Category: 93643-24-4

Discovery of Quinazolines as Histamine H₄ Receptor Inverse Agonists Using a Scaffold Hopping Approach was written by Smits, Rogier A.;de Esch, Iwan J. P.;Zuiderveld, Obbe P.;Broeker, Joachim;Sansuk, Kamonchanok;Guaita, Elena;Coruzzi, Gabriella;Adami, Maristella;Haaksma, Eric;Leurs, Rob. And the article was included in Journal of Medicinal Chemistry in 2008.Application In Synthesis of (S)-1,4-Diazabicyclo[4.3.0]nonane This article mentions the following:

From a series of small fragments that was designed to probe the histamine H₄ receptor (H₄R), we previously described quinoxaline-containing fragments that were grown into high affinity H₄R ligands in a process that was guided by pharmacophore modeling. With a scaffold hopping exercise and using the same in silico models, we now report the identification and optimization of a series of quinazoline-containing H₄R compounds This approach led to the discovery of 6-chloro-N-(furan-3-ylmethyl)2-(4-methylpiperazin-1-yl)quinazolin-4-amine (VUF10499, 54) and 6-chloro-2-(4-methylpiperazin-1-yl)-N-(thiophen-2-ylmethyl)quinazolin-4-amine (VUF10497, 55) as potent human H₄R inverse agonists (pK_i = 8.12 and 7.57, resp.). Interestingly, both compounds also possess considerable affinity for the human histamine H₁ receptor (H₁R) and therefore represent a novel class of dual action H₁R/H₄R ligands, a profile that potentially leads to added therapeutic benefit. Compounds from this novel series of quinazolines are antagonists at the rat H₄R and were found to possess anti-inflammatory properties in vivo in the rat. In the experiment, the researchers used many compounds, for example, (S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4Application In Synthesis of (S)-1,4-Diazabicyclo[4.3.0]nonane).

(S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Application In Synthesis of (S)-1,4-Diazabicyclo[4.3.0]nonane

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Synthesis and inhibitory activity on carbonic anhydrase of some new sulpiride analogs studied by means of a new method was written by Botre, Claudio;Botre, Francesco;Jommi, Giancarlo;Signorini, Roberto. And the article was included in Journal of Medicinal Chemistry in 1986.Computed Properties of C7H14N2 This article mentions the following:

The pharmacol. activity of new sulpiride analogs was studied by a potentiometric technique with a pCO₂ sensor, capable of detecting carbonic anhydrase inhibition at equilibrium conditions. This procedure gives results state as percent of inhibition of enzymic activity. To prove the reliability of the approach and to study structure-activity relationships, several new mols., e.g., sulfamoylbenzamides I (R = Et₂NCH₂CH₂, 2-piperidinoethyl, morpholinoethyl) and piperazine amides II (R¹ = H, allyl, Me₂CHCH₂, EtO₂CCH₂, PhCH₂, etc.) were prepared and tested in comparison with the two sulpiride enantiomers. An inhibition mechanism is discussed in terms of exptl. evidence obtained from the interactions between the mol. structures of the new synthesized compounds and carbonic anhydrase. In the experiment, the researchers used many compounds, for example, (S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4Computed Properties of C7H14N2).

(S)-1,4-Diazabicyclo[4.3.0]nonane (cas: 93643-24-4) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Computed Properties of C7H14N2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics