نتایج جستجو برای: antituberculosis activity
تعداد نتایج: 1135927 فیلتر نتایج به سال:
Clofazimine, a member of the riminophenazine class, is one of the few antibiotics that are still active against multidrug-resistant Mycobacterium tuberculosis (M. tuberculosis). However, the clinical utility of this agent is limited by its undesirable physicochemical properties and skin pigmentation potential. With the goal of maintaining potent antituberculosis activity while improving physico...
Benzothiazinones (BTZs) are antituberculosis drug candidates with nanomolar bactericidal activity against tubercle bacilli. Here we demonstrate that BTZs are suicide substrates of the FAD-dependent decaprenylphosphoryl-β-D-ribofuranose 2'-oxidase DprE1, an enzyme involved in cell-wall biogenesis. BTZs are reduced by DprE1 to an electrophile, which then reacts in a near-quantitative manner with ...
Two new series of 2′-hydroxy-retro-chalcone derivatives have been synthesized and fully characterized by IR, 1H NMR, 13C NMR, and mass spectral data. All of these derivatives were evaluated for their antituberculosis activity against Mycobacterium tuberculosis H37Rv. Eight of the tested compounds inhibited the growth of the mycobacterial strain. Among them, compound (E)-1-[4-(decyloxy)phenyl]-3...
A novel series of sulpha/ substituted phenyl azo indoles is synthesised by the condensation reaction of N.phenacyl sulpha/ substituted phenyl amine with diazonium salt of sulpha/substituted benzene. They were characterized by IR, NMR and UV spectra and screened for their promising antituberculosis activity and antifertility activity. Keyword: indoles, sulpha/ substituted, drug, biological activ...
The unique geographic features of Taiwan are attributed to the rich indigenous and endemic plant species in Taiwan. These plants serve as resourceful bank for biologically active phytochemicals. Given that these plant-derived chemicals are prototypes of potential drugs for diseases, databases connecting the chemical structures and pharmacological activities may facilitate drug development. To e...
The condensation of chlorides of substituted pyrazinecarboxylic acids with ringsubstituted anilines yielded twelve substituted pyrazinecarboxylic acid amides. The synthetic approach, analytical, and lipophilicity data of the newly synthesized compounds are presented. Two antituberculosis assays were used. Firstly, the antimycobacterial activity against four different Mycobacterium strains in a ...
Multiple drug hypersensitivity (MDH) is an allergy to two or more chemically unrelated drugs. We present a case of MDH caused by antituberculosis agents during the treatment of tuberculous meningitis (TBM). A 64-year-old man without a history of drug allergy developed fever and severe headache. Examination of cerebrospinal fluid showed lymphocytosis, a low glucose level, and a high ADA activity...
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