Synthesis, antimicrobial and cytotoxic activities of pyrimidinyl benzoxazole, benzothiazole and benzimidazole

D Seenaiah; P Ramachandra Reddy; G Mallikarjuna Reddy; A Padmaja; V Padmavathi; N Siva Krishna

doi:10.1016/j.ejmech.2014.02.050

Synthesis, antimicrobial and cytotoxic activities of pyrimidinyl benzoxazole, benzothiazole and benzimidazole

Eur J Med Chem. 2014 Apr 22:77:1-7. doi: 10.1016/j.ejmech.2014.02.050. Epub 2014 Feb 20.

Authors

D Seenaiah¹, P Ramachandra Reddy¹, G Mallikarjuna Reddy¹, A Padmaja¹, V Padmavathi², N Siva Krishna³

Affiliations

¹ Department of Chemistry, Sri Venkateswara University, Tirupati 517 502, Andhra Pradesh, India.
² Department of Chemistry, Sri Venkateswara University, Tirupati 517 502, Andhra Pradesh, India. Electronic address: vkpuram2001@yahoo.com.
³ Department of Molecular Reproduction Development and Genetics, Indian Institute of Science, Bangalore 560 012, Karnataka, India.

PMID: 24607584
DOI: 10.1016/j.ejmech.2014.02.050

Abstract

A variety of pyrimidinyl benzoxazoles, benzothiazoles and benzimidazoles linked by thio, methylthio and amino moieties were prepared and studied their antimicrobial and cytotoxic activities. The compound pyrimidinyl bis methylthio benzimidazole 22 was a potent antimicrobial agent particularly against Staphylococcus aureus (29 mm, MIC 12.5 μg/mL) and Penicillium chrysogenum (38 mm, MIC 12.5 μg/mL). The amino linked pyrimidinyl bis benzothiazole 24 exhibited cytotoxic activity on A549 cells with IC50 value of 10.5 μM.

Keywords: Antimicrobial activity; Benzimidazole; Benzothiazole; Cytotoxic activity; Pyrimidinyl benzoxazole.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Anti-Bacterial Agents / chemical synthesis
Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / pharmacology*
Antifungal Agents / chemical synthesis
Antifungal Agents / chemistry
Antifungal Agents / pharmacology*
Benzimidazoles / chemical synthesis
Benzimidazoles / chemistry
Benzimidazoles / pharmacology
Benzimidazoles / toxicity*
Benzothiazoles / chemical synthesis
Benzothiazoles / chemistry
Benzothiazoles / pharmacology
Benzothiazoles / toxicity*
Benzoxazoles / chemical synthesis
Benzoxazoles / chemistry
Benzoxazoles / pharmacology
Benzoxazoles / toxicity*
Cell Line, Tumor
Cell Proliferation / drug effects
Cell Survival / drug effects
Dose-Response Relationship, Drug
Humans
Microbial Sensitivity Tests
Molecular Structure
Penicillium chrysogenum / drug effects
Staphylococcus aureus / drug effects
Structure-Activity Relationship

Substances

Anti-Bacterial Agents
Antifungal Agents
Benzimidazoles
Benzothiazoles
Benzoxazoles
benzimidazole
benzothiazole