Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Vaishali Humnabadkar"'
Autor:
Vaishali Humnabadkar, Claire Sadler, Tanjore S. Balganesh, Prakash Vachaspati, Disha Awasthy, Manoranjan Panda, Mick D. Fellows, Parvinder Kaur, Stewart T. Cole, Florence Pojer, Vasan K. Sambandamurthy, João Neres, Sreevalli Sharma, V. Balasubramanian, Kannan Murugan, Meenakshi Mallya, Suresh Rudrapatna, Balachandra Bandodkar, Sudhir Landge, Bheemarao G. Ugarkar, Jyothi Mahadevaswamy, Kavitha Nagalapur, Amrita B. Mullick, Vasanthi Ramachandran, Anirban Ghosh, Venkita Subbulakshmi
Publikováno v:
Bioorganic & Medicinal Chemistry. 23:7694-7710
We report the discovery of benzothiazoles, a novel anti-mycobacterial series, identified from a whole cell based screening campaign. Benzothiazoles exert their bactericidal activity against Mycobacterium tuberculosis (Mtb) through potent inhibition o
Autor:
Sunita M. de Sousa, Prashanti Madhavapeddi, Aishwarya Sundaram, Md. Gulebahar Sheikh, Kakoli Mukherjee, Reetobrata Basu, Vaishali Humnabadkar, Rajendra Rane, Halesha D. Basavarajappa, Prateek Verma
Publikováno v:
SLAS Discovery. 20:265-274
Mycobacterium tuberculosis (Mtb) DNA gyrase ATPase was the target of a tuberculosis drug discovery program. The low specific activity of the Mtb ATPase prompted the use of Mycobacterium smegmatis (Msm) enzyme as a surrogate for lead generation, since
Autor:
Sreevalli Sharma, Monalisa Chatterji, Ashwini Narayan, Sudha Ravishankar, Vasanthi Ramachandran, Vaishali Humnabadkar, Supreeth Guptha, Shahul Hameed, Praveena Manjrekar, Murugan Chinnapattu, K.R. Prabhakar
Publikováno v:
Antimicrobial Agents and Chemotherapy. 58:6165-6171
The Mur ligases play an essential role in the biosynthesis of bacterial peptidoglycan and hence are attractive antibacterial targets. A screen of the AstraZeneca compound library led to the identification of compound A, a pyrazolopyrimidine, as a pot
Autor:
V. K. Ramya, Vijender Panduga, Gajanan Shanbhag, Michelle Coulson, Sowmya Bharath, Vaishali Humnabadkar, Prashanti Madhavapeddi, Vasan K. Sambandamurthy, Disha Awasthy, Jim Werngren, Praveena Manjrekar, Chandan Narayan, Vijayashree Achar, Mahesh Kumar Kn, Sunita M. de Sousa, Jitendar Reddy, C. N. Naveen Kumar, Kakoli Mukherjee, Sreenivasaiah Menasinakai, Ugarkar Bheemarao, Samit Ganguly, Umender Sharma, David Waterson, Vikas Patil, Sven Hoffner, Radha Nandishaiah, Sreevalli Sharma, Shahul Hameed P, Uma Arora, Anandkumar Raichurkar, Suresh Solapure, Parvinder Kaur, Jayashree Puttur, Vikas Shinde, Murugan Chinnapattu, Suresh Rudrapatana, Sheshagiri Gaonkar, Anirban Ghosh
Publikováno v:
Journal of Medicinal Chemistry. 57:4889-4905
DNA gyrase is a clinically validated target for developing drugs against Mycobacterium tuberculosis (Mtb). Despite the promise of fluoroquinolones (FQs) as anti-tuberculosis drugs, the prevalence of pre-existing resistance to FQs is likely to restric
Autor:
Parvinder Kaur, Anisha Ambady, Sreevalli Sharma, Vinayak Hosagrahara, Ashwini Narayan, Vasanthi Ramachandran, Suresh Rudrapatna, Supreeth Guptha, Pravin S. Shirude, Vasan K. Sambandamurthy, Jyothi Mahadevaswamy, Ramachandran Sreekanth A, Kavitha Nagalapur, Anandkumar Raichurkar, Naina Hegde, Manoranjan Panda, Vaishali Humnabadkar
Publikováno v:
Journal of Medicinal Chemistry. 57:4761-4771
A novel pyrazolopyridone class of inhibitors was identified from whole cell screening against Mycobacterium tuberculosis (Mtb). The series exhibits excellent bactericidality in vitro, resulting in a 4 log reduction in colony forming units following c
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
Publikováno v:
SLAS Discovery. 16:303-312
1-deoxy-D-xylulose 5-phosphate reductoisomerase (Dxr) is involved in the synthesis of isoprenoids by the methylerythritol phosphate pathway. Dxr is essential in Mycobacterium tuberculosis (Mtu), absent in humans and amenable to structure-aided design
Autor:
Ekaterina Gelman, V. Balasubramanian, Sreevalli Sharma, Vijayashree Achar, Neeraj Dhar, Vasanthi Ramachandran, Chandan Narayan, Neela Dinesh, Vaishali Humnabadkar, D. Bhattacharjee
Publikováno v:
Antimicrobial agents and chemotherapy. 58(10)
A major obstacle in the process of discovery of drugs against Mycobacterium tuberculosis is its extremely slow growth rate and long generation time (∼20 to 24 h). Consequently, determination of MICs and minimum bactericidal concentrations (MBCs) of
Autor:
Claire Sadler, Shubha Sriram, Naina Vinay Mudugal, Boudewijn L. M. de Jonge, Gajanan Shanbhag, David C. McKinney, Praveena Manjrekar, Paul Robert Fleming, Beena Paul, Charles J. Eyermann, Vasan K. Sambandamurthy, Anisha Ambady, Sudha Ravishankar, Parvinder Kaur, Murugan Chinnapattu, Anandkumar Raichurkar, Shahul Hameed P, Chaitanyakumar Kedari, Supreeth Guptha, Manoranjan Panda, Vaishali Humnabadkar
Publikováno v:
ACS chemical biology. 9(10)
The bacterial peptidoglycan biosynthesis pathway provides multiple targets for antibacterials, as proven by the clinical success of β-lactam and glycopeptide classes of antibiotics. The Mur ligases play an essential role in the biosynthesis of the p
Autor:
Vijender Panduga, Robert Nanduri, Pravin Iyer, Manoranjan Panda, Lalit kumar Jena, Claire Sadler, Anisha Ambady, Sudha Ravishankar, Rudrapatna S. Suresh, M. R. Manjunatha, Shridhar Narayanan, K.R. Prabhakar, Khisi Mdluli, Sreevalli Sharma, James D. Whiteaker, Scott Butler, Pravin S. Shirude, Radha Shandil, Vaishali Humnabadkar, Monalisa Chatterji, Abhishek Srivastava, Ramanatha Saralaya, Jitendar Reddy, Robert E. McLaughlin, Christopher B. Cooper, Vasan K. Sambandamurthy
Publikováno v:
Journal of medicinal chemistry. 57(13)
In a previous report, we described the discovery of 1,4-azaindoles, a chemical series with excellent in vitro and in vivo antimycobacterial potency through noncovalent inhibition of decaprenylphosphoryl-β-d-ribose-2'-epimerase (DprE1). Nevertheless,