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1.
İshak Bildirici Ahmet Şener Ekrem Atalan Abdulhamit Battal Hasan Genç 《Medicinal chemistry research》2009,18(5):327-340
A new 1H-pyrazole-3-carboxylic acid 2, along with hydrazono-pyridazinone 3, a by-product, and its derivatives 4–7 were synthesized and the structures confirmed by infrared (IR) and 1H and 13C nuclear magnetic resonance (NMR) data. These new compounds were evaluated for their antibacterial activities against Gram-positive
and Gram-negative bacteria using the tube dilution method. The minimal inhibitory concentrations (MICs) experiments revealed
that most compounds exerted inhibitor effects against Klebsiella pneumonia, Escherichia coli, Bacillus subtilus, and Xanthomonas compestris test microorganisms. Moreover, the results showed that the pyrazolo[3,4-d]pyridazine compounds were the best compounds of the series, exhibiting antibacterial activity against both Gram-positive
and Gram-negative bacteria. 相似文献
2.
A series of bioactive 3H,7H,8H,11H-9-[(5″-(6′-methyl-2-oxo-2H-[1]-4′-benzopyranoxy)-2″,4″-dihydro-[1″,2″,4″]-triazol-3″-one)methyl]-3,8,11-trioxo-dipyrano[2,3-f;2,3-c]quinoline (4) and 3H,7H,8H,11H-9-[(2′-(3″-phenyl-thiazolidin-4″-one)-phenoxymethyl]-3,8,11-trioxo-dipyrano[2,3-f;2,3-c]quinoline (7) analogs of 3H,7H,8H,11H-9-bromomethyl-3,8,11-trioxo-dipyrano[2,3-f;2,3-c]quinoline (1) have been synthesized and evaluated for their antibacterial activity against Gram-positive bacteria (S. aureus) and Gram-negative bacteria (S. typhi and E. coli). Pyranoquinolines with triazole and thiazolidine moieties exhibited promising antibacterial activity. The structures of
all synthesised compounds were confirmed on the basis of analytical and spectral data. 相似文献
3.
Nimesh R. Kamdar Dhaval D. Haveliwala Prashant T. Mistry Saurabh K. Patel 《Medicinal chemistry research》2011,20(7):854-864
Novel 5-phenyl-1,5-dihydro-2H-chromeno[2,3-d]pyrimidine-2,4(3H)-dithiones, 5-phenyl-3,5-dihydro-4H-chromeno[2,3-d]pyrimidin-4-ones, 7-phenyl-7,9-dihydro-8H pyrimido[5′,4′:5,6]pyrano[3,2-h]quinolin-8-ones, and 4-amino-5-phenyl-1,5-dihydro-2H-chromeno[2,3-d]pyrimidine-2-thiones were synthesized form 2-amino-4-phenyl-4H-chromene-3-carbonitrile. The newly synthesized compounds were characterized by IR, 1H-NMR, 13C-NMR, Mass spectra, and Elemental analysis. The compounds were evaluated for their in vitro antitubercular activity against
Mycobacterium tuberculosis H
37
Rv and antibacterial activity against Staphylococcus Aureus [ATCC-25923] and Streptococcus pyogenes [MTCC-443] as Gram-positive, Escherichia coli [ATCC-25922], and Pseudomonas aeruginosa [MTCC-441] as Gram-negative bacterial strains and antifungal activity against Aspergillus
niger [MTCC-282]. Some of these derivatives exhibited pronounced antitubercular and antimicrobial activities. 相似文献
4.
Detlef Geffken Raafat Soliman Farid S. G. Soliman Magdi M. Abdel-Khalek Doaa A. E. Issa 《Medicinal chemistry research》2011,20(4):408-420
Two series of pyrazolo[4,3-d]pyrimidin-7-ones and pyrido[2,3-d]pyrimidin-4-ones were designed, synthesised, and evaluated
for their antibacterial activities and CDKs inhibitory activities. The pyridazine derivative: 6-phenyl-5-phenylhydrazono-2,3,4,5-tetrahydropyridazine-3,4-dione
(3a) revealed activity against Staphylococcus aureus as Gram-positive bacteria while compound 2-(2-Ethoxyphenyl-5-Phenylpiperazinosulfonamido)-3H-pyrido[2,3-d]pyrimidin-4-one (13c) was showing moderate antifungal activity against Candida albicans. 相似文献
5.
Keeping the objective to build up a new structural class of potent antimicrobials, a series of some new 4-Benzimidazol-2-yl
tetrazolo[1,5-a]quinoline derivatives has been synthesized by reaction of tetrazolo[1,5-a]quinoline-4-carbaldehyde and o-phenylenediamine in the presence of an organocatalyst p-TsOH under the influence of microwave irradiation. The identity of all the compounds has been established by 1H NMR, 13C NMR, FTIR, and elemental analysis. The synthesized compounds were subjected to in vitro antimicrobial screening against
a representative panel of pathogenic strains including three Gram-positive bacteria (Bacillus subtilis, Clostridium tetani, and Streptococcus pneumoniae) and three Gram-negative bacteria (Escherichia coli, Salmonella typhi, and Vibrio cholerae) as well as two fungal organisms (Aspergillus fumigatus and Candida albicans) by employing broth microdilution method. Of the compounds studied, compound 5e demonstrated significant activity against a Gram-positive bacteria Bacillus subtilis. 相似文献
6.
