Research in the thematic area of tuberculosis
Tuberculosis (TB) is a global epidemic disease and has been listed as the leading cause of death from a single infectious agent, ranking it above HIV/AIDS. It has been estimated that one fourth (~25%) of the world's population is infected with TB and is highly communicable as the TB-bacteria can survive in air for about 4 hours, so if a person with TB coughs, speaks, or sings, people nearby may inhale these bacteria and become infected. According to WHO report-2018, it is estimated that each year approximately 10 million people fall sick with TB and 1.3 million died in the year 2016 alone. India alone accounts for about 33% of global TB deaths making it the largest TB burdened country in the world. The most problematic issue today in treating this infectious disease is that the TB-bacteria is becoming resistance to almost all drugs which leads to Multi-Drug Resistance-TB (MDRTB) and extensively drug-resistant tuberculosis (XDR-TB). Currently, the treatment regime is very prolonged of 6-9 months duration with multiple drug regimens (7 to 8 drugs) which leads to drug toxicity. In this direction, studies have shown that the most successful approach to develop novel TB-drugs is re-engineering of old TB-drug classes and improve their antimycobacterial potencies. Through our research efforts in organic chemistry, we are trying to develop efficacious antitubercular drug candidates. Some of our works which have been published in the area of antitubercular research are given below-
Title: Synthesis and Evaluation of Novel Coumarin-Oxime Ethers as Potential Anti-tubercular Agents: Their DNA Cleavage Ability and BSA Interaction Study; European Journal of Medicinal Chemistry, 2018, 150, 864-875; doi: https://doi.org/10.1016/j.ejmech.2018.03.042
Authors: Dinesh S. Reddy, Manasa Kongot, Sandeep P. Netalkar, Mahantesh M. Kurjogi, Rakesh Kumar, Fernando Avecilla, Amit Kumar
- Evaluation of coumarin-oxime analogs as potent anti-tubercular agents.
- Compound 1h, exhibit MIC of 0.04µg mL-1against MTBH37Rv strain.
- Compound 1h binds with BSA without disrupting its secondary structure.
- Active compounds were stable at varied pH conditions.
- Compound 1h displayed a low level of toxicity in Vero cells along with a good safety profile in vitro.