2. Academic Validation
  3. New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation

New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation

  • Bioorg Med Chem Lett. 2017 Jan 15;27(2):288-294. doi: 10.1016/j.bmcl.2016.11.056.
Mahendra B Bhalerao 1,  Sambhaji T Dhumal 1,  Amarsinh R Deshmukh 1,  Laxman U Nawale 2,  Vijay Khedkar 3,  Dhiman Sarkar 2,  Ramrao A Mane 4
Affiliations

Affiliations

  • 1 Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431004, Maharashtra, India.
  • 2 Combi-Chem Bio Resource Center, CSIR-National Chemical Laboratory, Pune 411008, Maharashtra, India.
  • 3 School of Health Sciences, University of KwaZulu Natal, Westville Campus, Durban 4000, South Africa; St. John Institute of Pharmacy and Research (SJIPR), St. John Technical Campus, Vevoor, Manor Road, Palghar (E), District Palghar 401404, Maharashtra, India.
  • 4 Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431004, Maharashtra, India. Electronic address: manera2011@gmail.com.
PMID: 27914801 DOI: 10.1016/j.bmcl.2016.11.056
Abstract

New bithiazolyl hydrazones (6a-l) have been first time synthesized by carrying novel one pot cyclocondensation of 5-acyl thiazoles (1a-b), thiosemicarbazide (2) and substituted phenacyl chlorides (4a-f) in freshly prepared ionic liquid, diisopropyl ethyl ammonium acetate (DIPEAc) at room temperature. The newly synthesized compounds have been evaluated for their antitubercular activity and the compounds 3b, 6a, 6b, 6d, 6e, 6f, 6g, and 6l have displayed noticeable antitubercular activity compared to Rifampicin with tolerable cytotoxicity. All these compounds were also screened for their Antibacterial activity and found that, compounds 6j and 6k have exhibited a very good Antibacterial activity. Molecular docking study has shown better harmony with the evaluation trend shown by these compounds under in vitro antitubercular screening.

Keywords

Antibacterial activity; Antitubercular activity; Bithiazole; Cytotoxicity; Ionic liquid; Molecular docking; Thiosemicarbazones.

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