3-substituted Pyrazoles Research Articles

3-Substituted pyrazole derivatives as inhibitors and inactivators of liver alcohol dehydrogenase

3-Substituted pyrazoles, HOCH2 (1), HOCH2CH2 (2), HOCH2CH2CH2 (3), ClCH2 (4), ClCH2CH2 (5), ClCH2CH2CH2 (6), and CH3CO (7), were synthesized and evaluated in vitro on horse liver alcohol dehydrogenase for their potential as inhibitors of ethanol metabolism. 1 to 6 bound to the enzyme-NAD+ complex with dissociation constants of 40 to 200 microM, much higher than the constants for the corresponding 4-substituted pyrazoles, but with the same absorption maximum at 295 nm. 4 inactivated the enzyme within a few minutes, but NAD+ protected against reaction, and 4 nonspecifically alkylated many sulfur atoms in the protein. The isomer, 4-(chloromethyl)pyrazole, behaved similarly, 5 and 6 strongly inhibited the enzyme in the presence of NAD+, due to formation of the slowly dissociable (10(-3)s-1) enzyme-NAD+-pyrazole complex, but did not irreversibly inactivate the enzyme. 7 inhibits the enzyme weakly (Kp = 5 mM). It appears that the 3-substituted pyrazoles bind to the enzyme-NAD+ complex with the reactive functional group improperly positioned for specific irreversible reaction.

ChemInform Abstract: SYNTHESIS OF α‐D‐ARABINOFURANOSIDES OF SUBSTITUTED PYRAZOLE

Chemischer InformationsdienstVolume 8, Issue 29 Natural Products ChemInform Abstract: SYNTHESIS OF α-D-ARABINOFURANOSIDES OF SUBSTITUTED PYRAZOLE I. A. KORBUKH, I. A. KORBUKHSearch for more papers by this authorL. N. ABRAMOVA, L. N. ABRAMOVASearch for more papers by this authorM. N. PREOBRAZHENSKAYA, M. N. PREOBRAZHENSKAYASearch for more papers by this author I. A. KORBUKH, I. A. KORBUKHSearch for more papers by this authorL. N. ABRAMOVA, L. N. ABRAMOVASearch for more papers by this authorM. N. PREOBRAZHENSKAYA, M. N. PREOBRAZHENSKAYASearch for more papers by this author First published: July 19, 1977 https://doi.org/10.1002/chin.197729356AboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL Share a linkShare onFacebookTwitterLinked InRedditWechat No abstract is available for this article. Volume8, Issue29July 19, 1977 RelatedInformation

ChemInform Abstract: POLAROGRAPHIC ADSORPTION WAVE CHARACTERISTICS OF COPPER COMPLEXES OF SUBSTITUTED PYRAZOLES

Chemischer InformationsdienstVolume 5, Issue 41 Organoelement Compounds ChemInform Abstract: POLAROGRAPHIC ADSORPTION WAVE CHARACTERISTICS OF COPPER COMPLEXES OF SUBSTITUTED PYRAZOLES D. R. CROW, D. R. CROWSearch for more papers by this authorP. K. AGGARWAL, P. K. AGGARWALSearch for more papers by this author D. R. CROW, D. R. CROWSearch for more papers by this authorP. K. AGGARWAL, P. K. AGGARWALSearch for more papers by this author First published: October 15, 1974 https://doi.org/10.1002/chin.197441386AboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL Share a linkShare onFacebookTwitterLinked InRedditWechat No abstract is available for this article. Volume5, Issue41October 15, 1974 RelatedInformation