Importance of the thiomorpholine introduction in new pyrrole derivatives as antimycobacterial agents analogues of BM 212

Biava, Mariangela; Porretta, Giulio Cesare; Deidda, Delia; Pompei, Raffaello; Tafi, Andrea; Manetti, Fabrizio

doi:10.1016/s0968-0896(02)00455-8

Cited by 74 publications

(42 citation statements)

References 10 publications

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“…2-Methyl-1,3,5-trisubstituted pyrroles have significant activity against Mycobacterium tuberculosis, as proved by Biava et al (4,5). Diguanidino-1-methyl-2,5-diaryl-1H-pyrrole derivatives have antifungal activity against Candida species, as reported by Jana et al (6).…”

mentioning

confidence: 82%

Synthesis of certain pyrrole derivatives as antimicro-bial agents

Mohamed¹,

El-Domany²,

El-Hameed³

2009

Acta Pharmaceutica

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Synthesis of certain pyrrole derivatives as antimicro-bial agentsIn an effort to establish new pyrroles and pyrrolo[2,3-d] pyrimidines with improved antimicrobial activity we report here the synthesis andin vitromicrobiological evaluation of a series of pyrrole derivatives. A series of new 2-aminopyrrole-3-carbonitriles (1a-d) were synthesized from the reaction of benzoin, primary aromatic amines and malononitrile, from which a number of pyrrole derivatives (2a-dto5a-d) and pyrrolo[2,3-d]pyrimidines (6a-dto10a, d) were synthesized. Thein vitroantimicrobial testing of the synthesized compounds was carried out against Gram-positive, Gram-negative bacteria and fungi. Some of the prepared compounds, [2-amino-1-(2-methylphenyl)-4,5-diphenyl-1H-pyrrole-3-carbonitriles (1b), 2-amino-3-carbamoyl-1-(3-methylphenyl)-4,5-diphenyl-1H-pyrroles (2b),N-(3-cyano-1-(2-methylphenyl)-4,5-diphenyl-1H-pyrrol-2-yl)-acetamides (3b),N-(3-cyano-1-(3-methylphenyl)-4,5-diphenyl-1H-pyrrol-2-yl)-acetamides (3c), 2-amino-1-(4-methoxyphenyl)-4,5-diphenyl-3-tetrazolo-1H-pyrroles (5d),7-(4-methoxyphenyl)-5,6-diphenyl-7H-pyrrolo [2,3-d]pyrimidin-4(3H)-ones (7d), 7-(3-methylphenyl)-5,6-diphenyl-7H-pyrrolo[2,3-d]pyrimidin-4(3H)-thione (9b) andN-(7-(2-methylphenyl)-5,6-diphenyl-7H-pyrrolo[2,3-d] pyrimidine)-N-aryl amines (10a)] showed potent antimicrobial activity.

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confidence: 82%

Synthesis of certain pyrrole derivatives as antimicro-bial agents

Mohamed¹,

El-Domany²,

El-Hameed³

2009

Acta Pharmaceutica

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“…In line with the structure-activity approach, it has been shown that an acid group is the key to mediating the antiviral activity of a compound [68]. Conversely, the presence of chlorine atoms simultaneously in the para position at both N1 and C5 of the pyrrole is reported to determine the extent of the antimycotic activity of a system [69]. Furthermore, Laatsch et al [70] have indicated that increasing the co-planarity of phenol and pyrrole rings by separating them leads to strengthening the potential intermolecular hydrogen bond with a hypothetical receptor; that bond strength being a measure of the antibacterial activity of an investigated compound.…”

Section: Chemically-prepared Pyrrole Derivativesmentioning

confidence: 96%

Living on pyrrolic foundations – Advances in natural and artificial bioactive pyrrole derivatives

Domagala

Jarosz

Łapkowski

2015

European Journal of Medicinal Chemistry

123

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“…A piperazine derivative BM 212 (28), which arose the interest with its very good in vitro activity of MIC 0.7 μg/mL against Mtb [50].…”

Section: Piperazine and Pyrazine Derivativesmentioning

confidence: 99%

Recent Efforts for the Development of Antitubercular Drug Containing Diazine Ring

Asif¹

2012

Med chem

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There has been considerable interest in the development of new molecule with antibacterial activities particularly against tuberclosis because mycobacterium species have developed resistant against currently used drugs, their toxic effect and long duration of therapy. The diazine (pyridazine, pyrimidine and piperazine) derivatives possess an important class of compound for new drugs research and development. Therefore, many researchers have synthesized these compounds as target structures and evaluated their antitubercular activity. These observations have been guiding for the development of new molecules that possess potent antitubercular activity with minimum side effects or effective against MDR, XDR mycobacterium strains, and also in patient co-infected with HIV/AIDS.

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Importance of the thiomorpholine introduction in new pyrrole derivatives as antimycobacterial agents analogues of BM 212

Cited by 74 publications

References 10 publications

Synthesis of certain pyrrole derivatives as antimicro-bial agents

Synthesis of certain pyrrole derivatives as antimicro-bial agents

Living on pyrrolic foundations – Advances in natural and artificial bioactive pyrrole derivatives

Recent Efforts for the Development of Antitubercular Drug Containing Diazine Ring

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