Substituted hexahydrobenzodipyrans as 5-HT2A/2C receptor probes
摘要:
A pair of substituted hexahydrobenzodipyrans was designed as molecular probes for determining the steric restrictions of the agonist binding site of serotonin 5-HT2A and 5-HT2C receptors. The rationale for the design of these receptor ligands, their chemical synthesis, rat behavioral pharmacology in the two-lever drug discrimination assay using LSD-trained rats, affinity for cloned rat 5-HT2A and 5-HT2c receptors and agonist functional activities are reported. (C) 2002 Elsevier Science Ltd. All rights reserved.
The present disclosure relates to certain new and known triazolium and/or imidazolium salts and to their therapeutic use, for example in methods of treating or preventing an infection by a
Plasmodium
or
Babesia
parasite in a subject in need thereof. The triazolium and imidazolium salts are compounds of the Formula (I) or (II): wherein R
1
-R
4
, R
1′
-R
3′
, R
8
-R
11
, X, X′, X″, Y, Y′ and Y″ are as defined in the disclosure.
Amphiphilic molecules linked by an aromatic nucleus were developed that showed high selectivity toward bacteria over mammalian cells, and lowdrugresistance. A promising compound 4g exhibited strong bactericidal activity against a panel of sensitive and resistant bacteria, low toxicity, the ability to reduce cell viability in biofilms, stability in mammalian fluids, rapid killing of pathogens, and
4-(Aryloxyalkyl)pyrazoles of the formula ##STR1## useful as antiviral agents, are prepared by reacting the corresponding diketones of the formula Ar--O--Alk--CH(COR')COR" with hydrazine or a substituted hydrazine H.sub.2 NNHR. Mono- or bis-pyrazoles are similarly obtained from bis-diketones of the formula ##STR2##
diphenyl- and dimethylglycolurils were synthesized. Sequential treatment of these compounds with imidazole, methyl iodide, and sodium tetrafluoroborate gave their corresponding tetra imidazolium salts. Some of these compounds because of their low melting points can be registered as a potential and new class of ionic liquids.
resistance to antibiotics constitutes an important and growing public health threat, and novel antibiotics are urgently needed. In this report, a series of symmetrical membrane-active agents linked by an aromatic nucleus were designed and synthesized. Some showed high antibacterial activity against clinical drug-resistant bacterial isolates including methicillin-resistant Staphylococcus aureus (MRSA)