A series of novel propylene-1H-1,2,3-triazole-4-methylene-tethered isatin-coumarin hybrids 7a-l that were composed of three anti-tubercular bioactive substances/pharmacophore coumarin, isatin, and I-A09 were designed, synthesized, and assessed for their in vitro anti-tubercular activity against Mycobacterium tuberculosis (MTB) H 37 Rv. In spite of the hybrids were inactive against the tested MTB H 37 Rv, the structure-activity relationship was enriched, and these hybrids may act as an ideal starting point for developing new isatin-coumarin anti-TB candidates with various linkers. Scheme 1. Synthesis of propylene-1H-1,2,3-triazole-4-methylene-tethered isatin-coumarin hybrids 7a-l.