In this study, 1<i>H</i>-pyrazole-3-carboxylic acids related to the cannabinoid type 1 (CB1) receptor antagonist rimonabant were amidated with valine or <i>tert</i>-leucine, and the resulting acids were further diversified as methyl esters, amides, and <i>N</i>-methyl amides. <i>In vitro</i> receptor binding and functional assays demonstrated a wide series of activities related to the CB1 receptors (CB1Rs). Compound <b>34</b> showed a high CB1R binding affinity (<i>K</i> <sub>i</sub> = 6.9 nM) and agonist activity (EC<sub>50</sub> = 46 nM; <i>E</i> <sub>max</sub> = 135%). Radioligand binding and [<sup>35</sup>S]GTPγS binding assays also demonstrated its selectivity and specificity to CB1Rs. Moreover, <i>in vivo</i> experiments revealed that <b>34</b> was slightly more effective than the CB1 agonist WIN55,212-2 in the early phase of the formalin test, indicating a short duration of the analgesic effect. Interestingly, in a mouse model of zymosan-induced hindlimb edema, <b>34</b> was able to maintain the percentage of paw volume below 75% for 24 h following subcutaneous injection. After intraperitoneal administration, <b>34</b> increased the food intake of mice, suggesting potential activity on CB1Rs.