Synthesis, Characterization and Antitubercular Evaluation of Novel Isatin Derivatives | Original Article

ABSTRACT:

Tuberculosis is caused by a bacterium called Mycobacterium tuberculosis, attacks the lungs but may also attack other parts of the body such as the kidney, spine, and brain. Tuberculosis may also be linked to certain risk factors, including alcoholism, IV drug abuse, and homelessness. Infection with Tubercle bacillus (most often M. tuberculosis) is characterized by the formation of tubercles. Since the main antitubercular drugs have developed resistant to the large proportion of TB patients. Bacteria’s are showing tolerances for more of antibiotics. The long treatment due to resistance causes heptotoxicity, nephrotoxicity etc. So there the Isatin was selected as template for modification and development of a compound library because anti-tubercular potential of novel Isatin derivatives like the first antitubercular potential of Isatin was confirmed by Erdman and Laurent in 1841. Isatin has medicinal potential to be used as drug template for identifying the novel drug candidates which can eliminate these treatments associated problems and can work potentially over first line drug resistant. The synthesized derivatives were potentially characterized for their purity through the chromatography and spectroscopic techniques. The confirmed derivatives were tested, the results showed like the few compounds from Bromoisatin derivatives found to show 50 MTB inhibition at concentration between 20µM to 30µM. The compounds with hydrocarbon attached substituent could show little good activity that may be due the little enhanced liphophilicity of the compounds which made the entry of the compounds easy into the MTB. The Pyrimidine derivatives of Bromoisatin were showed good results than the Bromoisatin derivatives due the significant medicinal effect of attached Pyrimidine ring which may have enhance the liphophilicity and metabolic resistance as well. Due that two compounds 32 and 33 could kill the 50 of MTB even at concentration lower than 20µM. The study led to the knowledge that the isatin has antitubercular value. The Isatin scaffold may be utilized as template for further modification and development of drug like candidate.