131052-36-3Relevant academic research and scientific papers
A Convenient One-Pot Synthesis of 1,5-Disubstituted Tetrazoles Containing an Amino or a Carboxy Group
Obushak, M. D.,Pokhodylo, N. T.,Shyyka, O. Ya.
, p. 802 - 812 (2020/07/03)
Abstract: A convenient method is proposed for constructing the tetrazole ring by a one-pot reaction of amides with phosphorus oxychloride and sodium azide. A series of 1,5-disubstituted tetrazoles containing an amino or a carboxy group, which present interest as buildings blocks for the synthesis of biologically active substances, were obtained.
PYRIDAZINONE DERIVATIVES AND USE THEREOF AS P2X7 RECEPTOR INHIBITORS
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Page/Page column 166, (2009/06/27)
Novel pyridazinone compounds of formula (I), which inhibit the purinergic P2X7 receptor and are useful for prevention, therapy and improvement of inflammatory and immunological diseases.
Biologically active amides
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, (2008/06/13)
Novel peptide compounds of the formula are provided together with their acid addition salts and their complexes with pharmaceutically acceptable metals. The compounds are LH-RH analogues and together with their salts and complexes exhibit LH-RH antagonist activity. In the formula X1 is selected from pyroglutamyl, a group V1 -Pro- where V1 is acyl, alkyloxycarbonyl or aralkyloxycarbonyl, and a group V2 --CO-- where V2 is cycloalkyl; X2 is selected from histidyl and a direct bond; X3 is selected from phenylalanyl optionally substituted in the benzene ring and tryptophyl; X4 is selected from glycyl, seryl, alanyl (D- or L), D-leucyl and D-valyl; X5 is phenylalanyl optionally substituted in the benzene ring; X6 is selected from glycyl, alanyl (D- or L-), D-leucyl and D-valyl; X7 is selected from phenylalanyl optionally substituted in the benzene ring and leucyl; X8 is a direct bond when X2 is histidyl and is otherwise arginyl or homoarginyl; and W is selected from glycine amide and a group --NR1 R2 where R1, R2 and the nitrogen atom together comprise a group selected from amino, N-alkylamino, N,N-dialkylamino, pyrrolidino, morpholino and 1-methyl-5-aminomethyltetrazolyl, the `alkyl` having from 1 to 4 carbon atoms and being optionally substituted by an hydroxyl group, provided that, when X1, X3, X4, X5, X7 and X8 are respectively pyroglutamyl, tryptophyl, seryl, tyrosyl, leucyl and arginyl, W is other than glycine amide or N-ethylamino when X6 is glycyl and is other than glycine amide when X6 is D-alanyl. All references are to the L-amino acids and their radicals except in the case of glycine and unless otherwise stated. Also provided are methods for the preparation of the peptides, salts and complexes, pharmaceutical formulations containing them and methods for the preparation of such formulations, and methods for the use of the peptides, salts and complexes in human and in veterinary medicine.
