Affiliations 

  • 1 1Faculty of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, 124001 India
  • 2 2Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), 42300 Bandar Puncak Alam, Selangor Darul Ehsan Malaysia
  • 3 5Department of Pharmacology and Toxicology, College of Pharmacy, Qassim University, Buraidah, 51452 Kingdom of Saudi Arabia
BMC Chem, 2019 Dec;13(1):12.
PMID: 31384761 DOI: 10.1186/s13065-019-0533-7

Abstract

Background: Dihydrofolate reductase (DHFR) is an important target for antimetabolite class of antimicrobials because it participates in purine synthesis. 2-mercaptobenzimidazole (2MBI) has similar structural features as purine nucleotides. Given that benzimidazole and similar heteroaromatics have been broadly examined for their anticancer potential, so, we hereby report the design, synthesis and biological studies (i.e. antimicrobial and anticancer studies) of 2MBI derivatives.

Methodology: The antimicrobial activity of synthesized 2MBI derivatives were evaluated against Gram positive and Gram negative bacterial species as well as fungal species by tube dilution technique whereas their anticancer activity was assessed against human colorectal carcinoma cell line (HCT116) by Sulforhodamine B (SRB) assay. They were also structurally characterized by IR, NMR, MS and elemental analyses.

Results discussion and conclusion: The antimicrobial activity findings revealed that compound N1 (MIC
bs,st,
ca
 = 1.27, 2.54, 1.27 µM), N8 (MIC
ec
= 1.43 µM), N22 (MIC
kp,an
= 2.60 µM), N23 and N25 (MIC
sa
= 2.65 µM) exhibited significant antimicrobial effects against tested strains, i.e. Gram-positive, Gram-negative (bacterial) and fungal strains. The anticancer screening results demonstrated that compounds N9, N18 (IC50 = 5.85, 4.53 µM) were the most potent compounds against cancer cell line (HCT116) even more than 5-FU, the standard drug (IC50 = 9.99 µM).

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.