73728-55-9Relevant academic research and scientific papers
Synthesis and biological evaluation of aminothiazoles against Histoplasma capsulatum and Cryptococcus neoformans
Ishita, Keisuke,Stefanopoulos, Stavros,Khalil, Ahmed,Cheng, Xiaolin,Tjarks, Werner,Rappleye, Chad A.
supporting information, p. 2251 - 2261 (2018/03/29)
The design and synthesis of a library of forty novel 2-aminoazole analogues as well as their evaluation as antifungal compounds against Histoplasma capsulatum and Cryptococcus neoformans is described. These structures were derived from N-[5-(1-naphthaleny
Thio-substituted tricyclic and bicyclic aromatic methanesulfinyl derivatives
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Page/Page column 26, (2008/06/13)
The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, Y, R1 and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder ("ADHD"), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.
Beta-thiopropionyl-amino acid derivatives and their use as beta-lactamase inhibitors
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, (2008/06/13)
PCT No. PCT/EP97/05709 Sec. 371 Date Apr. 7, 1999 Sec. 102(e) Date Apr. 7, 1999 PCT Filed Oct. 10, 1997 PCT Pub. No. WO98/17639 PCT Pub. Date Apr. 30, 1998Mercapto amino acid derivatives of formula (I), wherein R is hydrogen, a salt-forming cation of a in vivo hydrolysable ester-forming group; R1 is selected from (a) and (b) in which A is a monocyclic aryl or heteroaryl ring and B is a monocyclic aryl, alicyclic or heterocyclic ring, C and D are independently -Zp-(CR8CR9)q- or -(CR8CR9)q-Zp- where p is 0 or 1, q is 0 to 3 provided that p+q in C is not 0, R8 and R9 are independently hydrogen or (C1-6)alkyl or together represent oxo and Z is O, NR10 or S(O)x where R10 is hydrogen, (C1-6)alkyl or aryl(C1-6)alkyl and x is 0-2, and wherein C and D are linked ortho to one another on each of the rings A and B in formula (b); R2 is hydrogen, (C1-6)alkyl or aryl(C1-6)alkyl; R3 is hydrogen, (C1-6)alkyl optionally substituted by up to three halogen atoms, (C3-7)cycloalkyl, fused aryl(C3-7)cycloalkyl, (C3-7)cycloalkyl(C2-6)alkyl, (C2-6)alkenyl, (C2-6)alkynyl, aryl, aryl-(CH2)m-X-(CH2)n, heterocyclyl or heterocyclyl-(CH2)m-X-(CH2)n, where m is 0 to 3, n is 1 to 3 and X is O or S(O)x where x is 0-2 or a bond; R4 is hydrogen or an in vivo hydrolysable acyl group; and R5 and R6 are independently hydrogen and (C1-6)alkyl or together represent (CH2)r, where r is 2 to 5; for use in treatment of bacterial infections in humans or animals by administration in combination with a beta -lactam antiobiotic.
Intramolecular reactivity of functionalized arylcarbenes: 1-(Hydroxymethyl)-9-fluorenylidene
Kirmse, Wolfgang,Krzossa, Birgit
, p. 799 - 802 (2007/10/03)
Photolyses of 9-diazo-1-fluorenylmethanol (22) in benzene or MeCN afford ≤95% of fluorene-1-carbaldehyde (14). In methanol, 14 and 9-methoxy-1-fluorenylmethanol (24) are formed competitively from 22. Intramolecular hydrogen transfer of triplet 1-(hydroxymethyl)-9-fluorenylidene (12) appears to be the major reaction path leading to 14. The photoenol 13 is suggested as an intermediate.
SAR of novel biarylmethylamine dopamine D4 receptor ligands
Arlt, Michael,Boettcher, Henning,Riethmueller, Angelika,Schneider, Guenter,Bartoszyk, Gerd D.,Greiner, Hartmut,Seyfried, Christoph A.
, p. 2033 - 2038 (2007/10/03)
SAR for a novel series of dopamine D4 receptor ligands is shown. Very selective, highly potent compounds like 1-(2-pyrimidinyl)-4-(3-(3-thienyl)- benzyl)-piperazine (5f) and 2-(4-(1-fluorenylmethyl)-1-piperazinyl)- pyrimidine (8c) were obtained.
SYNTHESIS OF TRICYCLIC BENZAZEPINES AND THEIR DOPAMINE D1- AND D2-AFFINITY
Horn Jensen, Eva,Nielsen, Per Halfdan
, p. 2441 - 2458 (2007/10/03)
A new group of angular 8,9-annelated 3-benzazepines has been found to be potent and selective dopamine D1-receptor antagonists of interest as possible pharmaceuticals in the treatment of schizophrenia.The synthesis of three new conformationally constrained representatives of this group of benzazepines is described and their affinity to the D1-receptor evaluated.Although none of these proved superior to the previously examined compounds, useful information on the receptor binding site was obtained.
Method for treating inflammation and compounds and compositions suitable for use therein
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, (2008/06/13)
The present invention relates to a method of treating an inflammatory condition, and to compounds and composition suitable for use in such a method, which compounds have the Formula: STR1 wherein: X is methylene, ethylene, ethyleneoxy, or oxygen; Q is STR2 where C' is a residue of a lipophilic amino acid, and Y is --CO2 H, --CH2 OH, --CONR1 R2, or --CO2 R1 where R1 and R2 hydrogen, alkyl, or aryl; R3 and R4 are, independently, hydrogen, alkyl or aryl; and A and B are, independently, hydrogen, fused phenyl, alkyl, aryl, alkaryl, aralkyl, alkoxy, alkoxyalkyl, halogen, or nitro; or pharmaceutically acceptable salts thereof.
