Abstract
The oxirane derivative (2) was allowed to react with hydrazine hydrate, 4-aminobenzoic acid and o-phenylene diamine to give β-hydrazine alcohol derivative (3) and β-amino derivatives (4) and (5). The hydrazide (8) reacted with glucose, phthalic anhydride and aromatic aldehydes to give the phthalazine derivatives (9), (15) and (16a-c). A new heterocyclic molecules were synthesized using ethyl acetoacetate, acetyl acetone and benzoyl chloride with the hydrazide (8) to give the pyrazole derivatives (12), (14) and the oxadiazole derivative (18). The new compounds were synthesized with the objective of studying their antifungal and antimicrobial activity. Some of them gave positive results. The newly synthesized compounds were characterized on the basis of their spectral (1H-NMR, Mass spectrum, IR and Elementary analysis).
Highlights
Phthalazin-1(2H)-ones are of considerable interest due to their antidiabetic [1], antiallergic [2], vasorelaxant [3], PDE4 inhibitors [4], VEGF receptor tyrosine kinases for the treatment of cancer [5,6], antiasthmatic agents with dual activities of thromboxane A2 (TXA2) synthetase inhibition and bronchodialation [7], herbicidal [8]
Most of the classical nonsteroidal anti-inflammatory drugs (NSAIDs) exerts their side effects by inhibition of COX-1 enzyme since the COX-1 isoform is the constitutive one that is responsible for regulation of physiological processes, and the COX-2 isoform is discovered to be the enzyme induced by a inflammatory stimuli, selective inhibition of COX-2 provides a rationale for developing anti-inflammatory and analgesic agents
The diaryl heterocyclic compounds are mainly studied as new class of NSAIDs without gastric side effects, many studies have focused on a different type of compounds to develop safer NSAIDs [27]
Summary
Phthalazin-1(2H)-ones are of considerable interest due to their antidiabetic [1], antiallergic [2] , vasorelaxant [3], PDE4 inhibitors [4], VEGF (vascular endothelical group factor) receptor tyrosine kinases for the treatment of cancer [5,6], antiasthmatic agents with dual activities of thromboxane A2 (TXA2) synthetase inhibition and bronchodialation [7], herbicidal [8]. Most of the current nonsteroidal anti-inflammatory drugs (NSAIDs) show serious side effects including gastrointestinal disorders and kidney damage These studies for developing safer NSAIDs lacking the gastrointestinal and renal side effects of current used ones have recently been of interest for many researches. In terms of this aspect, many studies have been focused on pyridazin-(3H)-ones, which are characterized to possess good analgesic and anti-inflammatory activities Beside pyridazinones, these studies have indicated that the heterocyclic ring substitutions at the six position, and the presence of acetamide side chain when linked to the lactam nitrogen of pyridazinone ring at the two position of the pyridazinone ring, improve the analgesic and antiflammatory activity along with nil or very low ulcerogenicity [29,30,31,32,33,34]. In view of the aforementioned facts, it seemed most interesting to synthesize some [4-(2-tetryl)-2-substituted phthalazin-1(2H)-one] derivatives with the aim to obtain more precise information about the course of reactions and biological activities
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