Synthesis, biological evaluation and molecular docking study of some new 4-aminosalicylic acid derivatives as anti-inflammatory and antimycobacterial agents.

In this study, new derivatives of the antitubercular and anti-inflammatory drug, 4-aminosaliclic acids (4-ASA) were synthesized, characterized, and evaluated for these activities. In vivo and in viro evaluation of anti-inflammatory activity revealed that compounds 10, 19 and 20 are the most active with potent cyclooxygenase-2 (COX-2) and 5-lipooxgenase (5-LOX) inhibition and without causing gasric lesions. The minimum inhibitory concentrations (MIC) of the newly synthesized compound were, also, measured against Mycobacterium tuberculosis H37RV. Among the tested compounds 17, 19 and 20 exhibited significant activities against the growth of M. tuberculosis. 20 is the most potent with (MIC 1.04 µM) 2.5 folds more potent than the parent drug 4-ASA. 20 displayed low cytotoxicity against normal cell providing a high therapeutic index. Important structure features were analyzed by docking and structure-activity relationship analysis to give better insights into the structural determinants for predicting the anti-inflammatory and anti-TB activities. Our results indicated that compounds 19 and 20 are potential lead compounds for the discovery of dual anti-inflammatory and anti-TB drug candidates.

Is plague a problem in the Egyptians returning back from Libya?

Many employees return home with fever with or without other accompanying symptoms. Fever can be a manifestation of a minor, self-limited process or can herald a progressive, life-threatening illness. The assessment of this group is often hampered by the clinician's lack of familiarity with the types of infections that the patient may have encountered while traveling. The evaluation of such patients should focus on: What infections are possible given where the patient has lived or traveled and the time when exposures may have occurred? Which of these infections is more probable given the patient's clinical findings and potential exposures? Which of these infections is treatable or transmissible or both? On the other hand, the outbreak of plague at the Libyan-Egyptian borders and the high density rodents and their ecto-parasitic fleas in many Egyptian governorates should be embarked a control program to rodents and fleas and to raise the awareness of the concerned authorizes.