ISSN 2321–3647
Sun, 19 Nov 2017

Design, Synthesis, Characterization and Biological Evaluation of New Heterocyclic Derivatives As Anti-Tubercular Agents

Ayyadurai Jerad Suresh1*, Geetha Lakshmi1, Sundaralingam Saranya1, Parakkot Ramakrishnan Surya1

1. College of Pharmacy, Madras Medical College, Chennai


ABSTRACT

Oxadiazole, a heterocyclic nucleus has attracted a wide attention of the chemist in search for the new therapeutic molecules. Some of the recent studies show that oxadiazole are reported to possess an anti-tubercular, anti-epileptic, analgesic, hypnotic, and sedative activity.1 Catechol is a chemical, but a catechol may also be used as the name of a substance, where it represents a 1, 2-dihydroxy benzene group2. In the present study 1, 3, 4-oxadiazole and phenyl amino benzene 1,2 -diol derivatives were docked against methoxymycolic acid synthase-2 and synthesized using reflux condensation reaction. The newly synthesized compounds were characterized by elemental and spectral methods. Compounds RSP1, RSP3 and RSP4 are novel compounds. Anti-tubercular activities of these compounds were carried out using Alamar blue assay method and these compounds exhibited good activity. Compound with phenyl amino benzene 1, 2 diol showed good activity and oxadiazole showed moderate activity compared with standard drugs. RSP1, RSP3, and RSP4 shows good activity at the range of 0.8µg -50ng.RSP6 and RSP7 shows activity at 12.5µg. A further refinement to the structure of the synthesized compounds is expected to yield new outlook to the development of promising molecules against Mycobacterium tuberculosis.

Keywords: Oxadiazole, anti-tubercular, catechol, phenyl amino benzene1, 2-diol, analgesic.


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