Optimization of 2-aminothiazole derivatives as CCR4 antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 10, 2006, Pages 2800-2803

  Wang, Xuemei ^a   Xu, Feng ^a   Xu, Qingge ^a   Mahmud, Hossen ^a   Houze, Jonathan ^a   Zhu, Liusheng ^a   Akerman, Michelle ^a   Tonn, George ^a   Tang, Liang ^a   McMaster, Brian E ^b   Dairaghi, Daniel J ^b   Schall, Thomas J ^b   Collins, Tassie L ^a   Medina, Julio C ^a  

^a AMGEN INC   (United States)

^b ChemoCentryx Inc   (United States)

Author keywords

CCL17; CCL22; CCR4; Chemokine; Chemokine receptor; GPCR; MDC; TARC

Indexed keywords

2 AMINOTHIAZOLE DERIVATIVE; CHEMOKINE RECEPTOR CCR5 ANTAGONIST;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DESIGN; DRUG HALF LIFE; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG RESEARCH; DRUG SCREENING; DRUG SYNTHESIS; NONHUMAN; PROCESS OPTIMIZATION; RAT; RECEPTOR AFFINITY;

CELL LINE; HUMANS; RECEPTORS, CHEMOKINE; THIAZOLES;

ANIMALIA;

EID: 33645893175     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.01.126     Document Type: Article

References (10)

1. Chvatchko Y., Hoogewerf A.J., Meyer A., Alouani S., Juillard P., Buser R., Conquet F., Proudfoot A.E.I., Wells T.N.C., and Power C.A. J. Exp. Med. 191 (2000) 1755
2. Power C.A., Meyer A., Nemeth K., Bacon K.B., Hoogewerf A.J., Proudfoot A.E.I., and Wells T.N.C. J. Biol. Chem. (1997) 19495
3. Imai T., Baba M., Nishimura M., Kakizaki M., Takagi S., and Yoshie O. J. Biol. Chem. 272 (1997) 15036
4. Imai T., Chantry D., Raport C.J., Wood C.L., Nishimura M., Godiska R., Yoshie O., and Gray P.W. J. Biol. Chem. 273 (1998) 1764
5. Hirata H., Arima M., Cheng G., Honda K., Fukushima F., Yoshida N., Eda F., and Fukuda T. J. Clin. Immunol. 23 (2003) 34
6. Teraki Y., Miyake A., Takebayashi R., and Shiohara T. Clin. Exp. Dermatol. 29 (2004) 658
7. Kakinuma T., Nakamura K., Wakugawa M., Mitsui H., Tada Y., Saeki H., Torii H., Asahina A., Onai N., Matsushima K., and Tamaki K. J. Allergy Clin. Immunol. 107 (2001) 535
8. Hüser N., Tertilt C., Gerauer K., Maier S., Traeger T., Aßfalg V., Reiter R., Heidecke C., and Pfeffer K. Eur. J. Immunol. 35 (2005) 128
9. 125I]TARC (Perkin-Elmer) was diluted to 100 pM in buffer; 100 μL was added to each well of the assay plate. The assay plates were incubated at room temperature for 2 h. The assay mixtures were filtered through GF/B filter plates using a FilterMate Harvester (Perkin-Elmer). Retained radioactivity was quantified by scintillation counting.
10. 2, 95% humidity) and incubated for 2 h. At the end of this incubation period, the cells were aspirated from the top of the filter and the filter was removed. Alamar blue (5 μL) was added to the bottom chamber, the plate was returned to the incubator and incubated for another hour. At the end of this incubation period, the plates were read on a fluorescent plate reader (530 absorbance, 590 emission).