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Along with the increasing resistance of <i>Candida</i> spp. to some antibiotics, it is necessary to find new antifungal drugs, one of which is from the medicinal plant Red Betel (<i>Piper crocatum</i>). The purpose of this research is to isolate antifungal constituents from <i>P. crocatum</i> and evaluate their activities as ergosterol biosynthesis inhibitors via an in silico study of ADMET and drug-likeness analysis. Two new active compounds <b>1</b> and <b>2</b> and a known compound <b>3</b> were isolated, and their structures were determined using spectroscopic methods, while their bioactivities were evaluated via in vitro and in silico studies, respectively. Antifungal compound <b>3</b> was the most active compared to <b>1</b> and <b>2</b> with zone inhibition values of 14.5, 11.9, and 13.0 mm, respectively, at a concentration of 10% <i>w</i>/<i>v</i>, together with MIC/MFC at 0.31/1.2% <i>w</i>/<i>v</i>. Further in silico study demonstrated that compound <b>3</b> had a stronger ΔG than the positive control and compounds <b>1</b> and <b>2</b> with −11.14, −12.78, −12.00, and −6.89 Kcal/mol against ERG1, ERG2, ERG11, and ERG24, respectively, and also that <b>3</b> had the best Ki with 6.8 × 10⁻³, 4 × 10⁻⁴, 1.6 × 10⁻³, and 8.88 μM. On the other hand, an ADMET analysis of <b>1</b>–<b>3</b> met five parameters, while <b>1</b> had one violation of Ro5. Based on the research data, the promising antifungal constituents of <i>P. crocatum</i> allow <i>P. crocatum</i> to be proposed as a new antifungal candidate to treat and cure infections due to <i>C. albicans</i>.