Evaluation of Anti‐inflammatory, Anti‐nociceptive, and Anti‐ulcerogenic Activities of Novel Synthesized Thiazolyl and Pyrrolyl Steroids

Abstract

Developing new therapeutic agents that can overcome gastrointestinal injury and at the same time could lead to an enhanced anti-inflammatory effect becomes an urgent need for inflammation patients. Thiazolyl and pyrrolyl steroids were synthesized via straight forward and efficient methods and their structures were established based on their correct elemental analysis and compatible IR, (1) H-NMR, (13) C-NMR, and mass spectral data. The dihydrothiazolyl-hydrazonoprogesterone 12 and the aminopyrrolylprogesterone 16a showed anti-inflammatory, antinociceptive, and anti-ulcerogenic activity with various intensities. Edema were significantly reduced by both doses of tested compounds (25 and 50 mg/kg) at 2, 3, and 4 h post-carrageenan. The high dose of compound 16a was the most effective in alleviating thermal pain. Gastric mucosal lesions, caused in the rats by the administration of ethanol or indomethacin (IND), were significantly inhibited by each of the two tested compounds. These results provide a unique opportunity to develop new anti-inflammatory drugs which devoid the ulcerogenic liabilities associated with currently marketed drugs.

In vitro Antioxidant, Antimicrobial and in vivo Peripheral Analgesic Activities of Methanol and Petroleum Ether Extracts of Whole Plant of Uraria lagopoides DC

“…Higher amount flavonoid content of petroleum ether extract (81.07±1.80 mg/g, QE) than methanol extract (31.33±0.72 mg/g, QE) may contribute to this better activity. Steroids also possess pain relieving activity [79][80][81][82][83]. Earlier four new compounds, namely 7′-carboxylic-n.-heptacosanyl-glutarate, n.-nonacosan-6-ol-1,13-dioic acid, 4,12-dimethyl-n.-tetradeca-6,8,10-triene-1ol-4-oic acid, and 8,14-13,17-diseco-stigmast-5,22-diene-3-α-ol, along with 2-hydroxytricontane and β-sitosterol glycoside, have been isolated from the aerial parts of Uraria lagopoides D.C. [84].…”

Synthesis of Thiophenyl, Thiazolyl, and Pyridinyl Androstane Derivatives: A Novel Class of Potent Anti-inflammatory and Anti-ulcerogenic Heterocyclic Steroids

“…One of the most important issues was the synthesis and biological study of many heterocyclic steroids as extremely potent anti-inflammatory agents [Elmegeed et al, 2005, Mohareb et al, 2011Cai et al, 2019]. The development of an efficient curative agent for inflammation treatment has experienced continuous evolution leading to the creation of more efficient types of drugs [Elgazwy et al, 2012].…”