Synthesis and evaluation of N-alkyl-S-[3-(piperidin-1-yl)propyl] isothioureas: High affinity and human/rat species-selective histamine H 3 receptor antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 23, 2013, Pages 6415-6420

  Harusawa, Shinya ^a   Sawada, Koichi ^b   Magata, Takuji ^a   Yoneyama, Hiroki ^a   Araki, Lisa ^a   Usami, Yoshihide ^a   Hatano, Kouta ^b   Yamamoto, Kouichi ^b   Yamamoto, Daisuke ^a   Yamatodani, Atsushi ^b  

^a OSAKA MEDICAL COLLEGE   (Japan)

^b OSAKA UNIVERSITY   (Japan)

Author keywords

Antagonist; Human H3 receptor; Molecular modeling; Rat H3 receptor; Species difference

Indexed keywords

1 (5 CHLORO 2 INDOLYLCARBONYL) 4 METHYLPIPERAZINE; CLOBENPROPIT; FUB 661; HISTAMINE; HISTAMINE H3 RECEPTOR; HISTAMINE H3 RECEPTOR ANTAGONIST; HISTAMINE H4 RECEPTOR; N ALKYL S [3 (PIPERIDIN 1 YL)PROPYL] ISOTHIOUREA DERIVATIVE; OUP 181; OUP 186; THIOUREA DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG DESIGN; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SCREENING; DRUG SELECTIVITY; DRUG SYNTHESIS; GENE MUTATION; HISTAMINE RELEASE; HUMAN; IN VITRO STUDY; IN VIVO STUDY; MICRODIALYSIS; MOLECULAR DOCKING; MOLECULAR MODEL; NONHUMAN; RAT; RECEPTOR AFFINITY; SPECIES DIFFERENCE; STRUCTURE ACTIVITY RELATION;

RATTUS;

ANTAGONIST; HUMAN H(3) RECEPTOR; MOLECULAR MODELING; RAT H(3) RECEPTOR; SPECIES DIFFERENCE;

ANIMALS; HISTAMINE H3 ANTAGONISTS; HUMANS; MODELS, MOLECULAR; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; THIOUREA;

EID: 84886947775     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.09.052     Document Type: Article

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