SDS of cas: 100-19-6. Recently I am researching about ALKALINE-PHOSPHATASE; BIOLOGICAL EVALUATION; PHOSPHODIESTERASE-I; DERIVATIVES; PROTEIN; IDENTIFICATION; AGENTS; CALCIFICATION; LOCALIZATION; THIAZOLES, Saw an article supported by the Higher Education Commission of PakistanHigher Education Commission of Pakistan; DAAD (Programm Deutsch-Pakistanische Hochschulzusammenarbeit); Organization for the Prohibition of Chemical Weapons (OPCW), The Hague, The NetherlandsNetherlands Government; Higher Education Commission of PakistanHigher Education Commission of Pakistan [20-3733/NRPU/RD/14/520]; Canadian Institutes of Health ResearchCanadian Institutes of Health Research (CIHR); Fonds de recherche du Quebec-Sante (FRQS). Published in ACADEMIC PRESS INC ELSEVIER SCIENCE in SAN DIEGO ,Authors: Andleeb, H; Hameed, S; Ejaz, SA; Khan, I; Zaib, S; Lecka, J; Sevigny, J; Iqbal, J. The CAS is 100-19-6. Through research, I have a further understanding and discovery of 1-(4-Nitrophenyl)ethanone
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.
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Reference:
Benzodioxan,
,1,4-Benzodioxane | C8H8O2 – PubChem