13214-53-4Relevant articles and documents
Synthesis, antileishmanial and antitrypanosomal activities of N-substituted tetrahydro-β-carbolines
Manda, Sudhakar,Khan, Shabana I.,Jain, Surendra K.,Mohammed, Shabber,Tekwani, Babu L.,Khan, Ikhlas A.,Vishwakarma, Ram A.,Bharate, Sandip B.
supporting information, p. 3247 - 3250 (2014/07/22)
A series of N-substituted tetrahydro-β-carbolines were synthesized and screened for antileishmanial activity through an in vitro assay that involves promastigotes and axenic amastigotes of Leishmania donovani, the causative agent for visceral leishmaniasis. The thiophen-2-yl analogs 9b and 11f and naphthyl analog 11h were found to show significant activity against promastigotes with IC50 values of 12.7, 9.1 and 22.1 μM, respectively. Analogs 9b and 11h were also effective against axenic amastigotes with IC50 values of 62.8 and 87.6 μM, respectively. The antileishmanial activity of analogs was then tested in human macrophage cell line infected with L. donovani amastigotes and 2-naphthyl linked analog 11h was found to be effective with IC50 value of 28.3 μM. Several analogs also displayed antitrypanosomal activity against Trypanosoma brucei, the causative agent for human African trypanosomiasis. Compounds 11e, 11f and 11h were more effective than others with IC50 values of 1.0, 8.9 and 10.2 μM, respectively. All synthesized analogs were not cytotoxic towards mammalian cell lines including Vero (monkey kidney fibroblasts), HEPG2 (human hepatoma cells), LLC-PK1 (pig kidney epithelial cells) and THP-1 (human macrophages).
Azlocillin. Ein neues Penicillin aus der Acylureidoreihe. Synthese und chemische Eigenschaften
Koenig, Hans-Bodo,Metzer, Karl-Georg,Offe, Hans-Albert,Schroeck, Wilfried
, p. 59 - 63 (2007/10/02)
Azlocillin, 6--penicillanic acid is a new semi synthetic acylureido-penicillin presenting a broad antibacterial spectrum, especially against Pseudomonas.Synthesis from ampicillin and 6-aminopenicillanic acid as well as physicochemical properties of free acid and sodium salt are described.Azlocillin is cleaved by penicillinase to penicilloate which is further degraded by acid to peniollate.Keywords: Azlocillin. - Acylureidopenicillin. - Antibacterial activity.
7-Ureido acetamido substituted cephalosporin antibiotics
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, (2008/06/13)
Cephalosporin antibiotics of the formula STR1 wherein R is STR2 and R" is H, C1 -C3 alkyl, allyl, propargyl, C3 -C6 cycloalkyl, phenyl, benzyl or furfuryl; R' is H or methyl; or R is a cyclic urea group for example, R is STR3 R1 is phenyl, thienyl, or furyl; R3 is a lower alkyl substituted 1H-tetrazole-5-thio or 1,3,4-thiadiazole-5-thio group and R4 is hydrogen or an active ester group, e.g., an acetoxymethyl group; are highly active broad spectrum antibiotics especially useful in the treatment of infections attributable to the gram-negative microorganisms.