17 research outputs found
Synthesis of novel benzo[4,5]imidazo[1,2-a]pyrimido- [4,5-d]pyrimidine derivatives as potent antimicrobial agents
445-453Synthesis of novel benzo[4,5]imidazo[1,2-a]pyrimido[4,5-d] pyrimidines 5/6 has been achieved by reaction of 2-amino-4-aryl-4,10-dihydrobenzo[4,5]imidazo[1,2-a]pyrimidine-3-carbonitriles 4 with formaldehyde/urea. The key intermediate 4, is obtained by reaction of 2-aminobenzaldehyde 1 with aromatic aldehyde and malononitrile by a three-component one-pot process. The newly synthesized title compounds 5/6 have been evaluated for their in vitro antimicrobial activity. Compounds 5 and 6 exhibit potent antimicrobial activity compared to that of standard drugs
A facile synthesis of 1-aryl pyrroles by Clauson-Kaas reaction using oxone as a Catalyst under microwave irradiation
A new and efficient methodology to synthesize N-substituted pyrrole derivatives by Clauson Kaas reaction employing Oxone as catalyst was developed. The transformation was performed in acetonitrile under microwave irradiation. This procedure has several advantages such as high yield, clean product formation, and short reaction time. KEY WORDS: Synthesis, Pyrrole, Oxone, Microwave irradiation Bull. Chem. Soc. Ethiop. 2019, 33(1), 143-148DOI: https://dx.doi.org/10.4314/bcse.v33i1.14
Antifungal activity of naphthothiazoles derived from Lawsone (Lawsonia inermis)
A series of Naphtho [2,3-d] thiazole-4, 9-diones was prepared by the condensation of bromolawsone with thiosemicarbazones derived from the aldehydes and ketones in dry dimethyl formamide (DMF). The products are also obtained by the cyclization of the intermediate 2-chlorobenzaldehyde thiosemicarbazone of 1,4-napthoquinone in ethanol containing K2CO3 obtained from 2,3-dichloro naphthoquinone. These compounds showed that maximum fungicidal activity varied with substituent on the compounds of Lawsone.Key words: Lawsonia inermis, 2,3-dichloronaphthoquinones, thiosemicarbazones, naphthothiazoles, fungicidal activity, Fusarium oxysporum, Curvularia lunata
Synthesis and antimicrobial activity of 2-((4-(1H-benzo[d]imidazol-2-yl)-6-(2-ethylcyclopentyl) pyrimidin-2-yl)thio)-N-methylacetamide
It was possible to synthesise a brand new series of 2-((4-(1H-benzo[d]imidazol-2-yl)-6-(2-ethylcyclopentyl)pyrimidin-2-yl)thio)-N-methyl acetamide (4a-h). The reaction of 1-(1H-benzimidazol-2-yl)ethanone with 2-ethylcyclopentane carbaldehyde with ethanol and KOH yielded (E)-1-(1H-benzo[d]imidazol-2-yl)-3-(2-ethylcyclopentyl)prop-2-en-1-one (1a-c). All compounds shown to have antimicrobial action via pharmacological study are listed here. . Chloramphenicol and Amphotericin B, two conventional antibiotics, were compared to the antibacterial and antifungal properties of synthetic compounds. It was discovered that Schlenter products had spectroscopic properties worth investigating
Synthesis and antimicrobial activity of novel benzo[4', 5']-imidazo[1',2':1,2]pyrrolo[3,4-b]isoxazolo[4,5-e]pyridines
174-183Synthesis of novel benzo [4',5'] imidazo [1',2':1,2] pyrrolo [3,4-b] isoxazolo [4,5-e] pyridines 8 has been achieved by reaction of 1-(prop-2-yn-1-yl)-1H-benzo [d] imidazo-2-carbaldehydes 5 with 5-amino -3-methylisoxazole 6 in presence of InCl3 in CH3CN media, followed by reaction of imine 7 with BF3.Et2O in DCE at 80°C. The newly synthesized title compounds 8 have been evaluated for their in vitro antimicrobial activity. Compounds 8 exhibit potent antimicrobial activity compared to that of standard drugs
Synthesis of novel benzo[4,5]imidazo[1,2-a]pyrimido- [4,5-d]pyrimidine derivatives as potent antimicrobial agents
Synthesis of novel benzo[4,5]imidazo[1,2-a]pyrimido[4,5-d] pyrimidines 5/6 has been achieved by reaction of 2-amino-4-aryl-4,10-dihydrobenzo[4,5]imidazo[1,2-a]pyrimidine-3-carbonitriles 4 with formaldehyde/urea. The key intermediate 4, is obtained by reaction of 2-aminobenzaldehyde 1 with aromatic aldehyde and malononitrile by a three-component one-pot process. The newly synthesized title compounds 5/6 have been evaluated for their in vitro antimicrobial activity. Compounds 5 and 6 exhibit potent antimicrobial activity compared to that of standard drugs
A simple and efficient one-pot synthesis of novel benzimidazo[1,2-a]- chromeno[4,3-d] pyrimidinones catalyzed by [Et3NH][HSO4]
1418-1424A simple and efficient one-pot synthesis of novel polyheterocyclic benzimidazo[1,2-a]- chromeno[4,3-d]pyrimidinones 4 via a three-component condensation of 2-aminobenzimidazole 1, aromatic aldehydes 2 and 4-hydroxy coumarin 3 catalyzed by Bronsted acid ionic liquid triethyl ammonium hydrogen sulphate [Et3NH][HSO4] under solvent-free conditions is reported. The main advantages of this protocol are short reaction time, easy work-up, operational simplicity, and excellent yields with high purity, without intervention of chromatography
Synthesis of 6,7-dihydroxy-3-aryl-5-undecyl-4,1,2-benzoxadiazines
1457-1461 Condensation of Embelin 1 with different aromatic acid hydrazides 2 in glacial acetic acid to give N1-5-hydroxy-6-undecyl-p-benzoaquinone-2-yl)-benzohydrides 3. Reductive cyclization of the product 3 with simultaneous acetylation in situ resulted in the formation of the compound 4 1-N-acetyl-6,7-diacetyl-3-aryl-5-undecyl-4,1,2-benzoxadiazine. In the final step the compound 4 is deacetylated to give the title products 5. The structures of the newly prepared compounds have been confirmed from analytical and spectral data. Some of the compounds exhibited antibacterial and antifungal activity. </smarttagtype
Synthesis and antimicrobial activity of 2-((4-(1H-benzo[d]imidazol-2-yl)-6- (2-ethylcyclopentyl) pyrimidin-2-yl)thio)-N-methylacetamide
816-822It has been possible to synthesise a brand new series of 2-((4-(1H-benzo[d]imidazol-2-yl)-6- (2-ethylcyclopentyl)pyrimidin-2-yl)thio)-N-methyl acetamide 4a-h. The reaction of 1-(1H-benzimidazol-2-yl)ethanone with 2-ethylcyclopentane carbaldehyde with ethanol and KOH yields (E)-1-(1H-benzo[d]imidazol-2-yl)-3- (2-ethylcyclopentyl)prop-2-en-1-one 1a-c. All compounds have been shown to have antimicrobial action via pharmacological study and are listed here. Chloramphenicol and Amphotericin B, two conventional antibiotics, have been compared to the antibacterial and antifungal properties of the synthetic compounds. It has been discovered that Schlenter products had spectroscopic properties worth investigating