𝔖 Bobbio Scriptorium
✦   LIBER   ✦

Design and synthesis of substituted N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides as positive allosteric modulators of the metabotropic glutamate receptor subtype 5

✍ Scribed by Mu-Fa Zou; Jianjing Cao; Alice L. Rodriguez; P. Jeffrey Conn; Amy Hauck Newman

Publisher
Elsevier Science
Year
2011
Tongue
English
Weight
510 KB
Volume
21
Category
Article
ISSN
0960-894X

No coin nor oath required. For personal study only.

✦ Synopsis

Based on SAR in the alkyne class of mGlu5 receptor negative allosteric modulators and a set of amidebased positive allosteric modulators, optimized substitution of the aryl 'b' ring was used to create substituted N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides. Results from an mGlu5 receptor functional assay, using calcium fluorescence, revealed varying efficacies and potencies that provide evidence that subtle changes in compounds within a close structural class can have marked effects on functional activity including switches in modes of efficacy (i.e., negative to positive allosteric modulation).

📜 SIMILAR VOLUMES

Synthesis of substituted N-[4(5-methyl/p
Synthesis of substituted N-[4(5-methyl/phenyl-1,3,4-oxadiazol-2-yl)-3,6-dihydropyridin-1(2H)-yl]benzamide/benzene sulfonamides as anti-inflammatory and anti-cancer agents
✍ Madhavi Gangapuram; Kinfe K. Redda 📂 Article 📅 2009 🏛 Journal of Heterocyclic Chemistry 🌐 English ⚖ 125 KB 👁 1 views

## Abstract magnified image Fourteen novel substituted __N__‐[4(5‐methyl/phenyl‐1,3,4‐oxadiazol‐2‐yl)‐3,6‐dihydropyridin‐1(2__H__)‐yl] benzamide/benzene sulfonamides (**11a**, **11b**, **11c**, **11d**, **11e**, **11f**, **11g**, **11h**, **11i**, **11j**, **11k**, **11l**, **11m**, **11n**) were

Synthesis of 1-(2,4-dichlorophenyl)-4-cy
Synthesis of 1-(2,4-dichlorophenyl)-4-cyano-5-(4-[11C]methoxyphenyl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide ([11C]JHU75528) and 1-(2-bromophenyl)-4-cyano-5-(4-[11C]methoxyphenyl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide ([11C]JHU75575) as potential radioligands for PET imaging of cerebral cannabinoid receptor
✍ Hong Fan; Hayden T. Ravert; Daniel P. Holt; Robert F. Dannals; Andrew G. Horti 📂 Article 📅 2006 🏛 John Wiley and Sons 🌐 French ⚖ 183 KB

## Abstract Two novel ligands for cerebral cannabinoid receptor (CB1), 1‐(2,4‐dichlorophenyl)‐4‐cyano‐5‐(4‐methoxyphenyl)‐__N__‐(piperidin‐1‐yl)‐1__H__‐pyrazole‐3‐carboxamide (JHU75528) and 1‐(2‐bromophenyl)‐4‐cyano‐5‐(4‐methoxyphenyl)‐__N__‐(piperidin‐1‐yl)‐1__H__‐pyrazole‐3‐carboxamide (JHU75575)

ChemInform Abstract: Synthesis and Bioef
ChemInform Abstract: Synthesis and Bioefficacy Evaluation of 2-[4-(3-Arylprop-2-enoyl)phenoxy]-N-substituted Acetamides and 2-[4-(5-Aryl-4,5-dihydro-1H-pyrazol-3-yl)phenoxy]acetic Acid Hydrazides as Potential Pesticides.
✍ Heetika Malik; Anjula Dahiya; Rakesh Kumar; M. S. Sangwan; Naresh Mehta; Naresh 📂 Article 📅 2010 🏛 John Wiley and Sons ⚖ 33 KB 👁 1 views

## Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable v