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'uncouplers' in keywords Facet   Publication Year 1975  [X]
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1975[X]
1Author    G. Schäfer, A. Trebst, K. H. BüchelRequires cookie*
 Title    2-Anilino-1.3.4-thiadiazole, Hemmstoffe der oxidativen und photosynthetischen Phosphorylierung 2-Anilino-l,3,4-Thiadiazoles, Inhibitors of Oxidative and Photosynthetic Phosphorylation  
 Abstract    2-anilino-l,3,4-thiadiazoles carrying various substituents in the 5-position as well as in the benzene-ring were synthesized. The compounds were tested with rat-liver-mitochondria and with spinach-chloroplasts and revealed to be potent uncouplers of both, oxidative and photosynthetic phosphorylation, with p l50-values rangeing from 6.79 to 4.05. At higher concentration all compounds are inhibitors of the Hill-reaction. In mitochondria a fair correlation exists between pKa of the acidic NH-group and the un­ coupling activity; a maximum is obtained around pKa= 6 .8 , whereas in chloroplasts activity is shifted to more acid pKa-values. The compounds meet the requirements for uncouplers according to the chemi-osmotic theory, being lipophilic weak acids. N-methylation causes total loss of activity in mitochondrial oxidative phosphorylation. The inhibitory action on photosynthetic electron transport is located within photosystem II. This latter activity is almost independent of substituent effects in contrast to uncoupling of either respiratory-or photo-phosphorylation. 
  Reference    (Z. Naturforsch. 30c, 183 [1975]; eingegangen am 19. Dezember 1974) 
  Published    1975 
  Keywords    Oxidative Phosphorylation, Photophosphorylation, Uncouplers, Structure-function Correlation 
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 TEI-XML for    default:Reihe_C/30/ZNC-1975-30c-0183.pdf 
 Identifier    ZNC-1975-30c-0183 
 Volume    30