khonde, Olalla, Sanz, Salvatore, Alfonso, Beatriz, Urones, Gerard, Drewes, Marcus, Bantscheff, Sonja, Ghidelli-Disse, Thomas R, Ioerger, Bhanupriya, Angala, Jiuyu, Liu, Richard E, Lee, James C, Sacchettini, Inna V, Krieger, Mary, Jackson, Kelly, Chibale, Sandeep R, Ghorpade
Publikováno v:
ACS infectious diseases. 8(11)
Alternative mode-of-inhibition of clinically validated targets is an effective strategy for circumventing existing clinical drug resistance. Herein, we report 1,3-diarylpyrazolyl-acylsulfonamides as potent inhibitors of HadAB/BC, a 3-hydroxyl-ACP deh
Autor:
Stephen Fienberg, Gregory S. Basarab, Anne J. Lenaerts, Virsinha Reddy, Sandeep R. Ghorpade, Mathew Njoroge, Grant A. Boyle, Charles J. Eyermann, Clifton E. Barry, Timothy G. Myers, Efrem Abay, Nina Lawrence, Alissa Myrick, Helena I. Boshoff, Vinayak Singh, Lutete Peguy Khonde, Lisa M. Massoudi, Paul D. van Helden, Frederick A. Sirgel, Gregory T. Robertson, Rudolf Müller, Kelly Chibale, Aloysius T. Nchinda, Qin Su
Publikováno v:
Journal of Medicinal Chemistry. 64:12790-12807
Phenotypic whole cell high-throughput screening of a ∼150,000 diverse set of compounds against Mycobacterium tuberculosis (Mtb) in cholesterol-containing media identified 1,3-diarylpyrazolyl-acylsulfonamide 1 as a moderately active hit. Structure-a
Autor:
Lutete Peguy, Khonde, Rudolf, Müller, Grant A, Boyle, Virsinha, Reddy, Aloysius T, Nchinda, Charles J, Eyermann, Stephen, Fienberg, Vinayak, Singh, Alissa, Myrick, Efrem, Abay, Mathew, Njoroge, Nina, Lawrence, Qin, Su, Timothy G, Myers, Helena I M, Boshoff, Clifton E, Barry, Frederick A, Sirgel, Paul D, van Helden, Lisa M, Massoudi, Gregory T, Robertson, Anne J, Lenaerts, Gregory S, Basarab, Sandeep R, Ghorpade, Kelly, Chibale
Publikováno v:
Journal of medicinal chemistry. 64(17)
Phenotypic whole cell high-throughput screening of a ∼150,000 diverse set of compounds against
Autor:
Kirsteen I. Buchanan, Clifton E. Barry, Simon Green, Gregory S. Basarab, Qin Su, Charles J. Eyermann, Curtis A. Engelhart, Anuradha Kumar, Paul D. van Helden, Frederick A. Sirgel, Paul G. Wyatt, Nina Lawrence, Sandeep R. Ghorpade, Dirk Schnappinger, Dale Taylor, Sandile B. Simelane, Helena I. Boshoff, Christel Brunschwig, Vinayak Singh, Kelly Chibale, Peter C. Ray, Tracy Bayliss, Candice Soares de Melo, Alissa Myrick, Tanya Parish, Timothy G. Myers
Publikováno v:
Journal of Medicinal Chemistry
Phenotypic screening of a Medicines for Malaria Venture compound library against Mycobacterium tuberculosis (Mtb) identified a cluster of pan-active 2-pyrazolylpyrimidinones. The biology triage of these actives using various tool strains of Mtb sugge
Autor:
P. Ann Boriack-Sjodin, B. K. Kishore Reddy, Ramesh R. Kale, Vijaykamal Ahuja, Sunita M. de Sousa, Krishnan Malolanarasimhan, Sheshagiri Gaonkar, Anandkumar Raichurkar, Sreenivasaiah Menasinakai, Halesha D. Basavarajappa, Prashanti Madhavapeddi, M. R. Manjunatha, Shahul Hameed, David Waterson, Radha Nandishaiah, Vasan K. Sambandamurthy, C. N. Naveen Kumar, Derek Ogg, Vikas Shinde, Vaishali Humnabadkar, Krishna Koushik, Sreevalli Sharma, K. N. Mahesh Kumar, Sandeep R. Ghorpade, Kale Manoj Ganpat, Samit Ganguly, Lalit kumar Jena
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:870-879
Scaffold hopping from the thiazolopyridine ureas led to thiazolopyridone ureas with potent antitubercular activity acting through inhibition of DNA GyrB ATPase activity. Structural diversity was introduced, by extension of substituents from the thiaz
Autor:
Vladimir Bartus, Gregory R. Cook, Viera Lukacova, Xiaomin Jin, Mukund P. Sibi, Shankar Manyem, Sandeep R. Ghorpade, Yufen Zhang, Ethirajan Manivannan, Xiaoping Nie, Guorong Sun, Stefan Balaz
Publikováno v:
Chemical Biology & Drug Design. 72:237-248
Binding to the extracellular matrix, one of the most abundant human protein complexes, significantly affects drug disposition. Specifically, the interactions with extracellular matrix determine the free concentrations of small molecules acting in tis
Autor:
Monalisa Chatterji, João Neres, Sreevalli Sharma, Prashanti Madhavapeddi, Vijender Panduga, James D. Whiteaker, Suresh Rudrapatna, Chandan Narayan, Krishna Koushik, Laurent R. Chiarelli, Gajanan Shanbhag, Vaishali Humnabadkar, Gopinath Gorai, Claudia Binda, Sandeep R. Ghorpade, Radha Shandil, Neeraj Dhar, Maria Rosalia Pasca, Stefan Kavanagh, Vasan K. Sambandamurthy, M. R. Manjunatha, K.R. Prabhakar, Vijayashree Achar, John D. McKinney, Neela Dinesh, Naina Hegde, Praveena Manjrekar, François Signorino-Gelo, Parvinder Kaur, Shridhar Narayanan, Jitendar Reddy, Subramanyam J. Tantry, Ashwini Narayan, Sandesh Jatheendranath, Lalit kumar Jena, Tommasi Ruben A, Jyothi Mahadevaswamy, Disha Awasthy, Ramanatha Saralaya, Manoranjan Panda, Bob McLaughlin, Anisha Ambady, Vinayak Hosagrahara, Pravin Iyer, Chandramohan Bathula, Maruti Naik, Giovanna Riccardi, Supreeth Guptha, Sudha Ravishankar, Vasanthi Ramachandran
Publikováno v:
Journal of medicinal chemistry. 57(12)
4-Aminoquinolone piperidine amides (AQs) were identified as a novel scaffold starting from a whole cell screen, with potent cidality on Mycobacterium tuberculosis (Mtb). Evaluation of the minimum inhibitory concentrations, followed by whole genome se