- Design, synthesis and antimicrobial study of novel 1-(1,3-benzothiazol-2-yl)-3-chloro-4H-spiro[azetidine-2,3'-indole]-2',4(1'H)-diones through ketene–imine cycloaddition reaction
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The present study deals with the synthesis of novel 1-(1,3-benzothiazol-2-yl)-3-chloro-4H-spiro[azetidine-2,3'-indole]-2',4(1'H)-dione derivatives from the reaction of 3-(1,3-benzothiazol-2-ylimino)-1,3-dihydro-2H-indol-2-one derivatives with chloroacetyl chloride in the presence of triethyl-amine (TEA). The mechanism involved simple acid or base catalysed reaction through the formation of Schiff base followed by cyclisation via ketene–imine cycloaddition reaction. All synthesized compounds were characterized by FT-IR,1H-NMR,13C-NMR, and elemental analysis. The antimicrobial activities of the synthesized derivatives 5a-5g were examined via Micro Broth Dilution method against bacterial strains Bacillius subtilis, Staphylcoccus aureus, E. coli, P. aeruginosa, and fungal strain Candida albicans for determining MIC values. Ampicillin, chloramphenicol, and griseofulvin were used as standard drugs. The MIC values for antimicrobial activity of synthesized compounds were examined using Micro Broth Dilution method. Compounds 5a, 5b, and 5c were found effective against E. coli (MTCC 442) and P.aeruginosa (MTCC 441) and all compounds showed moderate to excellent activity against Streptococcus aureus (MTCC 96) and Bacillius subtilis (MTCC 441). Regarding the antifungal screening, compounds 5a, 5b, and 5c exhibited excellent activity against Candida albicans MTCC 227. 1-(1,3-benzothiazol-2-yl)-3-chloro-4H-spiro[azetidine-2,3'-indole]-2',4(1'H)-dione derivatives may be used as potential lead molecules as effective antimicrobial agents.
- Agarwal, Dinesh Kr.,Agarwal, Shikha,Gandhi, Divyani,Prajapat, Prakash,Sethiya, Ayushi
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p. 141 - 148
(2020/02/04)
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- Multicomponent one-pot synthesis of substituted 4h-pyrimido [2,1-b] [1,3] benzothiazole curcumin derivatives and their antimicrobial evaluation
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A novel series of ten substituted 4H-pyrimido [2,1-b] [1,3] benzothiazole curcumin derivatives have been synthesized and evaluated for their antimicrobial activity against Gram positive and Gram negative bacteria viz. Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus cereus and against fungi viz. Alternaria solani, Aspergillus niger, Fusarium culmorum and Rhizopus stolonifer. The mechanism involves condensation of substituted benzaldehyde and curcumin via Knovenegal reaction which further reacts with substituted benzothiazole through Michael addition in the presence of pyridine catalyst using methanol as a solvent. The synthesized compounds were analyzed by elemental and spectral analysis.
- Agarwal, Shikha,Agarwal, Dinesh Kr.,Gandhi, Divyani,Goyal, Kshamta,Goyal, Pradeep
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p. 863 - 869
(2018/11/06)
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- Synthesis and in vitro Antimicrobial evaluation of Benzothiazole incorporated Thiazolidin-4-ones derivatives
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In the course of work on new pharmacologically active antimicrobial agents, we have reported the synthesis of a new class of structurally novel derivatives, incorporating two bioactive structures, a benzothiazole and thiazolidin-4-one, to yield a class of
- Agarwal, Shikha,Agarwal, Dinesh Kumar,Gautam, Naveen,Agarwal, Kshamta,Gautam, Dinesh Chandra
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