1,4-azaindole, A potential drug candidate for treatment of tuberculosis

Antimicrobial Agents and Chemotherapy

Volumn 58, Issue 9, 2014, Pages 5325-5331

  Chatterji, Monalisa ^a   Shandil, Radha ^a   Manjunatha, M R ^a   Solapure, Suresh ^a   Ramachandran, Vasanthi ^a   Kumar, Naveen ^a   Saralaya, Ramanatha ^a   Panduga, Vijender ^a   Reddy, Jitendar ^a   Prabhakar, K R ^a   Sharma, Sreevalli ^a   Sadler, Claire ^a   Cooper, Christopher B ^b   Mdluli, Khisi ^b   Iyer, Pravin S ^a   Narayanan, Shridhar ^a   Shirude, Pravin S ^a  

^a ASTRAZENECA   (United Kingdom)

^b GLOBAL ALLIANCE FOR TB DRUG DEVELOPMENT   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 [(6 (DIMETHYLAMINO) 5 METHYLPYRIMIDIN 4 YL)METHYL] N (2 HYDROXYETHYL) 6 METHYL 1H PYRROLO[3,2 B]PYRIDINE 3 CARBOXAMIDE; 1,4 AZAINDOLE; BEDAQUILINE; N (2 HYDROXYETHYL) 1 [(6 METHOXY 5 METHYLPYRIMIDIN 4 YL)METHYL] 6 METHYL 1H PYRROLO [3,2B]PYRIDINE 3 CARBOXAMIDE; PRETOMANID; TUBERCULOSTATIC AGENT; UNCLASSIFIED DRUG; INDOLE DERIVATIVE; PYRIDINE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DRUG EFFICACY; DRUG POTENTIATION; ENZYME INHIBITION; EXTENSIVELY DRUG RESISTANT TUBERCULOSIS; FEMALE; IN VITRO STUDY; IN VIVO STUDY; MALE; MOUSE; MULTIDRUG RESISTANT TUBERCULOSIS; MYCOBACTERIUM TUBERCULOSIS; NONHUMAN; PHYSICAL CHEMISTRY; PREDICTION; PRIORITY JOURNAL; RAT; ANIMAL; BAGG ALBINO MOUSE; DOG; DRUG COMBINATION; HUMAN; SYNTHESIS; TUBERCULOSIS, PULMONARY;

ANIMALS; ANTITUBERCULAR AGENTS; DOGS; DRUG THERAPY, COMBINATION; FEMALE; HUMANS; INDOLES; MALE; MICE; MICE, INBRED BALB C; PYRIDINES; RATS; TUBERCULOSIS, PULMONARY;

EID: 84906091763     PISSN: 00664804     EISSN: 10986596     Source Type: Journal    
DOI: 10.1128/AAC.03233-14     Document Type: Article

References (17)

