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- W2593992901 abstract "A series of congeners structurally related to pritelivir, N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide, a helicase-primase inhibitor for the treatment of herpes simplex virus infections, was prepared. The synthesized primary and secondary sulfonamides were investigated as inhibitors of six physiologically and pharmacologically relevant human (h) carbonic anhydrase (hCA, EC 4.2.1.1) isoforms, the cytosolic enzymes hCA I and II, the mitochondrial ones hCA VA and VB, and the transmembrane, tumor associated hCA IX and XII. Low nanomolar inhibition KI values were detected for all of them, with a very interesting and well-defined structure–activity relationship. As many CAs are involved in serious pathologies, among which are cancer, obesity, epilepsy, glaucoma, etc., sulfonamide inhibitors as those reported here may be of interest as drug candidates. Furthermore, pritelivir itself is an effective inhibitor of some CAs, also inhibiting whole blood enzymes from several mammalian species, which may be a favorable pharmacokinetic feature of the drug which can be transported throughout the body bound to blood CA I and II." @default.
- W2593992901 created "2017-03-16" @default.
- W2593992901 creator A5004728480 @default.
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- W2593992901 creator A5081648093 @default.
- W2593992901 date "2017-03-17" @default.
- W2593992901 modified "2023-10-14" @default.
- W2593992901 title "Lead Development of Thiazolylsulfonamides with Carbonic Anhydrase Inhibitory Action" @default.
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- W2593992901 doi "https://doi.org/10.1021/acs.jmedchem.7b00183" @default.
- W2593992901 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/28272885" @default.
- W2593992901 hasPublicationYear "2017" @default.
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