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Items: 15

1.

Discovery of cofactor-specific, bactericidal Mycobacterium tuberculosis InhA inhibitors using DNA-encoded library technology.

Soutter HH, Centrella P, Clark MA, Cuozzo JW, Dumelin CE, Guie MA, Habeshian S, Keefe AD, Kennedy KM, Sigel EA, Troast DM, Zhang Y, Ferguson AD, Davies G, Stead ER, Breed J, Madhavapeddi P, Read JA.

Proc Natl Acad Sci U S A. 2016 Dec 6;113(49):E7880-E7889. Epub 2016 Nov 18.

2.

Left-Hand Side Exploration of Novel Bacterial Topoisomerase Inhibitors to Improve Selectivity against hERG Binding.

Hameed P S, Manjrekar P, Raichurkar A, Shinde V, Puttur J, Shanbhag G, Chinnapattu M, Patil V, Rudrapatana S, Sharma S, Kumar CN, Nandishaiah R, Madhavapeddi P, Sriram D, Solapure S, Sambandamurthy VK.

ACS Med Chem Lett. 2015 May 22;6(7):741-6. doi: 10.1021/ml500531p. eCollection 2015 Jul 9.

3.

Assays, surrogates, and alternative technologies for a TB lead identification program targeting DNA gyrase ATPase.

Humnabadkar V, Madhavapeddi P, Basavarajappa H, Sheikh MG, Rane R, Basu R, Verma P, Sundaram A, Mukherjee K, de Sousa SM.

J Biomol Screen. 2015 Feb;20(2):265-74. doi: 10.1177/1087057114554170. Epub 2014 Oct 9.

PMID:
25300873
4.

Benzimidazoles: novel mycobacterial gyrase inhibitors from scaffold morphing.

Hameed P S, Raichurkar A, Madhavapeddi P, Menasinakai S, Sharma S, Kaur P, Nandishaiah R, Panduga V, Reddy J, Sambandamurthy VK, Sriram D.

ACS Med Chem Lett. 2014 Jun 2;5(7):820-5. doi: 10.1021/ml5001728. eCollection 2014 Jul 10.

5.

4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.

Naik M, Humnabadkar V, Tantry SJ, Panda M, Narayan A, Guptha S, Panduga V, Manjrekar P, Jena LK, Koushik K, Shanbhag G, Jatheendranath S, Manjunatha MR, Gorai G, Bathula C, Rudrapatna S, Achar V, Sharma S, Ambady A, Hegde N, Mahadevaswamy J, Kaur P, Sambandamurthy VK, Awasthy D, Narayan C, Ravishankar S, Madhavapeddi P, Reddy J, Prabhakar K, Saralaya R, Chatterji M, Whiteaker J, McLaughlin B, Chiarelli LR, Riccardi G, Pasca MR, Binda C, Neres J, Dhar N, Signorino-Gelo F, McKinney JD, Ramachandran V, Shandil R, Tommasi R, Iyer PS, Narayanan S, Hosagrahara V, Kavanagh S, Dinesh N, Ghorpade SR.

J Med Chem. 2014 Jun 26;57(12):5419-34. doi: 10.1021/jm5005978. Epub 2014 Jun 11.

PMID:
24871036
6.

Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.

Hameed P S, Patil V, Solapure S, Sharma U, Madhavapeddi P, Raichurkar A, Chinnapattu M, Manjrekar P, Shanbhag G, Puttur J, Shinde V, Menasinakai S, Rudrapatana S, Achar V, Awasthy D, Nandishaiah R, Humnabadkar V, Ghosh A, Narayan C, Ramya VK, Kaur P, Sharma S, Werngren J, Hoffner S, Panduga V, Kumar CN, Reddy J, Kumar K N M, Ganguly S, Bharath S, Bheemarao U, Mukherjee K, Arora U, Gaonkar S, Coulson M, Waterson D, Sambandamurthy VK, de Sousa SM.

J Med Chem. 2014 Jun 12;57(11):4889-905. doi: 10.1021/jm500432n. Epub 2014 May 23.

PMID:
24809953
7.

Thiazolopyridone ureas as DNA gyrase B inhibitors: optimization of antitubercular activity and efficacy.

Kale RR, Kale MG, Waterson D, Raichurkar A, Hameed SP, Manjunatha MR, Kishore Reddy BK, Malolanarasimhan K, Shinde V, Koushik K, Jena LK, Menasinakai S, Humnabadkar V, Madhavapeddi P, Basavarajappa H, Sharma S, Nandishaiah R, Mahesh Kumar KN, Ganguly S, Ahuja V, Gaonkar S, Naveen Kumar CN, Ogg D, Boriack-Sjodin PA, Sambandamurthy VK, de Sousa SM, Ghorpade SR.

