摘要:
Novel 5,8-dihydro-8-oxo-1,3-dioxolo[4,5-g]quinoline-7-carboxylic acids substituted in the 5-position by lower-alkylamino or di-lower-alkylamino, useful as antibacterial agents, are prepared from 8-hydroxy-1,3-dioxolo[4,5-g]quinoline-7-carboxylic acid or a lower-alkyl ester thereof via a series of novel intermediates.
摘要:
Compounds of the formula ##STR1## wherein R is hydrogen or formyl; and R' and R" are hydrogen or lower-alkyl, are useful as antibacterial agents or as intermediates, and are prepared from the corresponding compounds unsubstituted in the 1-position.
摘要:
Novel 1-R-1,4-dihydro-4-oxo-6-fluoro-7-(Z.dbd.N--)-quinolinecarboxylic acids and esters thereof, where R is amino, lower-alkylamino, 2-propenylamino or di-lower-alkylamino, R" is hydrogen or lower-alkyl, and Z.dbd.N is a heterocyclic group, useful as antibacterial agents, are prepared by reacting the corresponding 7-chloroquinoline derivatives with the appropriate heterocyclic compound, Z.dbd.NH. A preferred group of compounds are those where Z.dbd.N is 1-piperazinyl or 4-lower-alkyl-1-piperazinyl.
摘要:
N-[alkylamino)alkyl]-3,4(or 4,5)-diaryl-1H-pyrazole-1-(branched)alkanamides and pyrazole-1-alkanamines useful for treating cardiac arrhythmias in mammals, are prepared by reacting a lower-alkyl ester of pyrazole-1-acetic acid with an appropriate diamine followed by reduction or by reacting the anion of a lower-alkyl ester of a pyrazole-1-acetic acid with an alkylating agent followed by displacement of the ester by an appropriate amine.
摘要:
N-[1-alkyl or arylmethyl)-4(1H)-pyridinylidine]-alkanamine and pharmaceutically acceptable acid addition salts thereof, for example, N-(1-octyl-4(1H)-pyridinylidine)-octanamine monohydrochloride salt, which are useful as antimicrobial agents, especially on living tissues and nonliving surfaces and most especially against pathogenic dental microbes, and a process for perparation, methods of use and compositions thereof are disclosed.
摘要:
The method of providing cytoprotection of the gastric mucosa in a mammal receiving aspirin (ASA) perorally which comprises orally administering either prior to or in combination with ASA a cytoprotectively effective amount of 3,3'-thiobis[propanoic acid] (TBPA) or in combination with a pharmaceutically acceptable carrier. Also shown is a composition for providing cytoprotection of the gastric mucosa in a mammal receiving ASA perorally which comprises ASA in combination with a cytoprotectively effective amount of TBPA.
摘要:
Novel 2-(hydroxyphenylamino)benzamides and oxidation products thereof, useful as inhibitors of lipoxygenase, are of the formulas ##STR1## wherein R is hydrogen, lower-alkyl, halo or lower-alkoxy; R' is hydrogen or lower-alkyl; R" is hydrogen, lower-alkyl or halo; and N.dbd.Z is amino or substituted amino. The compounds of Formula I are prepared by de-etherification of the corresponding alkyl or benzyl ethers; and the compounds of Formula II are prepared by oxidation of the compounds of Formula I where R' is hydrogen and OH is in the 4-position.
摘要:
.alpha.,.alpha.'-Bis-[4-(R-amino)-1-pyridinium]xylenes are prepared by reacting a 4-(R-amino)pyridine with an appropriate .alpha.,.alpha.'-disubstituted xylene. The compounds are useful as antibacterial and antifungal agents.
摘要:
N-[(alkylamino)alkyl]-4,5-diaryl-1H-imidazole-1-acetamides useful for treating cardiac arrhythmias in mammals, are prepared by reacting a lower-alkyl ester of a diaryl imidazole-1-acetic acid with an appropriate diamine.
摘要:
Novel lower-alkyl 2-(hydroxyphenylamino)benzoates, useful as inhibitors of lipoxygenase, are of the formula ##STR1## wherein R is hydrogen, lower-alkyl or lower-alkoxy; R' is hydrogen or lower-alkyl; R" is hydrogen, lower-alkyl or halo; and Alk is lower-alkyl. The compounds are prepared by de-etherification of the corresponding alkyl or benzyl ethers.