Background: Today, the occurrence and recurrence of multidrug-resistant tuberculosis
strains and comorbidities are the main reasons for long-term morbidity and mortality from tuberculosis
from the nasty acid-fast pathogen Mycobacterium tuberculosis. Therefore, discovering and developing
well-tolerated and non-toxic antituberculosis regimens are directly needed to defend the variants
strains of M. tuberculosis and, alternatively, support WHO’s ‘END-TB’ campaign.
Objective: Alternatively, phytochemicals from various common and medicinal plants have always
been vital therapeutic agents since the primitive era. Thus, proper scientific documentation as diversity,
potency, structure, drug-chemistry and overall critical analysis are essential tools to accelerate the
phytochemical-based anti-TB drug development.
Methods: In the present review, we have used some specific keywords such as ‘antituberculosis phytochemicals’,
&; antituberculosis phytochemicals from plant source&; ‘natural products against tuberculosis’
in Google, PubMed, ScienceDirect sites to get more appropriate research publications.
Further, based on lower minimum inhibitory concentration within fifty μ g/mL, a total of twohundred-
twenty-one bioactive anti-TB phytochemicals were selected for critical drug-chemistry and
structural activity relationship analyses to select most potential ‘lead candidate’ for anti-TB drug development.
Results: Based on lower concentration, abietane, ethyl-p-methoxycinnamate, ergosterol peroxide,
mono-O-methyl curcumin isoxazole, 7-methyljuglone, 12-demethylmulticaulin, 12-methyl-5-
dehydroacetylhorminone, tryptanthrin, etc. are some of the potential anti-TB phytochemicals. Interestingly,
existing and clinical drug pipelines for TB contain several active phytochemical pharmacophores
illustrated from the structural analysis.
Conclusion: Therefore, updated experimental documentation and structural-cum-critical drugchemistry
analysis on isolated antituberculosis phytochemicals at the primary level are more beneficial
for drug developers, R&D centres, and pharmaceutical companies to accelerate anti-TB drug
development using phytochemicals.