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<i>Crocus sativus</i> L. is one of the world’s most famous saffron production crops and its enormous by-products, such as leaves, are an excellent source of bioactive compounds with potential nutritional applications. The total phenolic content of <i>Crocus</i> leaves was 5.44 ± 0.01 mg GAE/g, and the total flavonoid content was 2.63 ± 0.05 mg RE/g, respectively. The main bioactive compounds in the leaves, such as polyphenols, flavonoids by HPLC and carboxylic acids, and amino acids, were also identified by GC-MS. HPLC analyses revealed mangiferin as a dominant constituent (1.26 ± 0.02 mg/g). <i>C. sativus</i> contains seven essential amino acids (ILE, LEU, LYS, MET, PHE, THR, TRP, VAL) in high concentration. Among them, isoleucine (7965 µg/g) was the dominant compound. In addition, the K and Ca concentrations in the leaves were significant (<i>p</i> < 0.05). The chemical composition revealed α-linolenic acid (22,490 µg/g) and linoelaidic acid (9880 µg/g) to be major constituents among all the acids found in the <i>Crocus</i> leaves. The extracts of <i>C. sativus</i> leaves showed the highest inhibitory activity for Gram-positive (<i>B. s</i><i>ubtilis</i> and <i>S. aureus</i>) bacteria in the <i>in vitro</i> assay. The current results identify and underline the potential of natural products from <i>C. sativus</i> leaves that can add value to saffron production.