Anti-histaminic activity

Cafieri F, Camuccio R, Fattorusso E, Taglialatela-Scafati O, Vallefuoco T (1997) Anti-Histaminic Activity of Bromopyrrole Alkaloids Isolated from Caribbean Agelas Sponges. Bioorg Med Chem Lett 7 2283... 

Agrawal et al. have studied the anti-histaminic activity of these 2,3-disubstituted thiazolidin-4-one analogues (Table 9) with graph theoretical indices and discovered the following equation for the activity in terms of the rooted Wiener index (Ww), rooted Szeged index (Szw), molecular redundancy index (MRI), and an indicator variable Ipi (for the p-alkyl of the aryl... 

Table 9 Physicochemical properties and anti-histaminic activity of 2,3-disubstituted thiazolidin-4-ones derivatives (Fig. 10) [109]...

Table 10 Thiazole and benzthiazole derivatives in modeling the anti-histaminic activity (Fig. 11) [111,112] ...

Cafieri, F., Camuccio, R., Fattorusso, E., Taglialatela-Seafati, O., Vallefuoco, T., (1997). Anti-histaminic activity of bromopyrrole alkaloids isolated from Caribbean Agelas sponges. Bioorg. Med. Chem. Lett. 7,2283-2288. 

Caraway is generally considered to have carminative and stomachic properties. Caraway oil has been reported to exhibit antibacterial activities in vitro as well as larvicidal proper-ties. ° It also has antispasmodic and anti-histaminic activities on isolated animal organs (HANGSU). - ... 

Syntheses of tryptic peptides corresponding to the sequences 1—5 (11) and 69—73 (12) of hen egg-white lysozyme and to the sequence 1—5 (13) of turkey egg-white lysozyme have been described. The anti-histaminic activity of (11)—(13) was examined. 

The most potent activities (gastric antisecretory activity in the pylorus-ligated rat or anti-ulcer activity on stress-induced gastric lesion in rat) have been observed with compounds (30), (31) [106], (32) [107], (33) and (34) [108], which were shown neither to be histamine H2 receptor inhibitors nor to act as anticholinergic agents. Thus, the activity of compound (32), for example, has been reported to be superior to that of cimetidine [107],... 

Histamine receptors on parietal cells belong to the H2 type (p. 114) and are blocked by H2-antihistaniines. Because histamine plays a pivotal role in the activation of parietal cells, H2-anti-histamines also diminish responsivity to other stimulants, e.g gastrin (in gas-2000 Thieme... 

Apart from their anti-inflammatory activity the NSAIDs also show, dependent on the condition and the type of pain, considerable analgesic efficacy. In some forms of postoperative pain the NSAID s can be as efficacious as opioids, especially when prostaglandins, bradykinin and histamine, which are released by inflammation, have caused sensitization of pain receptors to normally painless stimuli. In Table 4 some advantages and disadvantages of NSAID s and opioids are compared. Although analgesic effects at peripheral or central neurons cannot be excluded completely, most studies indicate that... 

Inhibits degranulation of mast cells also inhibits release of histamine and SRS-A (a leukotriene) from the mast cell. This inhibits the early asthmatic response by stabilizing the mast cell also inhibits the late asthmatic response. It has no intrinsic bronchodilator, antihistaminic, anticholinergic, vasoconstrictor, or anti-inflammatory activity. 

The anti-inflammatory effects of FP and triflupromazine, either alone or in combination with triamcinolone, were studied in rats after one single dose and 8 days, measuring histamine, serotonin, prostaglandin (PGE2), volume of exudate and histaminase enzyme [174]. The results indicated that the administration of FP and triflupromazine in these conditions induced a significant anti-inflammatory activity which could be attributed to the inhibition of prostaglandin E2. 

Miscellaneous - Two novel agents reported to possess auitiinflanuna-tory, antipyretic and analgesic activities nearly comparable to phenylbutazone are N,N-Di(m-aaninophenyl )butyl-ethylmalonamide (Gy-97, XIX) and l-(4-chlorophenyl)-4- 2-[3-(2-pyridyl)acryloxy ethyl piperazine (DA 1529 XX).Gy-97 also has anti-histaminic and anti-... 

Such a procedure has been exploited for the synthesis of several derivatives for which an anti-inflammatory activity has been claimed [58]. A derivative under study as the Histamine H3 antagonist was prepared by the thermal intramolecular Diels-Alder reaction of a triene derivative of buta-1,3-diene-1-sulfonic acid amide. 1,3-Butadiene sulfonamides 182 (a 67%, b 69%, c 99%, d 51%) were prepared by the base mediated condensation of M-Boc-methanesulfonamides (181) with a series of aldheydes. N-akylation of 182 to give trienes 183 (a 69%, b 76%, c 82%, d 59%) was achieved by reacting the sodium salts with allyl bromide in THF at reflux. The intramolecular Diels-Alder reactions of compounds 183 were performed at 145 °C in toluene in a sealed vessel under argon. Under these conditions compounds 184 and 184 were obtained in good yields (a 76% ratio 6 1, b 71% ratio 6 1, c 92% ratio 3 1, d 87% ratio 3 1). 

---