By János Fischer, C. Robin Ganellin
Born out of a venture of the IUPAC's committee on Medicinal Chemistry and Drug improvement, this reference addresses previous and present concepts for winning drug analog improvement, extending the formerly released quantity by means of 9 new analog periods and 8 case reports. Like its precursor, this quantity additionally features a normal part discussing universally appropriate ideas for analog discovery and improvement. Spanning a variety of healing fields and chemical periods, the 2 volumes jointly represent the 1st systematic method of drug analog development.Of curiosity to almost each researcher operating in drug discovery and pharmaceutical chemistry.
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Additional resources for Analogue-based Drug Discovery II, Volume 2
Int. , 45, 5072–5129. J. (1962) Derivatives of 6aminopenicillanic acid. Part III. 2, 6Dialkoxybenzoyl derivatives. J. Chem. , 1453–1458. R. (1961) New penicillins stable towards both acid and penicillinase. Nature, 192, 1183. R. (1963) Derivatives of 6-aminopenicillanic acid. Part VI. Penicillins from 3- and 5phenylisoxazole-4-carboxylic acids and their alkyl and halogen derivatives. J. Chem. , 5838. C. C. (1962) (Beecham) British Patent 978,299. Gothard, P. R. (2004) Voriconazole for serious fungal infections.
1) are direct analogues; however, they also have a close metabolic relationship since paracetamol is the active metabolite of both acetanilide and phenacetin. Acetanilide (1) was discovered as an antipyretic drug after it was mistakenly used instead of naphthalene in an antiworming regimen in 1886 . 1 Paracetamol and its former analogues. Hoescht Dyeworks. Acetanilide was cheaper and easier to prepare than other antipyretics and it remained in use for many decades. In 1887, the Bayer Company introduced the 4-ethoxy derivative, phenacetin, as a less toxic analogue of acetanilide.
8). Chlorpromazine was marketed by Rhône-Poulenc in 1952. Chlorpromazine initiated an analogue-based drug research, and several direct analogues were discovered and introduced as antipsychotic drugs without the knowledge of their mechanism of action. In vivo pharmacological models, such as conditioned avoidance response test, were typically used to drive these discovery efforts. A completely different approach in the Janssen Laboratories in 1958 afforded more potent drugs. The sedative effect of an analgesic pethidine derivative (R1187) was reminiscent of the sedation produced by chlorpromazine and, after exploring hundreds of derivatives, haloperidol was discovered.
Analogue-based Drug Discovery II, Volume 2 by János Fischer, C. Robin Ganellin