methyl indole derivative of some 6-aryl-4,5-dihydropyridazin-3(2h)-ones (3a-e) were synthesized by mannich reaction and evaluated as anticonvulsant against mes (50ma, for 2sec), inh (250mg/kg), scptz (80mg/kg) and str (3mg/kg) induced convulsion methods at 50 mg/kg dose level. all compounds 3a-e were also evaluated as antitubercular agent against m. tuberculosis h37rv by maba method. all compou...

OBJECTIVE To ascertain the epidemiological characteristics, clinical symptoms, and evolution of drug-induced hepatitis over the last 22 years. EXPERIMENTAL DESIGN AND SUBJECTS: An observational, retrospective study between 1982 and 1993, and prospective study between 1994 and 2003. All patients in our department diagnosed with having drug-induced hepatitis were studied analyzing epidemiological...

One way to speed up the TB drug discovery process is to search for antitubercular activity among compound series that already possess some of the key properties needed in anti-infective drug discovery, such as whole-cell activity and oral absorption. Here, we present MGIs, a new series of Mycobacterium tuberculosis gyrase inhibitors, which stem from the long-term efforts GSK has dedicated to th...

Background: Tuberculosis is a global and serious Public Health problem due to the increase of multidrugresistant and extensively drug-resistant cases; as a result, diverse research groups worldwide are focusing their efforts on finding novel antituberculous agents that can provide greater effectiveness, less toxicity and having a specific mechanism of action, possibly being coadjuvants in the t...

Mycobacterium tuberculosis, the causative agent of tuberculosis (TB), is a remarkably successful pathogen that has latently infected a third of the world population (Zhang et al., 2006). Infection occurs via aerosol, and inhalation of a few droplets containing M. tuberculosis bacilli is enough for lung infection (Hassan et al., 2006). After infection, M. tuberculosis pathogenesis occurs in two ...

Bedaquiline (BDQ) is a novel and highly potent last-line antituberculosis drug that was approved by the US FDA in 2013. Owing to its stereo-structural complexity, chemical synthesis and compound optimization are rather difficult and expensive. This study describes the structural simplification of bedaquiline while preserving antitubercular activity. The compound's structure was split into fragm...

OBJECTIVES Analyse a series of halogenated 3-deaza-adenosine analogues for efficacy against Mycobacterium tuberculosis H37Ra and determine if adenosine (Ado) kinase plays a role in the mechanism of action of these compounds. METHODS The MIC as determined by microdilution broth assay provided a measure of antitubercular efficacy. MIC values were measured in M. tuberculosis strains H37Ra, SRICK...

As a part of our research to develop novel antimicrobial and antitubercular agents, a series of 4-(2-aryl-4-oxo-1,3thiazolidine)-5-mercapto-3-(5-nitroindazolyl methyl)-1,2,4triazoles (5a-j) have been synthesized by conventional as well as microwave method. The structures of these compounds were confirmed by IR, H NMR, C NMR, FABmass spectra and also by microanalytical data. These compounds were...

A series of 14 patients suffering from tuberculosis of the sternum with a mean follow-up of 2.8 years (2 to 3.6) is presented. All were treated with antitubercular therapy: ten with primary therapy, two needed second-line therapy, and two required surgery (debridement). All showed complete healing and no evidence of recurrence at the last follow-up. MRI was useful in making the diagnosis at an ...