Despite advances in molecular methods for the diagnosis of tuberculosis (TB) and its resistant forms, it remains more prevalent in the world today than at any other time in human history. Of equal concern is the slow moving antitubercular drug development pipeline which calls for research efforts to be intensified and directed towards the discovery of new molecular scaffolds and/or the remodelling of some old TB drug families. In support of the latter, this review highlights synthetic methodologies and structure activity relationships (SARs) elaborated for natural products and/or natural product derivatives with promising antitubercular activity. It further attests to the enormous potential of natural products in the antitubercular drug discovery process.