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Rational approaches to discovery of orally active and brain-penetrable quinazolinone inhibitors of poly(ADP-ribose)polymerase.
J Med Chem. 2004 Aug 12; 47(17):4151-4.JM

Abstract

A novel class of quinazolinone derivatives as potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors has been discovered. Key to success was application of a rational discovery strategy involving structure-based design, combinatorial chemistry, and classical SAR for improvement of potency and bioavailability. The new inhibitors were shown to bind to the nicotinamide-ribose binding site (NI site) and the adenosine-ribose binding site (AD site) of NAD+.

Authors+Show Affiliations

Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., 2-1-6 Kashima, Yodogawa-ku, Osaka 532-8514, Japan. kouji_hattori@ po.fujisawa.co.jpNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

15293985

Citation

Hattori, Kouji, et al. "Rational Approaches to Discovery of Orally Active and Brain-penetrable Quinazolinone Inhibitors of Poly(ADP-ribose)polymerase." Journal of Medicinal Chemistry, vol. 47, no. 17, 2004, pp. 4151-4.
Hattori K, Kido Y, Yamamoto H, et al. Rational approaches to discovery of orally active and brain-penetrable quinazolinone inhibitors of poly(ADP-ribose)polymerase. J Med Chem. 2004;47(17):4151-4.
Hattori, K., Kido, Y., Yamamoto, H., Ishida, J., Kamijo, K., Murano, K., Ohkubo, M., Kinoshita, T., Iwashita, A., Mihara, K., Yamazaki, S., Matsuoka, N., Teramura, Y., & Miyake, H. (2004). Rational approaches to discovery of orally active and brain-penetrable quinazolinone inhibitors of poly(ADP-ribose)polymerase. Journal of Medicinal Chemistry, 47(17), 4151-4.
Hattori K, et al. Rational Approaches to Discovery of Orally Active and Brain-penetrable Quinazolinone Inhibitors of Poly(ADP-ribose)polymerase. J Med Chem. 2004 Aug 12;47(17):4151-4. PubMed PMID: 15293985.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Rational approaches to discovery of orally active and brain-penetrable quinazolinone inhibitors of poly(ADP-ribose)polymerase. AU - Hattori,Kouji, AU - Kido,Yoshiyuki, AU - Yamamoto,Hirofumi, AU - Ishida,Junya, AU - Kamijo,Kazunori, AU - Murano,Kenji, AU - Ohkubo,Mitsuru, AU - Kinoshita,Takayoshi, AU - Iwashita,Akinori, AU - Mihara,Kayoko, AU - Yamazaki,Syunji, AU - Matsuoka,Nobuya, AU - Teramura,Yoshinori, AU - Miyake,Hiroshi, PY - 2004/8/6/pubmed PY - 2004/8/31/medline PY - 2004/8/6/entrez SP - 4151 EP - 4 JF - Journal of medicinal chemistry JO - J Med Chem VL - 47 IS - 17 N2 - A novel class of quinazolinone derivatives as potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors has been discovered. Key to success was application of a rational discovery strategy involving structure-based design, combinatorial chemistry, and classical SAR for improvement of potency and bioavailability. The new inhibitors were shown to bind to the nicotinamide-ribose binding site (NI site) and the adenosine-ribose binding site (AD site) of NAD+. SN - 0022-2623 UR - https://www.unboundmedicine.com/medline/citation/15293985/Rational_approaches_to_discovery_of_orally_active_and_brain_penetrable_quinazolinone_inhibitors_of_poly_ADP_ribose_polymerase_ DB - PRIME DP - Unbound Medicine ER -