43201-13-4Relevant academic research and scientific papers
1,2,4- THIADIAZOL-5-THIO COMPOUNDS AND THE DERIVATIVES THEREOF, METHODS FOR THE PRODUCTION THEREOF AND USE THEREOF AS UREASE AND NITRIFICATION INHIBITORS
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Page/Page column 16, (2008/06/13)
The invention relates to methods for the production and use of novel 1,2,4-thiadiazols of general formulae (I) or (II) as agents for regulating the inhibition of enzymatic urea hydrolysis, wherein R1 = hydrogen, C1-C8-alkyl or C6-C10-aryl and R2 = hydrogen, C1-C8- alkyl/heteroalkyl, C2-C8 -alkenyl/heteroalkenyl, C2-C8 -alkinyl/heteroalkinyl, C3-C8- cycloalkyl/heterocycloalkyl, C3-C8 -cycloalkenyl/heterocycloalkenyl, C6-C10 -aryl/heteroaryl, aralkyl, heteroarylalkyl, alkaryl, akheteroaryl, alkoxy, aryloxy, hetaryloxy, alkylthio, arylthio, hetarylthio, acyl, aroyl, hetaroyl, acyloxy, aroyloxy, hetaroyloxy, alkoxycarbonyl, aryloxycarbonyl, hetaryloxycarbonyl, amino, alkylamino, dialkylamino, alkylsulfonyl, arylsulfonyl, fluorine, chlorine, bromine, iodine, hydroxy, cyano, nitro, sulfo, carbonyl, carboxy, carbamoyl, sulfamoyl, the radicals R1 and/or R2 can, optionally, be per se and individually substituted by one or several of the above-mentioned groups. With a limited spectrum of substituents in R2, said compounds can be claimed as nitrification inhibitors. The inventive 1,2,4-thiadiazols thus used are effective urease inhibitors and have a good resistance to hydrolysis and can be produced according to known methods. They are also effective nitrification inhibitors and can delay transformation of ammonia. They are the first inhibitors which effectively eliminate the two main sources of loss during the application of manure, i.e. urease-catalyzed urea hydrolysis and nitrification of ammonia nitrogen. The inventive compounds can also be combined with more potent nitrification inhibitors, whereby nitrogen losses can also be reduced, without any problem.
studies on anti-helicobacter pylori agents. Part 2: New cephem derivatives
Yoshida, Yoshiki,Matsuda, Keiji,Sasaki, Hiroshi,Matsumoto, Yoshimi,Matsumoto, Satoru,Tawara, Shuichi,Takasugi, Hisashi
, p. 2317 - 2335 (2007/10/03)
The synthesis and optimization of the anti-Helicobacter pylori activity of a novel series of cephem derivatives are described. Introduction of thio-heterocyclic groups containing N- and S-atoms to the 3-position and phenyl or thienyl acetamido groups to the 7-position of the cephem nucleus dramatically improved the activity. From this series of derivatives, compound 13i was found to have extremely potent in vitro anti-H. pylori activity, superior therapeutic efficacy compared to AMPC and CAM, no cross-resistance between CAM or MNZ and low potential for causing diarrhea due to instability to β-lactamase. Copyright (C) 2000 Elsevier Science Ltd.
