872552-44-8Relevant academic research and scientific papers
Structure-guided design and development of novel benzimidazole class of compounds targeting DNA gyraseB enzyme of Staphylococcus aureus
Janupally, Renuka,Jeankumar, Variam Ullas,Bobesh, Karyakulam Andrews,Soni, Vijay,Devi, Parthiban Brindha,Pulla, Venkat Koushik,Suryadevara, Priyanka,Chennubhotla, Keerthana Sharma,Kulkarni, Pushkar,Yogeeswari, Perumal,Sriram, Dharmarajan
, p. 5970 - 5987 (2014)
The gyraseB subunit of Staphylococcus aureus DNA gyrase is a well-established and validated target though less explored for the development of novel antimicrobial agents. Starting from the available structural information in PDB (3TTZ), we identified a novel series of benzimidazole used as inhibitors of DNA gyraseB with low micromolar inhibitory activity by employing structure-based drug design strategy. Subsequently, this chemical class of DNA gyrase inhibitors was extensively investigated biologically through in vitro assays, biofilm inhibition assays, cytotoxicity, and in vivo studies. The binding affinity of the most potent inhibitor 10 was further ascertained biophysically through differential scanning fluorimetry. Further, the most potent analogues did not show any signs of cardiotoxicity in Zebra fish ether-a-go-go-related gene (zERG), a major breakthrough among the previously reported cardiotoxic gyraseB inhibitors.
Benzimidazole compounds for regulating IgE
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, (2008/06/13)
This invention relates to a family of phenylbenzimidazole analogs, which are inhibitors of the IgE response to allergens. These compounds are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic.
Benzimidazole compounds for regulating IgE
-
, (2008/06/13)
This invention relates to a family of phenylbenzimidazole analogs, which are inhibitors of the IgE response to allergens. These compounds are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic.
Benzimidazole analogs as down-regulators of IgE
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, (2008/06/13)
This invention relates to a family of diacyl benzimidazole analogs, which are inhibitors of the IgE response to allergens. These compounds are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic.
