H2-Antihistaminika, 6. Mitt. Synthese und Wirkung N-substituierter 4-[(2-Amino-ethylmercapto)-methyl]-imidazole
作者:Rainer Barzen、Walter Schunack
DOI:10.1002/ardp.19803130610
日期:——
Es wurden die N‐substituierten 4‐[(2‐Amino‐ethylmercapto)‐methyl]‐imidazole 2 und 3 dargestellt und auf histaminartige Wirkung untersucht. Die Thioharnstoff‐ und Cyanoguanidin‐Derivate von 3b zeigten keine H2‐antihistaminische Wirksamkeit.
Es wurden die N-substituierten 4-[(2-Amino-ethylmercapto)-methyl]-imidazole 2 und 3 dargestellt und auf histaminartige Wirkung untersucht。Die Thioharnstoff- 和 Cyanoguanidin-Derivate von 3b zeigten keine H2-antihistaminische Wirksamkeit。
Ion Exchange Studies of Transguanylation Reactions. II. Rearrangement of 3-Aminopropylisothiourea and N-Substituted Aminoethyl- and Aminopropylisothioureas to Mercaptoalkylguanidines and 2-Aminothiazolines or Penthiazolines
作者:Joseph X. Khym、David G. Doherty、Raymond Shapira
DOI:10.1021/ja01546a038
日期:1958.7
intratransguanylation is dependent on pH as well as on the number of carbon atoms between the amino and isothiourea groups. The aminoethyl- and aminopropylisothioureas intratransguanylate readily at neutral pH but 5,4- aminobutylisothiourea does not. At pH's 3--6, 2-aminothiazolines and - penthiazolines are formed, whereas in strong ailali, mixtures of mercaptoguanidines and mercaptoamines are formed. NAlkyl substitution
<i>C</i>-Nucleosides and related compounds. XV. The synthesis of <scp>D</scp>,<scp>L</scp>-2′-<i>epi</i>-showdomycin and <scp>D</scp>,<scp>L</scp>-showdomycin
作者:George Just、T. J. Liak、Mu-Ill Lim、Pierre Potvin、Youla S. Tsantrizos
DOI:10.1139/v80-322
日期:1980.10.1
The conversion of the Diels–Alder adduct of methyl β-nitroacrylate with furan to the title compounds and to D,L-2,5-anhydroglucose derivatives is described.
6,7-Dichloro-2,3-dihydro-2-benzo[b]furancarboxylic acidderivatives having a 3,3-N,S-disubstituted-2-propenoyl group at the 5-position were prepared by alkylation of 5-(thiocarbamoyl)acetylderivatives of the 2,3-dihydro-2-benzo[b]furancarboxylic acidester or by acetal exchange reaction of 5-[3,3-bis(alkylthio)-2-propenoyl] derivatives. Synthesis of 5-[4 and/or 5-(di)substituted-4-thiazolin-2-ylidene]acetyl-2
Soft Drugs V: Thiazolidine-Type Derivatives of Progesterone and Testosterone
作者:Nicholas Bodor、Kenneth B. Sloan
DOI:10.1002/jps.2600710509
日期:1982.5
Progesterone and testosterone are natural softdrugs, but to be used as drugs, their fast and facile metabolism must be prevented and their delivery controlled. A prodrug-soft drug combination can serve this purpose. Thiazolidines of testosterone, testosterone 17-propionate and progesterone were synthesized from the reaction of cysteine alkyl esters, N-methylaminoethanethiol, and mercaptamine and their