Benzimidazole derivatives are represented by a wide variety of medicines, such as albendazole, thiabendazole, omeprazole, carbendazim, mebendazole, and timoprazole [1-3], while in nature the benzimidazole moiety is found in the structure of vitamin B12 [4]. In our previous studies, we have synthesized some bioactive benzimidazole derivatives. Some of the compounds were shown to demonstrate important antitumor, antioxidant, and lipase inhibition activities [5-8]. In the last of these studies we focused on the synthesis of novel benzimidazole as potent anti-tyrosinase and antioxidant agents [8]. In the current study we synthesized, with a green approach, from these benzimidazoles (1a-f) to benzimidazole-acetates (2a-f) and benzimidazole-acetohydrazides (3a-f) derivatives. These 12 derivatives have been screened for their antimicrobial and antioxidant activities.