68282-55-3Relevant academic research and scientific papers
Process for preparing 6-alkylidene penem derivatives
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, (2008/06/13)
The present invention provides a process of making compounds of formula I, which are useful for the treatment of bacterial infection or disease.
Novel imidazole substituted 6-methylidene-penems as broad-spectrum β-lactamase inhibitors
Venkatesan, Aranapakam M.,Agarwal, Atul,Abe, Takao,Ushirogochi, Hideki,Yamamura, Itsuki,Kumagai, Toshio,Petersen, Peter J.,Weiss, William J.,Lenoy, Eileen,Yang, Youjun,Shlaes, David M.,Ryan, John L.,Mansour, Tarek S.
, p. 5807 - 5817 (2007/10/03)
A series of novel imidazole substituted 6-methylidene-penems has been synthesized (R = heterocycle) and was shown to be potent, broad-spectrum β-lactamase inhibitors against class-A and class-C enzymes. The present paper deals with the design, synthesis, and structure-activity relationships (SAR) of compounds 11-15. β-Lactamases are serine and metallo-dependent enzymes produced by the bacteria in defense against β-lactam antibiotics. Production of class-A, class-B, and class-C enzymes by the bacteria make the use of β-lactam antibiotics ineffective in certain cases. To overcome resistance to β-lactam antibiotics, several β-lactamase inhibitors such as clavulanic acid, sulbactam, and tazobactam are widely used in the clinic in combination with β-lactam antibiotics. However, single point mutations within these enzymes have allowed bacteria to overcome the inhibitory effect of the commercially approved β-lactamase inhibitors. Although the commercially available β-lactamase inhibitor/β-lactam antibiotic combinations are effective against class-A producing bacteria and many extended spectrum β-lactamase (ESBL's) producing bacteria they are less effective against class-C enzymes expressing bacteria. To circumvent this problem, based on modeling studies several novel imidazole substituted 6-methylidene-penem derivatives were synthesized and tested against various β-lactamase producing isolates. The present paper deals with the synthesis and structure-activity relationships (SAR) of these compounds.
Imidazotriazines as Potential Antiasthma Agents
Paul, Rolf,Brockman, John A.,Hallett, W. A.,Hanifin, John W.,Tarrant, M. Ernestine,et al.
, p. 1704 - 1716 (2007/10/02)
By using inhibition of histamine release from antigen-challenged, sensitized human basophils as a means of identifying a potentialy prophylactic drug for the treatment of asthma, a series of substituted imidazotriazines were found, which wer
Imidazo[1,5-d]-as-triazine-4(3H)-ones and thiones
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, (2008/06/13)
There is provided substituted imidazo[1,5-d]-as-triazine-4(3H)-ones and substituted imidazo[1,5-d]-as-triazin-4(3H)-thiones useful as inhibitors of the enzyme cyclic-AMP phosphodiesterase and as broad spectrum herbicides.
Method for the control of undesired plant species using imidazo-as-triazinones and triazine-thiones
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, (2008/06/13)
This disclosure describes herbicidal methods for the pre- and postemergence control of undesired mono- and dicotyledonous plants using substituted imidazo[1,5-d]-as-triazin-4(3H)-ones and substituted imidazo[1,5-d]-as-triazine-4(3H)-thiones.
SUBSTITUTED 3-(4-IMIDAZOLYLMETHYLENE)CARBAZIC AND THIOCARBAZIC ACID ESTERS
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, (2008/06/13)
There are provided substituted 3-(4-imidazolyl-methylene)carbazic acid esters and 3-(4-imidazolylmethylene)dithiocarbazic acid esters useful as intermediates for the preparation of compounds which inhibit the enzyme cyclic-AMP phosphodiesterase
IMIDAZO [1,5-d]-AS-TRIAZINE-4(3H)-ONES AND THIONES
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, (2008/06/13)
There is provided substituted imidazo[1,5-d]-as-triazine-4(3H)-ones and substituted imidazo[1,5-d]-as-triazin-4(3H)-thiones useful as inhibitors of the enzyme cyclic-AMP phosphodiesterase and as broad spectrum herbicides
