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Corticotropin-Releasing Hormone Receptor Antagonists: Framework Design and Synthesis Guided by Ligand Conformational Studies

Autor: Paul Krenitsky, Strucely P, Robert Scott Cheeseman, Hodge Carl Nicholas, Thomas E. Christos, Zelda R. Wasserman, Paul J. Gilligan, Ciganek E, Nemeth Ga, Fernandez Ch, Everett Latham Scholfield, Argyrios G. Arvanitis, Aldrich Pe, Robert J. Chorvat

Publikováno v: Journal of Medicinal Chemistry. 42:819-832

As described in the preceding paper (Arvanitis et al. J. Med. Chem. 1999, 42), anilinopyrimidines I were identified as potent antagonists of corticotropin-releasing hormone-1 receptor (CRH1-R, also referred to as corticotropin-releasing factor, CRF1-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::42bf303a90348d0e84a147404df8be90
https://doi.org/10.1021/jm980223o

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Studies on Orally Available Inhibitors of HIV Protease. Peptidyl Aldehydes and Trifluoromethyl Ketones

Autor: Hodge Carl Nicholas, Susan Erickson-Viitanen, Y. N. Wong, M. M. Rayner, M. J. Otto, Fernandez Ch, Aldrich Pe

Publikováno v: Antiviral Chemistry and Chemotherapy. 5:257-262

Low-molecular-weight peptidyl aldehyde inhibitors of HIV protease that reach in vivo plasma concentrations after oral administration substantiailly in excess of the antiviral IC90 are described. We also report efforts to improve the potency and stabi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::0e964180057e59d3025ee9ede9123cd0
https://doi.org/10.1177/095632029400500407

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Design, synthesis, and evaluation of tetrahydropyrimidinones as an example of a general approach to nonpeptide HIV protease inhibitors

Autor: De Lucca Gv, Joseph C. Calabrese, Beverly C. Cordova, Ronald M. Klabe, M. M. Rayner, Aldrich Pe, C.-H. Chang, Jing Liang

Publikováno v: Journal of medicinal chemistry. 40(11)

Re-examination of the design of the cyclic urea class of HIV protease (HIVPR) inhibitors suggests a general approach to designing novel nonpeptide cyclic HIVPR inhibitors. This process involves the inversion of the stereochemical centers of the core

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ec6b9e8fe8bc9f3ecee17786f0a22201
https://pubmed.ncbi.nlm.nih.gov/9171880

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Akademický článek

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Akademický článek

Packaged release and targeted delivery of cytokines by migrasomes in circulation.

Autor: Jiao, Haifeng, Li, Xiaopeng, Li, Ying, Guo, Ziyi, Yang, Yuzhuo, Luo, Yiqun, Hu, Xiaoyu, Yu, Li

Publikováno v: Cell Discovery; 12/9/2024, Vol. 10 Issue 1, p1-12, 12p

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Akademický článek

Synthesis, corticotropin-releasing factor receptor binding affinity, and pharmacokinetic properties of triazolo-, imidazo-, and pyrrolopyrimidines and -pyridines.

Autor: Chorvat RJ; Department of Chemical and Physical Sciences, DuPont Pharmaceuticals Company, Experimental Station, P.O. Box 80500, Wilmington, Delaware 19880-0500, USA., Bakthavatchalam R, Beck JP, Gilligan PJ, Wilde RG, Cocuzza AJ, Hobbs FW, Cheeseman RS, Curry M, Rescinito JP, Krenitsky P, Chidester D, Yarem JA, Klaczkiewicz JD, Hodge CN, Aldrich PE, Wasserman ZR, Fernandez CH, Zaczek R, Fitzgerald LW, Huang SM, Shen HL, Wong YN, Chien BM, Arvanitis A, et. al.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 1999 Mar 11; Vol. 42 (5), pp. 833-48.

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Akademický článek

Cyclic HIV protease inhibitors: synthesis, conformational analysis, P2/P2' structure-activity relationship, and molecular recognition of cyclic ureas.

Autor: Lam PY; DuPont Merck Pharmaceutical Company, DuPont Merck Experimental Station, Wilmington, Delaware 19880-0500, USA. lampy@carbon.dmpc.com, Ru Y, Jadhav PK, Aldrich PE, DeLucca GV, Eyermann CJ, Chang CH, Emmett G, Holler ER, Daneker WF, Li L, Confalone PN, McHugh RJ, Han Q, Li R, Markwalder JA, Seitz SP, Sharpe TR, Bacheler LT, Rayner MM, Klabe RM, Shum L, Winslow DL, Kornhauser DM, Hodge CN, et. al.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 1996 Aug 30; Vol. 39 (18), pp. 3514-25.

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Akademický článek

Improved cyclic urea inhibitors of the HIV-1 protease: synthesis, potency, resistance profile, human pharmacokinetics and X-ray crystal structure of DMP 450.

Autor: Hodge CN; Department of Chemical Sciences, DuPont Merck Pharmaceutical Co., Wilmington, DE 19880, USA. hodgecn@carbon.dmpc.com, Aldrich PE, Bacheler LT, Chang CH, Eyermann CJ, Garber S, Grubb M, Jackson DA, Jadhav PK, Korant B, Lam PY, Maurin MB, Meek JL, Otto MJ, Rayner MM, Reid C, Sharpe TR, Shum L, Winslow DL, Erickson-Viitanen S

Publikováno v: Chemistry & biology [Chem Biol] 1996 Apr; Vol. 3 (4), pp. 301-14.

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Akademický článek

DMP 323, a nonpeptide cyclic urea inhibitor of human immunodeficiency virus (HIV) protease, specifically and persistently blocks intracellular processing of HIV gag polyprotein.

Autor: Rayner MM; DuPont Merck Pharmaceutical Company, Wilmington, Delaware 19880., Cordova BC, Meade RP, Aldrich PE, Jadhav PK, Ru Y, Lam PY

Publikováno v: Antimicrobial agents and chemotherapy [Antimicrob Agents Chemother] 1994 Jul; Vol. 38 (7), pp. 1635-40.

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Akademický článek

Pharmacology of 2-amino-1,4-dihydro-4-(2-[4-[4-(2-methoxyphenyl)-1- piperazinyl]butylsulfinyl]phenyl)-6-methyl-5-nitro-3-pyridine carboxylic acid methyl ester (XB513), a novel calcium agonist with alpha-1 adrenergic receptor antagonistic.

Autor: Wong PC; Du Pont Merck Pharmaceutical Company, Wilmington, Delaware., Aldrich PE, Chiu AT, Earl RA, Hart SD, Johnson AL, Ma P, McCall DE, Price WA Jr, Smith RD, et. al.

Publikováno v: The Journal of pharmacology and experimental therapeutics [J Pharmacol Exp Ther] 1993 Jun; Vol. 265 (3), pp. 1088-95.

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