FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W4210369736> ?p ?o ?g. }

• W4210369736 abstract "Pyrido[2,3-d]pyrimidine-2,4(1H,3H)-diones were synthesized, for the first time, from indole chalcones and 6-aminouracil, and their ability to inhibit leishmaniasis and tuberculosis (Tb) infections was evaluated. The in vitro antileishmanial activity against promastigotes of Leishmania donovani revealed exceptional activities of compounds 3, 12 and 13, with IC50 values ranging from 10.23 ± 1.50 to 15.58 ± 1.67 µg/ml, which is better than the IC50 value of the standard drug pentostam of 500 μg/ml. The selectivity of the compounds towards Leishmania parasites was evaluated via ex vivo studies in Swiss albino mice. The efficiency of these compounds against Tb infection was then evaluated using the in vitro anti-Tb microplate Alamar Blue assay. Five compounds, 3, 7, 8, 9 and 12, showed MIC100 values against the Mycobacterium tuberculosis H37 Rv strain at 25 µg/ml, and compound 20 yielded an MIC100 value of 50 µg/ml. Molecular modelling of these compounds highlighted interactions with binding sites of dihydrofolate reductase, pteridine reductase and thymidylate kinase, thus establishing the rationale of their pharmacological activity against both pathogens, which is consistent with the in vitro results. From the above results, it is clear that compounds 3 and 12 are promising lead candidates for Leishmania and Mycobacterium infections and may be promising for coinfections." @default.
• W4210369736 created "2022-02-08" @default.
• W4210369736 creator A5002886899 @default.
• W4210369736 creator A5014650986 @default.
• W4210369736 creator A5034502331 @default.
• W4210369736 creator A5034613514 @default.
• W4210369736 creator A5037277002 @default.
• W4210369736 creator A5047237761 @default.
• W4210369736 creator A5049197977 @default.
• W4210369736 creator A5085931640 @default.
• W4210369736 creator A5090080837 @default.
• W4210369736 creator A5054492145 @default.
• W4210369736 date "2022-02-01" @default.
• W4210369736 modified "2023-10-10" @default.
• W4210369736 title "First‐in‐class pyrido[2,3‐<i>d</i>]pyrimidine‐2,4(1<i>H</i>,3<i>H</i>)‐diones against leishmaniasis and tuberculosis: Rationale, in vitro, ex vivo studies and mechanistic insights" @default.
• W4210369736 cites W1495809390 @default.
• W4210369736 cites W1504899110 @default.
• W4210369736 cites W1549911162 @default.
• W4210369736 cites W1603625551 @default.
• W4210369736 cites W1843371601 @default.
• W4210369736 cites W1906600722 @default.
• W4210369736 cites W1975492167 @default.
• W4210369736 cites W1976163006 @default.
• W4210369736 cites W1980191878 @default.
• W4210369736 cites W1983606421 @default.
• W4210369736 cites W1988149555 @default.
• W4210369736 cites W2000351383 @default.
• W4210369736 cites W2003602993 @default.
• W4210369736 cites W2006567450 @default.
• W4210369736 cites W2007721552 @default.
• W4210369736 cites W2008403530 @default.
• W4210369736 cites W2008684950 @default.
• W4210369736 cites W2010576440 @default.
• W4210369736 cites W2012297516 @default.
• W4210369736 cites W2018582033 @default.
• W4210369736 cites W2018752901 @default.
• W4210369736 cites W2021823985 @default.
• W4210369736 cites W2025897779 @default.
• W4210369736 cites W2026178918 @default.
• W4210369736 cites W2030174273 @default.
• W4210369736 cites W2033120249 @default.
• W4210369736 cites W2033695597 @default.
• W4210369736 cites W2048435189 @default.
• W4210369736 cites W2048688989 @default.
• W4210369736 cites W2050197274 @default.
• W4210369736 cites W2052032843 @default.
• W4210369736 cites W2054159557 @default.
• W4210369736 cites W2063207123 @default.
• W4210369736 cites W2082684548 @default.
• W4210369736 cites W2085363005 @default.
• W4210369736 cites W2090642051 @default.
• W4210369736 cites W2094052123 @default.
• W4210369736 cites W2104211072 @default.
• W4210369736 cites W2105058945 @default.
• W4210369736 cites W2105105987 @default.
• W4210369736 cites W2105649494 @default.
• W4210369736 cites W2113777272 @default.
• W4210369736 cites W2124017621 @default.
• W4210369736 cites W2124398283 @default.
• W4210369736 cites W2126576359 @default.
• W4210369736 cites W2151823004 @default.
• W4210369736 cites W2154885738 @default.
• W4210369736 cites W2155632442 @default.
• W4210369736 cites W2160723017 @default.
• W4210369736 cites W2166824666 @default.
• W4210369736 cites W2173181090 @default.
• W4210369736 cites W2182593958 @default.
• W4210369736 cites W2263469841 @default.
• W4210369736 cites W2321980425 @default.
• W4210369736 cites W2407040666 @default.
• W4210369736 cites W2521282568 @default.
• W4210369736 cites W2529242276 @default.
• W4210369736 cites W254422662 @default.
• W4210369736 cites W2554309767 @default.
• W4210369736 cites W2566541501 @default.
• W4210369736 cites W2577184123 @default.
• W4210369736 cites W2786275130 @default.
• W4210369736 cites W2792501878 @default.
• W4210369736 cites W2802224675 @default.
• W4210369736 cites W2802251588 @default.
• W4210369736 cites W2804538994 @default.
• W4210369736 cites W2805761887 @default.
• W4210369736 cites W2806721450 @default.
• W4210369736 cites W2808223966 @default.
• W4210369736 cites W2889861811 @default.
• W4210369736 cites W2897075077 @default.
• W4210369736 cites W2897968199 @default.
• W4210369736 cites W2900723132 @default.
• W4210369736 cites W2908152294 @default.
• W4210369736 cites W2912048033 @default.
• W4210369736 cites W2933745292 @default.
• W4210369736 cites W2939016188 @default.
• W4210369736 cites W2941757011 @default.
• W4210369736 cites W2942626681 @default.
• W4210369736 cites W2946697697 @default.
• W4210369736 cites W2951090471 @default.
• W4210369736 cites W2952290160 @default.
• W4210369736 cites W2952853804 @default.
• W4210369736 cites W2979957800 @default.
• W4210369736 cites W3018721272 @default.

• next