Designing and Synthesising Novel Benzophenone Biscyclic Imides Comprising Drug Moity with Investigating their Antimicrobial Activity

Abstract

The present work involved designing and synthesizing of a series of new. compounds which their molecules are composed from two biologically active components namely sulfamethoxazole or β-lactam containing drugs and cyclic imides. The target new compounds were synthesized by two steps in the first one a series of six bis (N-drug phthalamic acid_4-yl) ketone (1-6) were prepared from the reaction of sulfamethoxazole or β-lactam containing drugs with benzophenone 3, 3′, 4, 4′ -tetracarboxylic dianhydride. In the second step, compounds (1-6) were introduced in dehydration reaction via fusion process producing the target compounds bis (N-drug phthalimidyl-4-yl) ketone (7-12). The antibacterial and antifungal high activities of the prepared compounds (7-12) were tested against (Bacillus subtilis, Klebsiella pneumoniae, Pseudomonas auroginosa and Staphylococcus aurus) and all compounds showed good to high antibacterial activity. However, the maximum inhibition zone was 38 mm against Staphyloccus aurus, 36 mm against Bacillus subtilis, 35 mm against Pseudomonas auroginosa, 28mm against Klebsiella pneumoniae and 19 mm against Rhizosporium fungi.

تحوير وتشخيص بعض مشتقات الليفوفلوكساسين الحلقية غير المتجانسة كمثبطات إنزيم Cox-2 وتقييم فاعليتها الحركية الدوائية عن طريق الالتحام الجزيئي ودراسات Adme السويسرية.

“…A mixture of Amic acid (3.7 mmol) in acetic anhydride (10 mL) and sodium acetate (3.7 mmol) was heated for 2 hrs (depending on TLC results, using ethyl acetate: petroleum ether; 4:2). The mixture was cooled for about 1 hrs at room temperature, then poured on ice water (5 mL), filtered out, and washed with Diethyl ether to give the final product 17,18 .Physiochemical properties are shown in Table 1.…”

Design, synthesis and characterization of a new series of 2,3-dihydroquinazolin-4(1H)-one (DHQZ-1) derivatives and evaluation of antitumor resistant (by Molecule Docking)

“…Examination of new cancer-treatment agents is a significant area in chemistry for the synthesis of new medicinal compounds. Fusedheterocyclic components containing nitrogen are essential for intercalating cancer agents as small molecule medications or synthetic compounds [1][2][3][4] as well as physiologically active natural items, could act as an anti-inflammatory, antimicrobial, anticancer, and anticonvulsant properties [5][6][7][8] , analgesic, antihypertonic diuretic, antihistamine, antidepressant and vasodilation activities [9][10][11] . (DHQZ-1) is a large family that attracts extraordinary attention because of its biological activity.…”

“…The objective of this work is to use multicomponent reactions (MCRs) to produce a novel series of quinazoline derivatives with high yield. This occurs in one-pot condensation among Pyridine-3carbaldehyde with 1H-3,1-benzoxazine-2,4-dione (Isatoic anhydride) and primary amines (3)(4)(5)(6)(7). The mixture refluxed into tetrahydrofuran (THF, aprotic solvent).…”