2. Academic Validation
  3. Synthesis of novel benzimidazole functionalized chiral thioureas and evaluation of their antibacterial and anticancer activities

Synthesis of novel benzimidazole functionalized chiral thioureas and evaluation of their antibacterial and anticancer activities

  • Bioorg Med Chem Lett. 2014 Oct 15;24(20):4822-5. doi: 10.1016/j.bmcl.2014.08.064.
Sridhar Madabhushi 1,  Kishore Kumar Reddy Mallu 2,  Venkata Sairam Vangipuram 2,  Srinivas Kurva 2,  Y Poornachandra 3,  C Ganesh Kumar 3
Affiliations

Affiliations

  • 1 Fluoroorganics Division, CSIR-Indian Institute of Chemical Technology, Uppal Road, Hyderabad 500 007, India. Electronic address: smiict@gmail.com.
  • 2 Fluoroorganics Division, CSIR-Indian Institute of Chemical Technology, Uppal Road, Hyderabad 500 007, India.
  • 3 Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Uppal Road, Hyderabad 500 007, India.
PMID: 25241926 DOI: 10.1016/j.bmcl.2014.08.064
Abstract

A small library of benzimidazole functionalized chiral thioureas was prepared starting from natural Amino acids (S)-alanine, (S)-phenylalanine, (S)-valine and (S)-leucine and also their (R)-isomers and studied their antimicrobial activity against a various Gram-positive and Gram-negative Bacterial strains. In this study, compounds 5g and 5j were found to exhibit good Antibacterial activity against both Gram-positive and Gram-negative Bacterial strains such as Staphylococcus aureus, Bacillus subtilis, Micrococcus luteus, Klebsiella planticola, Escherichia coli and Pseudomonas aeruginosa. In the cytotoxicity study, thioureas derived from non-natural Amino acids 5a-l showed good activity against human Cancer cell lines A549, MCF7, DU145, HeLa, and no cytotoxicity was observed with their antipodes 6a-l.

Keywords

Amino acids; Antibacterial activity; Anticancer activity; Chiral thioureas.

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