57332-84-0Relevant articles and documents
Novel Pyrazole-Containing Compounds Active against Mycobacterium tuberculosis
Poce, Giovanna,Consalvi, Sara,Venditti, Giulia,Alfonso, Salvatore,Desideri, Nicoletta,Fernandez-Menendez, Raquel,Bates, Robert H.,Ballell, Lluis,Barros Aguirre, David,Rullas, Joaquin,De Logu, Alessandro,Gardner, Michelle,Ioerger, Thomas R.,Rubin, Eric J.,Biava, Mariangela
, p. 1423 - 1429 (2019)
In this study, a series of 49 five-membered heterocyclic compounds containing either a pyridine- or a pyrrole-type nitrogen were synthesized and tested against Mycobacterium tuberculosis. Among them, only the 1,3,5-trisubstituted pyrazoles 5-49 exhibited
PHENYL AND PYRIDINYL SUBSTITUTED IMIDAZOLES AS MODULATORS OF RORyT
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Paragraph 0366-0367, (2020/01/08)
The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, Ra, Rb, Q1, and Q2 are defined in the specification. The invention also comprises a method of treating or ameliorating a ROR-γ-t mediated syndrome, disorder or disease, including wherein the syndrome, disorder or disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, and psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
Melanin-Concentrating Hormone Receptor 1 Antagonists Lacking an Aliphatic Amine: Synthesis and Structure-Activity Relationships of Novel 1-(Imidazo[1,2-a]pyridin-6-yl)pyridin-2(1H)-one Derivatives
Igawa, Hideyuki,Takahashi, Masashi,Kakegawa, Keiko,Kina, Asato,Ikoma, Minoru,Aida, Jumpei,Yasuma, Tsuneo,Kawata, Yayoi,Ashina, Shuntaro,Yamamoto, Syunsuke,Kundu, Mrinalkanti,Khamrai, Uttam,Hirabayashi, Hideki,Nakayama, Masaharu,Nagisa, Yasutaka,Kasai, Shizuo,Maekawa, Tsuyoshi
supporting information, p. 1116 - 1139 (2016/02/23)
Aiming to discover melanin-concentrating hormone receptor 1 (MCHR1) antagonists with improved safety profiles, we hypothesized that the aliphatic amine employed in most antagonists reported to date could be removed if the bicyclic motif of the compound scaffold interacted with Asp123 and/or Tyr272 of MCHR1. We excluded aliphatic amines from our compound designs, with a cutoff value of pKa 8, and explored aliphatic amine-free MCHR1 antagonists in a CNS-oriented chemical space limited by four descriptors (TPSA, ClogP, MW, and HBD count). Screening of novel bicyclic motifs with high intrinsic binding affinity for MCHR1 identified the imidazo[1,2-a]pyridine ring (represented in compounds 6a and 6b), and subsequent cyclization of the central aliphatic amide linkage led to the discovery of a potent, orally bioavailable MCHR1 antagonist 4-[(4-chlorobenzyl)oxy]-1-(2-cyclopropyl-3-methylimidazo[1,2-a]pyridin-6-yl)pyridin-2(1H)-one 10a. It exhibited low potential for hERG inhibition and phospholipidosis induction as well as sufficient brain concentration to exert antiobesity effects in diet-induced obese rats.