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Eur J Med Chem ; 45(10): 4545-53, 2010 Oct.
Article in English | MEDLINE | ID: mdl-20705368

ABSTRACT

In an effort to discover new and effective chemotherapeutic agents from this laboratory for the treatment of tuberculosis, here in we describe the synthesis and biological evaluation of a series of novel benzothiadiazine 1,1-dioxide (BTD) based congeners by using rifampicin, streptomycin; ciprofloxacin and amphotericin as positive controls. Further, to understand structural requirements for exploring the structure activity relationship of BTDs, cytotoxicity and in vivo study of recently reported potent molecule 4 (MIC = 1 microg/mL) is also discussed.


Subject(s)
Antitubercular Agents/chemistry , Antitubercular Agents/therapeutic use , Benzothiadiazines/chemistry , Benzothiadiazines/therapeutic use , Mycobacterium tuberculosis/drug effects , Tuberculosis/drug therapy , Animals , Antitubercular Agents/chemical synthesis , Antitubercular Agents/pharmacology , Bacteria/drug effects , Benzothiadiazines/chemical synthesis , Benzothiadiazines/pharmacology , Cell Line , Cell Survival/drug effects , Female , Fungi/drug effects , Humans , Mice , Mice, Inbred BALB C , Microbial Sensitivity Tests
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