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Isonicotinic acid hydrazide synthesis essay
The designed compounds were synthesized in good yield according to . Compounds 2a-2e was prepared from the reaction of 4-aminobenzoic acid with appropriate benzoyl chlorides (). Hydrazides 4a-4e was synthesized through esterification of the corresponding acids followed by treatment with hydrazine hydrate (, ). The final products 5a-5e and 6a-6e were obtained from the reaction of proper hydrazides with phthalic and succinic anhydride respectively. Molecular structures of the synthesized compounds were confirmed by IR, Mass, and 1HNMR spectroscopy. The unusual result was observed in 1HNMR data of the butanoic acid analogues (6a-6e). Two vicinal methylene groups of the butanoyl moiety were singlet. It seems that they have an exactly equal chemical shift accidentally so they couldn’t split each other. Docking study on designed sEH inhibitors confirms that the analogues fit in the hydrolase catalytic pocket of X-ray crystal structure of sEH. As shown in , it is obvious that 4-(2-(4-(4-chlorobenzamido) benzoyl)hydrazinyl)-4-oxobutanoic acid (6c) in the active site pocket have a suitable distance from the three amino acids of Tyr383, Tyr466 and Asp335 for effective hydrogen bonding and additional hydrogen bonds could be formed between this compound and Phe497, Lue408 and Lue428 of the catalytic pocket.
According to the pharmacophore model suggested for sEH inhibitors (, , ), we designed, synthesized and biologically evaluated two series of 4-benzamidobenzoic acid hydrazide derivatives as novel soluble epoxide hydrolase inhibitors (). The amide group in the represented structures is considered as the primary pharmacophore (P1) and the hydrazide group is the secondary pharmacophore (P2). Phenyl ring joins P1 and P2 together as a lipophilic spacer. Oxobutanoic acid and carbonylbenzoic acid moieties play the role of terminal pharmacophore (L2/P3). Phenyl ring with various hydrophobic or hydrophilic substitutes in the R position were added to the main structure.
Acetic acid hydrazide synthesis essay - CORLYTICS
According to , most of the synthesized compounds show a considerable inhibitory activity in 1 nM concentration in comparison with inhibitory activity of AUDA, the potent urea-based inhibitor with 50 % inhibitory ratio in the equal concentration. The most potent compounds in both series are those with chloro substituent on the 4-position of the phenyl ring (5c and 6c) with inhibitory activity of 47% and 72% respectively. Generally the butanoic acid analogues (6a-6e) were found to be more potent than the corresponding benzoic acid derivatives (5a-5e) and also have a better water solubility property. Since all of the synthesized compounds have carboxylic moiety, the solubility of these compounds could be improved more by synthesis of the corresponding carboxylate salts. It seems the butanoic acid derivatives could be appropriate candidates for more investigation about new therapeutic agents due to acceptable solubility with proper inhibitory activity. In conclusion, new 4-benzamidobenzoic acid hydrazide derivatives against soluble epoxide hydrolase enzyme were investigated. According to the inhibitory activities and solubility properties the designed structures might be valuable lead scaffold to development of the potent inhibitors with improved pharmacokinetic properties.
Inhibitors of soluble epoxide hydrolase (sEH) represent one of the novel pharmaceutical approaches for treating hypertension, vascular inflammation, pain and other cardiovascular related diseases. Most of the potent sEH inhibitors reported in literature often suffer from poor solubility and bioavailability. Toward improving pharmacokinetic profile beside favorable potency, two series of 4-benzamidobenzoic acid hydrazide derivatives with hydrazide group as a novel secondary pharmacophore against sEH enzyme were developed. The designed compounds were synthesized in acceptable yield and their in vitro assay was determined. Most of the synthesized compounds have appropriate physical properties and exhibited considerable in-vitro sEH inhibitory activity in comparison with 12-(3-Adamantan-1-yl-ureido)- dodecanoicacid (AUDA), a potent urea-based sEH inhibitor. 4-(2-(4-(4-chlorobenzamido) benzoyl)hydrazinyl)-4-oxobutanoic acid 6c was found to be the most potent inhibitor with inhibitory activity of 72% targeting sEH enzyme.
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An agreement acid hydrazide on cooperation acid between the synthesis Permanent acid isonicotinic hydrazide Committee of the Union State of Belarus and Russia, hydrazide the Accounts hydrazide hydrazide Chamber of Russia, 3035">
The inner life of the Christian religion is influenced by various factors: moral earnestness, for example, and a serious realization of the aims of the Church on the part of Christians promote the attainment of her interests; on the other hand, when a worldly spirit and a low standard of morality infect many of her members, the Church's action.
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