Drugs, leads, and drug-likeness: An analysis of some recently launched drugs

被引:193
作者
Proudfoot, JR [1 ]
机构
[1] Boehringer Ingelheim Pharmaceut Inc, Dept Med Chem, Ridgefield, CT 06877 USA
关键词
D O I
10.1016/S0960-894X(02)00244-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
An analysis of the origins of recently launched drugs reveals that most were derived by modification of known drug structures or from lead structures obtained from the scientific literature. High-throughput screening did not have a significant impact on the derivation of these drugs. The drug structures are very closely related to their leads. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1647 / 1650
页数:4
相关论文
共 41 条
[1]   Can we learn to distinguish between "drug-like" and "nondrug-like" molecules? [J].
Ajay ;
Walters, WP ;
Murcko, MA .
JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (18) :3314-3324
[2]  
[Anonymous], COMPREHENSIVE MED CH
[3]   Properties of known drugs. 2. Side chains [J].
Bemis, GW ;
Murcko, MA .
JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (25) :5095-5099
[4]  
BHAT B, 1981, INDIAN J CHEM B, V20, P703
[5]   SYNTHESIS OF SPIRORENONE - A NOVEL HIGHLY-ACTIVE ALDOSTERONE ANTAGONIST [J].
BITTLER, D ;
HOFMEISTER, H ;
LAURENT, H ;
NICKISCH, K ;
NICKOLSON, R ;
PETZOLDT, K ;
WIECHERT, R .
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION IN ENGLISH, 1982, 21 (09) :696-697
[6]   SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF NOVEL RETINOID-X RECEPTOR-SELECTIVE RETINOIDS [J].
BOEHM, MF ;
ZHANG, L ;
BADEA, BA ;
WHITE, SK ;
MAIS, DE ;
BERGER, E ;
SUTO, CM ;
GOLDMAN, ME ;
HEYMAN, RA .
JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (18) :2930-2941
[7]   SYNTHESIS OF HIGH SPECIFIC ACTIVITY [H-3] 9-CIS-RETINOIC ACID AND ITS APPLICATION FOR IDENTIFYING RETINOIDS WITH UNUSUAL BINDING-PROPERTIES [J].
BOEHM, MF ;
MCCLURG, MR ;
PATHIRANA, C ;
MANGELSDORF, D ;
WHITE, SK ;
HEBERT, J ;
WINN, D ;
GOLDMAN, ME ;
HEYMAN, RA .
JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (03) :408-414
[8]   Pharmacological characterization of almotriptan:: an indolic 5-HT receptor agonist for the treatment of migraine [J].
Bou, J ;
Domènech, T ;
Puig, J ;
Heredia, A ;
Gras, J ;
Fernández-Forner, D ;
Beleta, J ;
Palacios, JM .
EUROPEAN JOURNAL OF PHARMACOLOGY, 2000, 410 (01) :33-41
[9]   Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant Gram-positive bacterial infections [J].
Brickner, SJ ;
Hutchinson, DK ;
Barbachyn, MR ;
Manninen, PR ;
Ulanowicz, DA ;
Garmon, SA ;
Grega, KC ;
Hendges, SK ;
Toops, DS ;
Ford, CW ;
Zurenko, GE .
JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (03) :673-679
[10]   ARTEETHER, A NEW ANTIMALARIAL DRUG - SYNTHESIS AND ANTIMALARIAL PROPERTIES [J].
BROSSI, A ;
VENUGOPALAN, B ;
GERPE, LD ;
YEH, HJC ;
FLIPPENANDERSON, JL ;
BUCHS, P ;
LUO, XD ;
MILHOUS, W ;
PETERS, W .
JOURNAL OF MEDICINAL CHEMISTRY, 1988, 31 (03) :645-650