1. Warner DF, Mizrahi V. 2013. Complex genetics of drug resistance in Mycobacterium tuberculosis. Nat. Genet. 45:1107-1108. http://dx.doi.org/10.1038/ ng.2769.
2. World Health Organization. 2013. Global tuberculosis report. World Health Organization, Geneva, Switzerland. http://www.who.int/iris/bitstream/10665/ 91355/1/9789241564656-eng.pdf?ua=1.
3. Raviglione M, Marais B, Floyd K, Lönnroth K, Getahun H, Migliori GB, Harries AD, Nunn P, Lienhardt C, Graham S, Chakaya J, Weyer K, Cole S, Kaufmann SH, Zumla A. 2012. Scaling up interventions to achieve global tuberculosis control: progress and new developments. Lancet 379:1902-1913. http://dx.doi.org/10.1016/S0140-6736(12)60727-2.
4. Lienhardta C, Vernonb A, Raviglionec MC. 2010. New drugs and new regimens for the treatment of tuberculosis: review of the drug development pipeline and implications for national programmes. Curr. Opin. Pulm. Med. 16:186-193. http://dx.doi.org/10.1097/MCP.0b013e328337580c.
5. Hett EC, Rubin EJ. 2008. Bacterial growth and cell division: a mycobacterial perspective. Microbiol. Mol. Biol. Rev. 72:126-156. http://dx.doi.org/10.1128/MMBR.00028-07. (Pubitemid 351398058)
6. Lu H, Tonge PJ. 2008. Inhibitors of FabI, an enzyme drug target in the bacterial fatty acid biosynthesis pathway. Acc. Chem. Res. 41:11-20. http://dx.doi.org/10.1021/ar700156e.
7. Jackson M, McNeil MR, Brennan PJ. 2013. Progress in targeting cell envelope biogenesis in Mycobacterium tuberculosis. Future Microbiol. 8:855-875. http://dx.doi.org/10.2217/fmb.13.52.
8. Mikušová K, Huang H, Yagi T, Holsters M, Vereecke D, D'Haeze W, Scherman MS, Brennan PJ, McNeil MR, Crick DC. 2005. Decaprenylphosphoryl arabinofuranose, the donor of the D-arabinofuranosyl residues of mycobacterial arabinan, is formed via a two step epimerization of decaprenylphosphoryl ribose. J. Bacteriol. 187:8020-8025. http://dx.doi.org/10. 1128/JB.187.23.8020-8025.2005. (Pubitemid 41691695)
9. Makarov V, Manina G, Mikusova K, Möllmann U, Ryabova O, Saint-Joanis B, Dhar N, Pasca MR, Buroni S, Lucarelli AP, Milano A, De Rossi E, Belanova M, Bobovska A, Dianiskova P, Kordulakova J, Sala C, Fullam E, Schneider P, McKinney JD, Brodin P, Christophe T, Waddell S, Butcher P, Albrethsen J, Rosenkrands I, Brosch R, Nandi V, Bharath S, Gaonkar S, Shandil RK, Balasubramanian V, Balganesh T, Tyagi S, Grosset J, Riccardi G, Cole ST. 2009. Benzothiazinones kill Mycobacterium tuberculosis by blocking arabinan synthesis. Science 324:801-804. http://dx.doi.org/10.1126/science.1171583.
10. Wang F, Sambandan D, Halder R, Wang J, Batt SM, Weinrick B, Ahmad I, Yang P, Zhang Y, Kim J, Hassani M, Huszar S, Trefzer C, Ma Z, Kaneko T, Mdluli KE, Franzblau S, Chatterjee AK, Johnsson K, Mikusova K, Besra GS, Fütterer K, Robbins SH, Barnes SW, Walker JR, Jacobs WR, Jr, Schultz PG. 2013. Identification of a small molecule with activity against drug-resistant and persistent tuberculosis. Proc. Natl. Acad. Sci. U. S. A. 110:E2510-E2517. http://dx.doi.org/10.1073/pnas.1309171110.
11. 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. 2013. Azaindoles: noncovalent DprE1 inhibitors from scaffold morphing efforts, kill Mycobacterium tuberculosis and are efficacious in vivo. J. Med. Chem. 56:9701-9708. http://dx.doi.org/10.1021/jm401382v.
12. Makarov V, Lechartier B, Zhang M, Neres J, van der Sar AM, Raadsen SA, Hartkoorn RC, Ryabova OB, Vocat A, Decosterd LA, Widmer N, Buclin T, Bitter W, Andries K, Pojer F, Dyson PJ, Cole ST. 2014. Towards a new combination therapy for tuberculosis with next generation benzothiazinones. EMBO Mol. Med. 6:372-383. http://dx.doi.org/10.1002/emmm.201303575.
13. Reference deleted.
14. Solapure S, Dinesh N, Shandil R, Ramachandran V, Sharma S, Bhattacharjee D, Ganguly S, Reddy J, Ahuja V, Panduga V, Parab M, Vishwas KG, Kumar N, Balganesh M, Balasubramanian V. 2013. In vitro and in vivo efficacy of β-lactams against replicating and slowly growing/nonreplicating Mycobacterium tuberculosis. Antimicrob. Agents Chemother. 57:2506-2510. http://dx.doi.org/10.1128/AAC.00023-13.
15. Gaonkar S, Bharath S, Kumar N, Balasubramanian V, Shandil RK. 2010. Aerosol infection model of tuberculosis in Wistar rats. Int. J. Microbiol. 2010:426035. http://dx.doi.org/10.1155/2010/426035.
16. Sohlenius-Sternbeck AK, Jones C, Ferguson D, Middleton BJ, Projean D, Floby E, Bylund J, Afzelius L. 2012. Practical use of the regression offset approach for the prediction of in vivo intrinsic clearance from hepatocytes. Xenobiotica 42:841-853. http://dx.doi.org/10.3109/00498254.2012.669080.
17. Lechartier B, Hartkoorn RC, Cole ST. 2012. In vitro combination studies of benzothiazinone lead compound BTZ043 against Mycobacterium tuberculosis. Antimicrob. Agents Chemother. 56:5790-5793. http://dx.doi.org/10.1128/AAC.01476- 12.