Bactericidal Activities of the Pyrrole Derivative BM212 against Multidrug-Resistant and Intramacrophagic
            <i>Mycobacterium tuberculosis</i>
            Strains

Deidda, Delia; Lampis, Giorgio; Fioravanti, Rossella; Biava, Mariangela; Porretta, Giulio Cesare; Zanetti, Stefania Anna Lucia; Pompei, Raffaello

doi:10.1128/aac.42.11.3035

Cited by 155 publications

(61 citation statements)

References 17 publications

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“…This compound also exerted its antimycobacterial activity on intracellular bacilli residing in the U937 human histiocytic lymphoma cell line, after 7 days of contact [17][18].…”

Section: -(Bm 212)mentioning

confidence: 98%

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BM 212 and its Derivatives as a New Class of Antimycobacterial Active Agents

Biava

2002

CMC

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During our investigation in pyrrole antibacterial area we have identified a subclass with a good potent in vitro activity against mycobacteria and fungi. We have individuated the salient structural feature and BM 212 as lead for the class. SAR studies allowed us to synthesize several analogue derivatives. Some of them revealed more active than BM 212 against mycobacteria, but they lost antifungal activity. In particular the Protection Index (PI) was very interesting for some derivatives, comparable to that of reference compounds, Isoniazid (INH), Streptomycin (SM) and Rifampin (RF). Many of the synthesized compounds revealed active against intracellular mycobacteria and they showed to be inhibitory to drug-resistant mycobacteria of clinical origin. On the base of microbiological results we have hypothesized a pharmacophore model that was also optimized. The rational design, and the evaluation of the in vitro activity against mycobacteria are described.

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“…This compound also exerted its antimycobacterial activity on intracellular bacilli residing in the U937 human histiocytic lymphoma cell line, after 7 days of contact [17][18].…”

Section: -(Bm 212)mentioning

confidence: 98%

“…Among all derivatives 1, the most active was 2-(B M 212), that was found to be potent active against both collection and clinical strains of Mycobacterium tuberculosis [17][18]. …”

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confidence: 98%

BM 212 and its Derivatives as a New Class of Antimycobacterial Active Agents

Biava

2002

CMC

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“…The invention appears to be based partly on earlier studies on certain substituted pyrroles that exhibited antimycobacterial activity [25,26]. Later, novel and improved pyrrole derivatives that exhibited superior anti-tubercular activity were synthesized by Lupin [27].…”

Section: Other Drugs Currently In Clinical Trialsmentioning

confidence: 99%

Social Leverage of Intellectual Property: Road to the Development of Better Therapy for Tuberculosis

Thangaraj

Reljić²

2009

PRI

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Current TB drug development is beset with many problems. There is a perceived lack of commercial return on investment, as the vast majority of TB patients come from impoverished areas of the world. Clinical trials for new TB drugs are complex, protracted and very expensive. Therefore, the development of new anti-tuberculosis drugs requires simultaneous forward planning of the design of the trials that will be required for licensing purposes. In this article we briefly review the current state of new TB drug development and discuss issues related to intellectual property (IP), with a special emphasis on how IP can facilitate rather than hinder the development of better TB drugs. We also list and discuss the major patent applications that underpin TB drugs that have entered prominent clinical trials and additional applications that were filed over the last five years for drugs resulting from basic upstream research.

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“…This class has been under investigation by an academic group from Italy and is in preclinical lead optimization [81][82][83][84][85][86].…”

Section: Small Molecules With Activity Against M Tuberculosismentioning

confidence: 99%

New Tuberculosis Drugs in Development

Laughon¹

2007

CTMC

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Over the past 50 years, no new drug classes have been introduced to treat tuberculosis. Tuberculosis (TB) kills nearly two million people a year mainly in the poorest communities in the developing world. It afflicts millions more. About one third of the world's population is silently infected with TB that may erupt into disease with increased age or suppression of the immune system. Nearly nine million new active cases develop every year. The World Health Organization (WHO) declared the disease a global emergency as long ago as 1993. Although huge efforts in public health control have reduced the disease burden within most established market economies, in Africa and Asia the epidemic continues to accelerate, particularly fueled by the HIV epidemic. Furthermore, resistance to the standard drugs isoniazid and rifampicin is increasing worldwide. Since the 1990s, mycobacteria have emerged with resistance patterns rendering all currently available antibiotics ineffectual. The pharmaceutical industry has mostly abandoned TB drug development due to perceived non-profitable consumer market and the diminishing number of companies engaged in anti-infective research. The public sector and infectious disease researchers have responded to advance fundamental science and to create new chemical entities as early drug candidates. With support from research funding agencies, philanthropic donors, and the STOP-TB Partnership, new chemical tools and new approaches to effectively implement TB control programs are evolving. Advanced preclinical development and strategies for Phase III clinical trials remain gap areas that will require additional engagement from all sectors.

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Bactericidal Activities of the Pyrrole Derivative BM212 against Multidrug-Resistant and Intramacrophagic Mycobacterium tuberculosis Strains

Cited by 155 publications

References 17 publications

BM 212 and its Derivatives as a New Class of Antimycobacterial Active Agents

BM 212 and its Derivatives as a New Class of Antimycobacterial Active Agents

Social Leverage of Intellectual Property: Road to the Development of Better Therapy for Tuberculosis

New Tuberculosis Drugs in Development

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