Synthesis and Antitubercular Studies on Pyridine 1, 2, 3-Triazole Derivatives

Prabh Simran Singh*¹, Manish Devgan², Minakshi Gupta³, Gagan Shah⁴, Ravi Kumar Dhawan^5
1Departments of Pharmaceutical Chemistry, Khalsa College of Pharmacy, Amritsar
²Faculty of pharmacy, R.P.E.T, Group of institutions, Karnal
³Department of pharmaceutical Sciences, Baba Mast Nath University, Rohtak
⁴Departments of Pharmacognosy, Khalsa College of Pharmacy, Amritsar
⁵Departments of Pharmacology, Khalsa College of Pharmacy, Amritsar

A B S T R A C T
Tuberculosis (TB), an infectious disease that usually attacks the lungs, is frighteningly on the rise. Once nearly vanquished by antibiotics, at least in the developed world, TB resurged in the late 1980’s, now second only to AIDS among infectious disease. Thirty million people are at risk of dying from TB in the next 10 years, most of them living in Africa. [1]It is a chronic disease caused by mycobacteria of the ‘‘tuberculosis complex’’, including primarily Mycobacterium tuberculosis, but also M. bovis and M. africanum. [2,3] The discovery of the causative agent of tuberculosis by Robert Koch in 1882 gave great hope that this ‘white plague’ would soon be vanquished. During the 20th century new anti-tuberculosis drugs were discovered. In the early 1980’s the great majority of patients could be cured by treatment with short-course curative chemotherapy that was possible as a consequence of several newly introduced anti-tuberculosis drugs. Only one decade later, an outbreak of HIV-related multi drug resistant tuberculosis in New York made TB suddenly the centre of attention. In the last decade, TB has re-emerged as one of the leading causes of death worldwide (nearly 3 million deaths annually). [4] The estimated 8.8 million new cases every year correspond to 52,000 deaths per week or more than 7,000 each day. [5,6]1,2,3-Triazoles are an important class of heterocyclic compounds due to their wide range of applications including as pharmaceutical agents. Different methods for synthesizing 1, 2, 3-triazole are described in the literature [7].In this work, the cycloaddition reactions between diazomalonaldehyde (1) and pyridine hydrochlorides in water were effectively used to prepare the pyridine based-1, 2, 3-triazole-4-carbaldehydes in moderate-to-good yields.
Keywords: Tuberculosis, Mycobacterium, Anti-tubercular, Multi drug resistance.