The discovery of small molecule inhibitors of neutral endopeptidase. Structure-activity studies on functionalized glutaramides

Chemical Biology and Drug Design

Volumn 67, Issue 1, 2006, Pages 74-77

  Maw, Graham N ^a   Stobie, Alan ^a   Planken, Simon ^a   Pryde, David C ^a   Sanderson, Vivienne ^a   Platts, Michelle Y ^a   Corless, Martin ^a   Stacey, Peter ^a   Wayman, Christopher ^a   Van Der Graaf, Piet ^a   Kohl, Christopher ^a   Coggon, Sara ^a   Beaumont, Kevin ^a  

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

Author keywords

Female sexual arousal; Glutaramides; Neutral endopeptidase

Indexed keywords

ETHYL 1,3,4 THIADIAZOLE GLUTARAMIDE; GLUTARAMIC ACID DERIVATIVE; PROTEINASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; COW; DRUG ABSORPTION; DRUG IDENTIFICATION; DRUG POTENCY; DRUG SCREENING; DRUG SELECTIVITY; DRUG SYNTHESIS; DRUG TARGETING; HUMAN; HUMAN CELL; MOLECULAR WEIGHT; NONHUMAN; PRIORITY JOURNAL; PROTEIN TARGETING; RAT; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; AMIDES; ANIMALS; CYCLOHEXANECARBOXYLIC ACIDS; DOGS; DRUG DESIGN; ENZYME INHIBITORS; FEMALE; HUMANS; MOLECULAR WEIGHT; NEPRILYSIN; PENTANOIC ACIDS; PROTEASE INHIBITORS; RATS; SEXUAL DYSFUNCTIONS, PSYCHOLOGICAL; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; THIADIAZOLES;

EID: 33745087743     PISSN: 17470277     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1747-0285.2005.00320.x     Document Type: Article

References (11)

1. Goldstein I. Berman J.R. ( 1998) Vasculogenic Female Sexual Dysfunction: Vaginal Engorgement and Clitoral Erectile Insufficiency Syndromes. Int J Impot Res 10 ( Suppl 2 S84 S90.
2. Werbin T. Salimpour P. Berman L. Krane R.J. Goldstein I. Berman J. ( 1999) Effect of sexual Stimulation and Age on Genital Blood Flow in Women with Sexual Arousal Disorder. J Urology 161 ( Suppl 4S 805 814.
3. Berman J. Berman L. Werbin T. Goldstein I. ( 1999) Female Sexual Dysfunction: Anatomy, Physiology, Evaluation and Treatment Options. Curr Op Urol 9 : 563 568.
4. Hoyle C.H.V. Stones R.W. Robson T. Whitley K. Bumstock G. ( 1996) Innervation of Vasculature and Microvasculature of the Human Vagina by NOS and Neuropeptide-Containing Nerves. J Anat 188 ( Part 3 633 644.
5. Ottesen B. Gerstenberg T. Ulrichsen H. Manthorpe T Fahrenkrug J. Wagner G. ( 1983) Vasoactive Intestinal Polypeptide (VIP) Increases Vaginal Blood Flow and Inhibits Uterine Smooth Muscle Activity in Women. Eu J Clin Investig 13 ( 4 321 324.
6. Roques B.P. Noble F. Dauge V. Fournie-Zaluski M-C. Beaumont A. ( 1993) Neutral Endopeptidase 24.11: Structure, Inhibition, and Experimental and Clinical Pharmacology. Pharmacol Revs 45 : 87 146.
7. Oefner C. D'Arcy A. Hennig M. Winkler F.K. Dale G.E. ( 2000) Structure of Human Neutral Endopeptidase (Neprilysin) Complexed with Phosphoramidon. J Mol Biol 296 : 341 349.
8. Duggan K.A. Jones D.M. Ye V.Z. Davis R.E. MacDonald G.J. ( 1995) Effects of Endopeptidase 24.11 Inhibition on Plasma and Tissue Concentrations of Vasoactive Intestinal Peptide. Clin Sci 89 : 267 271.
9. Kaye B. Brearley C.J. Cussans N.J. Herron M. Humphrey M.J. Mollatt A.R. ( 1997) Formation and Pharmacokinetics of the Active Drug Candoxatrilat in Mouse, Rat, Rabbit, Dog and Man Following Administration of the Prodrug Candoxatril. Xenobiotica 27 ( 10 1091 1102.
10. McDowell G. Nicholls D.P. ( 2000) The Therapeutic Potential of Candoxatril, a Neutral Endopeptidase Inhibitor, in Humans. Cardiovasc Drug Revs 18 ( 4 259 270.
11. Medeiros M.A. Franca M.S. Boileau G. Juliano L. Carvalho K.M. ( 1997) Specific Fluorogenic Substrates for Neprilysin (EC3.4.24.11) which are Highly Resistant to Serine and Metalloproteases. Braz J Med Biol Res 30 ( 10 1157 1162.