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• Chemotherapy is the only way of treatment for helminthiasis. • Anthelmintic drug resistance has been reported for commercially available anthelmintic drugs. • Benzimidazole derivatives are commercially used as anthelmintic drug. • Structural optimization of benzimidazole nucleus can be produced important anthelmintics. • The broad-spectrum activity of benzimidazole carbamates is attributed to their ability to inhibit tubulin polymerization. Globally, helminthiasis is one of the most prevalent causes of mortality and morbidity and threatens humans and livestock. An effective anthelmintic vaccine is also lacking. As a result, nematode infections are mostly treated with chemotherapy, such as benzimidazoles, but due to drug resistance, their effectiveness is limited.This review focuses on previously synthesized benzimidazole derivatives and their structure-activity relationships related to effectiveness in treating helminthiasis. For example, structural modifications have been introduced in developing benzimidazole-based drugs for helminthiasis chemotherapy at positions 2, 5, or 6, whereas positions 4 and 7 should not be altered. For benzimidazole to be effective as an anthelmintic, it must have a free hydrogen atom at its 1-position.Using the results of this review as a guide, we have proposed designs that will allow the development of more effective and less toxic drugs for helminthiasis chemotherapy. Despite this, a better understanding of parasite biochemistry and host-parasite interactions is necessary to develop innovative lead molecules with greater efficacy. [Display omitted] [ABSTRACT FROM AUTHOR]