97941-89-4Relevant academic research and scientific papers
2,3-Dihydro-6,7-dichloro-pyrido[2,3-b]pyrazine-8-oxide as selective glycine antagonist with in vivo activity
Micheli, Fabrizio,Cugola, Alfredo,Donati, Daniele,Missio, Andrea,Pecunioso, Angelo,Reggiani, Angelo,Tarzia, Giorgio
, p. 2129 - 2132 (1997)
2,3-Dihydro-6,7-dichloro-pyrido[2,3-b]pyrazine-8-oxide was synthesized and evaluated for in vitro/in vivo antagonistic activity at the strychnine insensitive glycine binding site on the NMDA receptor revealing it to be a useful tool to evaluate the effectiveness of glycine antagonists in vivo.
Synthesis of new imidazopyridine nucleoside derivatives designed as maribavir analogues
Papadakis, Georgios,Gerasi, Maria,Snoeck, Robert,Marakos, Panagiotis,Andrei, Graciela,Lougiakis, Nikolaos,Pouli, Nicole
, (2020/10/18)
The strong inhibition of Human Cytomegalovirus (HCMV) replication by benzimidazole nucleosides, like Triciribine and Maribavir, has prompted us to expand the structure-activity relationships of the benzimidazole series, using as a central core the imidazo[4,5-b]pyridine scafflold. We have thus synthesized a number of novel amino substituted imidazopyridine nucleoside derivatives, which can be considered as 4-(or 7)-aza-d-isosters of Maribavir and have evaluated their potential antiviral activity. The target compounds were synthesized upon glycosylation of suitably substituted 2-aminoimidazopyridines, which were prepared in six steps starting from 2-amino-6-chloropyridine. Even if the new compounds possessed only a slight structural modification when compared to the original drug, they were not endowed with interesting antiviral activity. Even so, three derivatives showed promising cytotoxic potential.
Discovery of a Novel Highly Selective Histamine H4 Receptor Antagonist for the Treatment of Atopic Dermatitis
Ko, Kwangseok,Kim, Hye-Jung,Ho, Pil-Su,Lee, Soon Ok,Lee, Ji-Eun,Min, Cho-Rong,Kim, Yu Chul,Yoon, Ju-Han,Park, Eun-Jung,Kwon, Young-Jin,Yun, Jee-Hun,Yoon, Dong-Oh,Kim, Jung-Sook,Park, Woul-Seong,Oh, Seung-Su,Song, Yu-Mi,Cho, Woon-Ki,Morikawa, Kazumi,Lee, Kyoung-June,Park, Chan-Hee
supporting information, p. 2949 - 2961 (2018/04/23)
The histamine H4 receptor (H4R), a member of the G-protein coupled receptor family, has been considered as a potential therapeutic target for treating atopic dermatitis (AD). A large number of H4R antagonists have been disclosed, but no efficient agents controlling both pruritus and inflammation in AD have been developed yet. Here, we have discovered a novel class of orally available H4R antagonists showing strong anti-itching and anti-inflammation activity as well as excellent selectivity against off-targets. A pharmacophore-based virtual screening system constructed in-house successfully identified initial hit compound 9, and the subsequent homology model-guided optimization efficiently led us to discover pyrido[2,3-e]tetrazolo[1,5-a]pyrazine analogue 48 as a novel chemotype of a potent and highly selective H4R antagonist. Importantly, orally administered compound 48 exhibits remarkable efficacy on antipruritus and anti-inflammation with a favorable pharmacokinetic (PK) profile in several mouse models of AD. Thus, these data strongly suggest that our compound 48 is a promising clinical candidate for treatment of AD.
Azabenzimidazole derivative having AMPK-activating activity
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, (2017/03/08)
Disclosed is a compound which is useful as an AMPK activator. A compound represented by formula: or a pharmaceutically acceptable salt thereof, wherein R4 is hydrogen, or substituted or unsubstituted alkyl, R1, R2 and R3 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl or the like, with the proviso that R1, R2 and R3 are not simultaneously hydrogen, X is a single bond, —S—, —O—, —NR5—, —C(═O)— or the like, R5 is hydrogen, or substituted or unsubstituted alkyl, Y is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heterocyclyl or the like.
NOVEL HETEROCYCLIC DERIVATIVES AND THEIR USES
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Paragraph 0522-0523, (2014/10/29)
The present invention relates to novel heterocyclic compounds useful in preparing drugs for treatment of diseases associated with various functions of the histamine 4 receptor. Especially, the said drugs are useful for treatment of inflammatory diseases, allergy, pain, nasal polyps, rhinitis, chronic sinusitis, nasal congestion, nasal itch, asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, atopic dermatitis, psoriasis, eczema, pruritus, itchy skin, urticaria, idiopathic chronic urticaria, scleroderma, conjunctivitis, keratoconjunctivitis, ocular inflammation, dry eye, cardiac dysfunction, arrhythmia, atherosclerosis, multiple sclerosis, inflammatory bowel disease (including colitis, Crohn's disease, ulcerative colitis), inflammatory pain, neuropathic pain, osteoarthritic pain, autoimmune thyroid disease, immune-mediated (also known as type I) diabetes, lupus, post-operative adhesions, vestibular disorders and cancer.
HETERO RING-FUSED IMIDAZOLE DERIVATIVE HAVING AMPK ACTIVATING EFFECT
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, (2013/07/25)
Disclosed is a compound which is useful as an AMPK activator. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein a group represented by the formula: is a group represented by the formula: R1 /s
Synthesis and biological evaluation of pyrido[2,3-b]pyrazine and pyrido[2,3-b]pyrazine-N-oxide as selective glycine antagonists
Cugola, Alfredo,Donati, Daniele,Guarneri,Micheli, Fabrizio,Missio, Andrea,Pecunioso, Angelo,Reggiani, Angelo,Tarzia,Zanirato
, p. 2749 - 2754 (2007/10/03)
Pyrido[2,3-b]pyrazines and pyrido[2,3-b]pyrazines-N-oxides have been synthesized and evaluated for in vitro/in vivo antagonistic activity at the glycine site on the NMDA receptor.
