Antimicrobial Cytidine Derivatives as Anticancer Agents with in Silico Studies | Chapter 9 | Novel Aspects on Chemistry and Biochemistry Vol. 7

 The present study focuses on the computational inquiry of the antibacterial, anticancer, and construction-activity connection (SAR) properties of cytidine and allure analogs. Nucleosides are glycosylamines that can be thinking of as nucleotides without a phosphate group. A nucleoside exists simply of a nucleobase (more termed a nitrogenous base) and a five-element sugar (ribose or 2'-deoxyribose) when in fact a nucleotide is composed of a nucleobase, a five-element sugar, and individual or more phosphate groups. In a nucleoside, the anomeric carbon is connected through a glycosidic bond to the N9 of a purine or the N1 of a pyrimidine. Nucleotides are the microscopic building blocks of DNA and RNA. Nucleoside analogs have a meaningful role in the drug and clinical areas as therapeutic powers and authorized pharmaceuticals. Microdilution persistent the modified analogs' completely clean activity, MIC, and MBC against human and phytopathogenic isolates. Compounds (7), (10), and (14) were ultimate potent against Escherichia coli and Salmonella abony strains, accompanying MIC and MBC values from 0.316 ± 0.02 to 2.50 ± 0.03 and 0.625 ± 0.04 to 5.01 ± 0.06 mg/ml, individually. The highest inhibitory venture was observed against grandam-positive microorganisms. Numerous analogs (10), (13), (14), and (15) exhibited good venture against the tested fungi Aspergillus niger and Aspergillus flavus. The anticancer project of the cytidine analogs was examined through an MTT colorimetric assay against Ehrlich’s ascites malignant growth (EAC) tumor containers, whereas compound 6 granted the maximum antiproliferative activity accompanying an IC50 value of 1168.97 µg/ml. Their microscopic docking studies against the urate oxidase 1R51 from A. flavus look at the binding mechanism, affinities, and nonbonding interplays to define this finding. The most of analogs bind more tightly than the original drug. The reinforced pharmacokinetic profile of cytidine analogs accompanying decreased severe oral toxicity was illustrated by in silico ADMET prediction, that was used to assess the drug-reproduction features. This research power result in the production of potential cytidine-based antimicrobial drug(s) established the in vitro and in silico results.

Author(s) Details:

Sarkar M. A. Kawsar,
Laboratory of Carbohydrate and Nucleoside Chemistry (LCNC), Department of Chemistry, Faculty of Science, University of Chittagong, Chittagong-4331, Bangladesh.

Please see the link here: https://stm.bookpi.org/NACB-V7/article/view/11967