Role of Pyridine Containing Azetidinone Derivatives as Privileged Scaffolds in Anti Tubercular Agents | Chapter 9 | Technological Innovation in Pharmaceutical Research Vol. 11

In the current study, we synthesised a novel series of 3-Chloro-1-phenyl-4-(pyridine-4yl-)azetidin-2-one derivatives using Schiff base as an intermediary in the quest for prospective Tuberculosis treatments. The resulting Schiff base is then eliminated, resulting in named Azetidinone derivatives. Nucleophilic addition followed by elimination is the mechanism involved in the production of Schiff base. The newly produced Schiff base is then cyclized to produce novel Azetedinone derivatives. The named compounds were physically examined and structurally investigated using spectroscopic methods (IR, 1H-NMR, MASS). The chemicals Azt-1 to Azt-6 were tested for anti-tubercular activity in vitro. The Micro plate Alamar Blue Assay (MABA) method was used to test anti-tubercular activity in vitro. Azt-1(H), Azt-2(Cl), Azt-5 (O-OH), and Azt-6 (P-OH) were the most active compounds in the series compared to standards. The presence of electron withdrawing group -Cl, (Azt-2) and electron donating substituents -OH at ortho and para positions in the phenyl ring of (Azt-5) and (Azt-6) respectively could explain the potent anti tubercular activity.

Author (S) Details

N. Pramod
Department of Pharmaceutical Chemistry, A.G.M College of Pharmacy, Varur-581207, Hubli, Karnataka, India.

C. Bharath Kumar
Department of Pharmaceutical Chemistry, Annamacharya College of Pharmacy, Rajampet-516126, Kadapa, Andhra Pradesh, India.

P. Sri Lekha
Department of Pharmaceutical Chemistry, Institute of Pharmaceutical Technology, SPMVV, Tirupati-517502, Andhra Pradesh, India.

B. Mayuri
Department of Pharmaceutical Chemistry, Annamacharya College of Pharmacy, Rajampet-516126, Kadapa, Andhra Pradesh, India.

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