Recommanded Product: 100-19-6. Welcome to talk about 100-19-6, If you have any questions, you can contact Andleeb, H; Hameed, S; Ejaz, SA; Khan, I; Zaib, S; Lecka, J; Sevigny, J; Iqbal, J or send Email.
Recommanded Product: 100-19-6. Andleeb, H; Hameed, S; Ejaz, SA; Khan, I; Zaib, S; Lecka, J; Sevigny, J; Iqbal, J in [Andleeb, Hina; Hameed, Shahid; Khan, Imtiaz] Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan; [Andleeb, Hina] Int Islamic Univ, Fac Basic & Appl Sci, Sulaiman Bin Abdullah Aba Al Khail Ctr Interdisci, Islamabad, Pakistan; [Ejaz, Syeda Abida; Zaib, Sumera; Iqbal, Jamshed] COMSATS Inst Informat Technol, Ctr Adv Drug Res, Abbottabad 22060, Pakistan; [Khan, Imtiaz] Univ Manchester, Sch Chem, Oxford Rd, Manchester M13 9PL, Lancs, England; [Khan, Imtiaz] Univ Manchester, Manchester Inst Biotechnol, 131 Princess St, Manchester M1 7DN, Lancs, England; [Lecka, Joanna; Sevigny, Jean] Univ Laval, Fac Med, Dept Microbiol Infectiol & Immunol, Quebec City, PQ G1V 0A6, Canada; [Lecka, Joanna; Sevigny, Jean] Univ Laval, CHU Quebec, Ctr Rech, Quebec City, PQ G1V 4G2, Canada published Probing the high potency of pyrazolyl pyrimidinetriones and thioxopyrimidinediones as selective and efficient non-nucleotide inhibitors of recombinant human ectonucleotidases in 2019.0, Cited 52.0. The Name is 1-(4-Nitrophenyl)ethanone. Through research, I have a further understanding and discovery of 100-19-6.
With the aim to discover novel, efficient and selective inhibitors of human alkaline phosphatase and nucleotide pyrophosphatase enzymes, two new series of pyrazolyl pyrimidinetriones (PPTs) (6a-g) and thioxopyrimidinediones (PTPs) (6h-n) were synthesized in good chemical yields using Knoevenagel condensation reaction between pyrazole carbaldehydes (4a-g) and pharmacologically active N-alkylated pyrimidinetrione (5a) and thioxopyrimidinedione (5b). The inhibition potential of the synthesized hybrid compounds was evaluated against human alkaline phosphatase (h-TNAP and h-IAP) and ectonucleotidase (h-NPP1 and h-NPP3) enzymes. Most of the tested analogs were highly potent with a variable degree of inhibition depending on the functionalized hybrid structure. The detailed structure-activity relationship (SAR) of PPT and PTP derivatives suggested that the compound with unsubstituted phenyl ring from PPT series led to selective and potent inhibition (6a; IC50= 0.33 +/- 0.02 mu M) of h-TNAP, whereas compound 6c selectively inhibited h-IAP isozyme with IC50 value of 0.86 +/- 0.04 mu M. Similarly, compounds 6b and 6h were identified as the lead scaffolds against h-NPP1 and h-NPP3, respectively. The probable binding modes for the most potent inhibitors were elucidated through molecular docking analysis. Structure-activity relationships, mechanism of action, cytotoxic effects and druglikeness properties are also discussed.
Recommanded Product: 100-19-6. Welcome to talk about 100-19-6, If you have any questions, you can contact Andleeb, H; Hameed, S; Ejaz, SA; Khan, I; Zaib, S; Lecka, J; Sevigny, J; Iqbal, J or send Email.
Reference:
Benzodioxan,
,1,4-Benzodioxane | C8H8O2 – PubChem