Hit optimization of the class of quinazoline containing histamine H4 receptor (H4R) ligands resulted in a sulfonamide substituted analogue with high affinity for the H4R. This moiety leads to improved physicochemical properties and is believed to probe a distinct H4R binding pocket that was previously identified using pharmacophore modeling. By introducing a variety of sulfonamide substituents, the H4R affinity was optimized. The interaction of the new ligands, in combination with a set of previously published quinazoline compounds, was described by a QSAR equation. Pharmacological studies revealed that the sulfonamide analogues have excellent H4R affinity and behave as inverse agonists at the human H4R. In vivo evaluation of the potent 2-(6-chloro-2-(4-methylpiperazin-1-yl)quinazoline-4-amino)-N-phenylethanesulfonamide (54) (pKi = 8.31 ± 0.10) revealed it to have anti-inflammatory activity in an animal model of acute inflammation.

Synthesis and QSAR of quinazoline sulfonamides as highly potent human histamine H4 receptor inverse agonists.

Interactions of taurine with GABAB binding sites in mouse brain.

Taurine and epilepsy.

In order to study the influence of the length of the amino acid chain of N,N-phthaloyl-amino acid amides as analogues of the former anticonvulsant taltrimide on the seizure-antagonizing activity glycine, beta -alanine and gamma -aminobutyric acid (GABA) derivatives were synthesized. The corresponding taurine derivatives were also included. Generally, the glycine-derived amides showed a higher activity than the beta -alanine and GABA derivatives in the maximal electroshock seizure (MES) test in mice upon intraperitoneal administration. The activity was comparable to the respective taurine derivatives. The N,N-phthaloyl-glycine, amides were also active in the MES test upon oral administration to rats. No significant activity was noted in the seizure threshold test with subcutaneous pentylenetetrazole. The ED50 of N,N-phthaloyl-glycine ethyl amide (4b) in the MES test upon intraperitoneal administration to mice was 19.1 mg/kg. On a molar basis this activity is comparable to the activity of phenytoin with little toxicity in the rotorod test. In conclusion, N,N-phthaloyl-glycine amides might represent promising antiepileptic drugs.

/pdf/synthesis-and-anticonvulsant-activity-of-n-n-phthaloyl-244aphd0rn.pdf

Synthesis and anticonvulsant activity of N,N‐phthaloyl derivatives of central nervous system inhibitory amino acids

Anticonvulsant activity of some 2-aminoethanesulphonic acid (taurine) derivatives.

Synthesis and anticonvulsant properties of some 2‐Aminoethanesulfonic acid (Taurine) derivatives

□ A series of 2-acylaminoethanesulfonamides were synthesized by treating the corresponding sulfonyl chlorides with ammonia, a primary, or a secondary amine. A few compounds displayed marked anticonvulsant activity in mice when tested for their potency in the maximal electroshock seizure test. The piperidino, benzamido, phthalimido, and phenylsuccinylimido derivatives were active, whereas the succinylimido, saccharinylimido, and norbornendicarboxylimido compounds showed no activity. The interference with the sodium-independent taurine binding to mouse brain synaptic membranes was assessed to elucidate the possible mode of anticonvulsant action.

Synthesis and anticonvulsant properties of some 2‐aminoethanesulfonic acid (taurine) derivatives

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Synthesis and anticonvulsant properties of some 2‐Aminoethanesulfonic acid (Taurine) derivatives

Synthesis and anticonvulsant properties of some 2‐aminoethanesulfonic acid (taurine) derivatives