Bioorg Med Chem Lett. 2014 Feb 1;24(3):870-9. doi: 10.1016/j.bmcl.2013.12.080. Epub 2013 Dec 25.

PMID:
24405701
8.

Azaindoles: noncovalent DprE1 inhibitors from scaffold morphing efforts, kill Mycobacterium tuberculosis and are efficacious in vivo.

Shirude PS, Shandil R, Sadler C, Naik M, Hosagrahara V, Hameed S, Shinde V, Bathula C, Humnabadkar V, Kumar N, Reddy J, Panduga V, Sharma S, Ambady A, Hegde N, Whiteaker J, McLaughlin RE, Gardner H, Madhavapeddi P, Ramachandran V, Kaur P, Narayan A, Guptha S, Awasthy D, Narayan C, Mahadevaswamy J, Vishwas KG, Ahuja V, Srivastava A, Prabhakar KR, Bharath S, Kale R, Ramaiah M, Choudhury NR, Sambandamurthy VK, Solapure S, Iyer PS, Narayanan S, Chatterji M.

J Med Chem. 2013 Dec 12;56(23):9701-8. doi: 10.1021/jm401382v. Epub 2013 Nov 21.

PMID:
24215368
9.

Optimization of pyrrolamides as mycobacterial GyrB ATPase inhibitors: structure-activity relationship and in vivo efficacy in a mouse model of tuberculosis.

P SH, Solapure S, Mukherjee K, Nandi V, Waterson D, Shandil R, Balganesh M, Sambandamurthy VK, Raichurkar AK, Deshpande A, Ghosh A, Awasthy D, Shanbhag G, Sheikh G, McMiken H, Puttur J, Reddy J, Werngren J, Read J, Kumar M, R M, Chinnapattu M, Madhavapeddi P, Manjrekar P, Basu R, Gaonkar S, Sharma S, Hoffner S, Humnabadkar V, Subbulakshmi V, Panduga V.

Antimicrob Agents Chemother. 2014;58(1):61-70. doi: 10.1128/AAC.01751-13. Epub 2013 Oct 14. Erratum in: Antimicrob Agents Chemother. 2014 Aug;58(8):4993-4.

10.

Methyl-thiazoles: a novel mode of inhibition with the potential to develop novel inhibitors targeting InhA in Mycobacterium tuberculosis.

Shirude PS, Madhavapeddi P, Naik M, Murugan K, Shinde V, Nandishaiah R, Bhat J, Kumar A, Hameed S, Holdgate G, Davies G, McMiken H, Hegde N, Ambady A, Venkatraman J, Panda M, Bandodkar B, Sambandamurthy VK, Read JA.

J Med Chem. 2013 Nov 14;56(21):8533-42. doi: 10.1021/jm4012033. Epub 2013 Oct 25.

PMID:
24107081
11.

Thiazolopyridine ureas as novel antitubercular agents acting through inhibition of DNA Gyrase B.

Kale MG, Raichurkar A, P SH, Waterson D, McKinney D, Manjunatha MR, Kranthi U, Koushik K, Jena Lk, Shinde V, Rudrapatna S, Barde S, Humnabadkar V, Madhavapeddi P, Basavarajappa H, Ghosh A, Ramya VK, Guptha S, Sharma S, Vachaspati P, Kumar KN, Giridhar J, Reddy J, Panduga V, Ganguly S, Ahuja V, Gaonkar S, Kumar CN, Ogg D, Tucker JA, Boriack-Sjodin PA, de Sousa SM, Sambandamurthy VK, Ghorpade SR.

J Med Chem. 2013 Nov 14;56(21):8834-48. doi: 10.1021/jm401268f. Epub 2013 Oct 18.

PMID:
24088190
12.

Aminopyrazinamides: novel and specific GyrB inhibitors that kill replicating and nonreplicating Mycobacterium tuberculosis.

Shirude PS, Madhavapeddi P, Tucker JA, Murugan K, Patil V, Basavarajappa H, Raichurkar AV, Humnabadkar V, Hussein S, Sharma S, Ramya VK, Narayan CB, Balganesh TS, Sambandamurthy VK.

ACS Chem Biol. 2013 Mar 15;8(3):519-23. doi: 10.1021/cb300510w. Epub 2012 Dec 31.

PMID:
23268609
13.

Pre-steady-state kinetic studies on the Glu171Gln active site mutant of adenosylcobalamin-dependent glutamate mutase.

Madhavapeddi P, Ballou DP, Marsh EN.

Biochemistry. 2002 Dec 31;41(52):15803-9.

PMID:
12501209
14.

Adenosylcobalamin-dependent glutamate mutase: pre-steady-state kinetic methods for investigating reaction mechanism.

Chih HW, Roymoulik I, Huhta MS, Madhavapeddi P, Marsh EN.

Methods Enzymol. 2002;354:380-99. No abstract available.

PMID:
12418241

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