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Product name : BM212
Item : C2493
Price : 200mg, $950;500mg, $1595; 1g, $2390; 2g, $3590
contact : Send inquiry to: info@acesobio.
CAS : 146204-42-4
Molecular Weight : 414.37
Formula : C₂₃H₂₅Cl₂N₃
Storage : at -20°C
Additional information : We offer significant discount for bulky quantity order.
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Details:
Description of:BM212
BM-212(CAS:146204-42-4) is a potent antimycobacterial agent and MmpL3 inhibitor. BM-212 was shown to possess strong inhibitory activity against both Mycobacterium tuberculosis and some nontuberculosis mycobacteria. BM212 was inhibitory to drug-resistant mycobacteria and also exerted bactericidal activity against intracellular bacilli residing in the U937 human histiocytic lymphoma cell line.

Quality control data:
Quality control by 1H-NMR, 13C-NMR, HPLC and LCMS.
Product will be shipped with supporting analytical data. 

REFERENCES

1: Bhakta S, Scalacci N, Maitra A, Brown AK, Dasugari S, Evangelopoulos D, McHugh TD, Mortazavi PN, Twist A, Petricci E, Manetti F, Castagnolo D. Design and synthesis of 1-((1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl)methyl)-4-methylpiperazine (BM212) and N-Adamantan-2-yl-N'-((E)-3,7-dimethyl-octa-2,6-dienyl)-ethane-1,2-diamine (SQ109) pyrrole hybrid derivatives: discovery of potent anti-tubercular agents effective against multi-drug resistant mycobacteria. J Med Chem. 2016 Feb 23. [Epub ahead of print] PubMed PMID: 26907951.

1: Li W, Upadhyay A, Fontes FL, North EJ, Wang Y, Crans DC, Grzegorzewicz AE, Jones V, Franzblau SG, Lee RE, Crick DC, Jackson M. Novel insights into the mechanism of inhibition of MmpL3, a target of multiple pharmacophores in Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2014 Nov;58(11):6413-23. doi: 10.1128/AAC.03229-14. Epub 2014 Aug 18. PubMed PMID: 25136022; PubMed Central PMCID: PMC4249373.

2: Poce G, Bates RH, Alfonso S, Cocozza M, Porretta GC, Ballell L, Rullas J, Ortega F, De Logu A, Agus E, La Rosa V, Pasca MR, De Rossi E, Wae B, Franzblau SG, Manetti F, Botta M, Biava M. Improved BM212 MmpL3 inhibitor analogue shows efficacy in acute murine model of tuberculosis infection. PLoS One. 2013;8(2):e56980. doi: 10.1371/journal.pone.0056980. Epub 2013 Feb 21. PubMed PMID: 23437287; PubMed Central PMCID: PMC3578785.

3: La Rosa V, Poce G, Canseco JO, Buroni S, Pasca MR, Biava M, Raju RM, Porretta GC, Alfonso S, Battilocchio C, Javid B, Sorrentino F, Ioerger TR, Sacchettini JC, Manetti F, Botta M, De Logu A, Rubin EJ, De Rossi E. MmpL3 is the cellular target of the antitubercular pyrrole derivative BM212. Antimicrob Agents Chemother. 2012 Jan;56(1):324-31. doi: 10.1128/AAC.05270-11. Epub 2011 Oct 24. PubMed PMID: 22024828; PubMed Central PMCID: PMC3256021.

4: Biava M, Porretta GC, Poce G, De Logu A, Meleddu R, De Rossi E, Manetti F, Botta M. 1,5-Diaryl-2-ethyl pyrrole derivatives as antimycobacterial agents: design, synthesis, and microbiological evaluation. Eur J Med Chem. 2009 Nov;44(11):4734-8. doi: 10.1016/j.ejmech.2009.06.005. Epub 2009 Jun 13. PubMed PMID: 19595488.

5: Biava M, Porretta GC, Poce G, De Logu A, Saddi M, Meleddu R, Manetti F, De Rossi E, Botta M. 1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings. J Med Chem. 2008 Jun 26;51(12):3644-8. doi: 10.1021/jm701560p. PubMed PMID: 18494459.

6: Biava M, Porretta GC, Manetti F. New derivatives of BM212: A class of antimycobacterial compounds based on the pyrrole ring as a scaffold. Mini Rev Med Chem. 2007 Jan;7(1):65-78. Review. PubMed PMID: 17266639.

7: Biava M, Porretta GC, Poce G, Supino S, Deidda D, Pompei R, Molicotti P, Manetti F, Botta M. Antimycobacterial agents. Novel diarylpyrrole derivatives of BM212 endowed with high activity toward Mycobacterium tuberculosis and low cytotoxicity. J Med Chem. 2006 Aug 10;49(16):4946-52. PubMed PMID: 16884306.

8: Biava M, Porretta GC, Deidda D, Pompei R. New trends in development of antimycobacterial compounds. Infect Disord Drug Targets. 2006 Jun;6(2):159-72. Review. PubMed PMID: 16789877.

9: Biava M, Porretta GC, Poce G, Deidda D, Pompei R, Tafi A, Manetti F. Antimycobacterial compounds. Optimization of the BM 212 structure, the lead compound for a new pyrrole derivative class. Bioorg Med Chem. 2005 Feb 15;13(4):1221-30. PubMed PMID: 15670931.

10: Biava M, Porretta GC, Deidda D, Pompei R, Tafi A, Manetti F. Antimycobacterial compounds. New pyrrole derivatives of BM212. Bioorg Med Chem. 2004 Mar 15;12(6):1453-8. PubMed PMID: 15018918.

11: Biava M, Cesare Porretta G, Deidda D, Pompei R, Tafi A, Manetti F. Importance of the thiomorpholine introduction in new pyrrole derivatives as antimycobacterial agents analogues of BM 212. Bioorg Med Chem. 2003 Feb 20;11(4):515-20. PubMed PMID: 12538016.

12: Biava M. BM 212 and its derivatives as a new class of antimycobacterial active agents. Curr Med Chem. 2002 Nov;9(21):1859-69. Review. PubMed PMID: 12369872.

13: Biava M, Fioravanti R, Porretta GC, Deidda D, Maullu C, Pompei R. New pyrrole derivatives as antimycobacterial agents analogs of BM212. Bioorg Med Chem Lett. 1999 Oct 18;9(20):2983-8. PubMed PMID: 10571160.

14: Duchêne P, Laneury JP, Tran G, Ladure P, Ollivier R, Buzas A, Merour JY, Houin G. Pharmacokinetics, metabolism and bioavailability of the new anti-allergic drug BM 113. Part III: Pharmacokinetics, metabolism, dose dependency and gender effect after single or repeated administration to human healthy volunteers. Arzneimittelforschung. 1999 Aug;49(8):699-704. PubMed PMID: 10483517.

15: Duchêne P, Tran G, Ladure P, Ollivier R, Buzas A, Merour JY, Houin G. Pharmacokinetics, metabolism and bioavailability of the new anti-allergic drug BM 113. Part I: Pharmacokinetics and tissular distribution in Sprague-Dawley rats. Arzneimittelforschung. 1999 Jun;49(6):504-8. PubMed PMID: 10417866.

16: Deidda D, Lampis G, Fioravanti R, Biava M, Porretta GC, Zanetti S, Pompei R. Bactericidal activities of the pyrrole derivative BM212 against multidrug-resistant and intramacrophagic Mycobacterium tuberculosis strains. Antimicrob Agents Chemother. 1998 Nov;42(11):3035-7. PubMed PMID: 9797251; PubMed Central PMCID: PMC105991.



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