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Synlett
DOI: 10.1055/a-2602-6763
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Pyrimidine Carboxylic Acids Linked through 1,4,5-Trisubstituted 1,2,3-Triazoles: Synthesis and RNase A Inhibition Studies

Kaustav Chakraborty
1   Chemistry, Indian Institute of Technology Kharagpur, Kharagpur, India (Ringgold ID: RIN30133)
,
Swagata Dasgupta
1   Chemistry, Indian Institute of Technology Kharagpur, Kharagpur, India (Ringgold ID: RIN30133)
,
Tanmaya Pathak 
1   Chemistry, Indian Institute of Technology Kharagpur, Kharagpur, India (Ringgold ID: RIN30133)
› Author AffiliationsSupported by: Department of Biotechnology, Ministry of Science and Technology, New Delhi project no. SB/S1/OC-30/2014
Supported by: none
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A series of triazolylated nucleoside carboxylic acid derivatives has been synthesized using 1,3-dipolar cycloaddition reaction. The Ribonuclease A (RNase A) inhibitory property of the synthesized molecules has been studied by experimental as well as theoretical techniques. The compounds were found to inhibit RNase A in a reversible competitive manner. The inhibitory potency was significantly enhanced with the incorporation of a larger number of carboxylic acid groups in the inhibitor. A theoretical justification of the observed results has been demonstrated by investigating the docked structures of the enzyme-inhibitor complexes.



Publication History

Received: 21 February 2025

Accepted after revision: 07 May 2025

Accepted Manuscript online:
07 May 2025

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