Alice Maria Rolim Bernardino Alexandre Reis de Azevedo Luiz Carlos da Silva Pinheiro Júlio Cesar Borges Vinícius Lucio Carvalho Milene Dias Miranda Marcelo Damião Ferreira de Meneses Marcelo Nascimento Davis Ferreira Moacyr Alcoforado Rebello Viveca Antonia Giongo Galvão da Silva Izabel Christina Palmer Paixão de Frugulhetti 《Medicinal chemistry research》2007,16(7-9):352-369
The synthesis of new 4-(phenylamino)-1-phenyl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid (3a-l) derivatives and the new 4-[(methylpyridin-2-yl)amino]-1-phenyl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid (5a–c) derivatives was achieved with an efficient synthetic route. Ethyl 4-chloro-1-phenyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylate (1) on fusion with appropriate substituted anilines or aminopicolines gave the required new ethyl 4-(phenylamino)-1-phenyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylates (2a–l) (52–82%) or new ethyl 4-[(methylpyridin-2-yl)amino]-1-phenyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylates (4a–c) (50–60%), respectively. Subsequent hydrolysis of the esters afforded the corresponding carboxylic acids (3a–l) (86–93%) and (5a–c) in high yield (80–93%). Inhibitory effects of 4-(phenylamino)/4-[(methylpyridin-2-yl)amino]-1-phenyl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acids. Derivatives on Herpes simplex virus type 1 (HSV-1), Mayaro virus (MAY) and vesicular stomatitis
virus (VSV) were investigated. Compounds 2d, 3f, 3a, and 3c exhibited antiviral activity against HSV-1, MAY, and VSV virus with EC50 values of 6.8, 2.2, 4.8, 0.52, 2.5, and 1.0. None of these compounds showed toxicity for Vero cells. 相似文献
7.
Dhananjaya Ranganath Abhishek Mazumdar Sirisha Mulukuri Raghava Doonaboina Murty Devarakonda Mailavaram Raghu Prasad 《Medicinal chemistry research》2012,21(9):2458-2464
A novel series of 2-substituted-aminomethyl-8-phenyl-pyrazolo[3,4-d][1,3,4]thiadiazolo[3,2-a]pyrimidin-4(1H)-ones have been synthesized by treating 2-chloromethyl-8-phenyl-pyrazolo[3,4-d][1,3,4]thiadiazolo[3,2-a]pyrimidin-4(1H)-one with various nucleophiles. The chloromethyl derivative was prepared by treating 2-amino-3-mercapto pyrazolo[3,4-d]pyrimidine with one carbon donor, chloroacetic acid. The intermediate 2-amino-3-mercapto pyrazolo[3,4-d]pyrimidine was prepared by a novel, eco-friendly route starting from 2-amino-3-carbethoxy-1-phenyl-pyrazole. The target compounds exhibited broad-spectrum antibacterial activity (Kirby Bauer’s Method). 相似文献
8.
A series of 2-N-ethoxyphthalimido 3-(4-substitutedphenyl)-6,6-diphenyl-3,3a-dihydro-2H-imidazo[2,1-b]pyrazolo[3,4-d][1,3]thiazol-7(6H)-one(7a–e) and 4-(4-substituted phenyl)-2-(N-ethoxyphthalimido amino)-7,7-diphenylimidazo[2′,1′:2,3][1,3]thiazolo[4,5-d] pyrimidin-8(7H)-one (9a–e) have been designed and synthesized starting from thiohydentoin (1). The structure of all synthesized compounds has been established by IR, 1H NMR, 13C NMR and mass studies. These compounds have been screened for antimicrobial activities in order to evaluate the possibility
of the derivatives to be used as potential chemotherapeutic agents. 相似文献
9.
Alaa A. El-Tombary 《Scientia pharmaceutica》2013,81(2):393-422
In the present investigation, some new pyrazolo[3,4-d]pyrimidin-4(5H)-one derivatives (7–12) as well as fused pyrazolo[3′,4′:4,5]pyrimido[1,2-b]pyridazin-4(1H)-one (14–16) and 7,8,9,10-tetrahydropyrazolo[3′,4′:4,5]pyrimido[1,2-b]-cinnolin-4(1H)-one (17) ring systems were synthesized using the starting compound 5-amino-6-methyl-1-phenyl-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (5). The structures of the newly synthesized compounds were elucidated by IR, 1H NMR, 13C NMR, mass spectroscopy, and elemental analysis. The theoretical calculation of their lipophilicity as C log P was performed. The anti-inflammatory activity of all newly synthesized compounds was evaluated using the carrageenan-induced paw edema test in rats using indomethacin as the reference drug. Ulcer indices for the most active compounds were calculated. Seven compounds (10b, 11a–f) showed consistently good anti-inflammatory activity. In particular, 5-{[4-(4-bromophenyl)-3-(4-chlorophenyl)-1,3-thiazol-2(3H)-ylidene]amino}-6-methyl-1-phenyl-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (11e) and its 3,4-bis(4-chlorophenyl) analog (11f) were found to be the most effective among the other derivatives, showing activity comparable to that of indomethacin with minimal ulcerogenic effects. Correlation of the biological data of the active compounds with their theoretically calculated C log P values revealed that lipophilicity influences the biological response. 相似文献
10.
Hao Yang Liang Fang Zhu-Bo Li Fang-Kui Ren Li-Ying Wang Xiao Tian Dong-Soo Shin Hua Zuo 《Medicinal chemistry research》2011,20(1):93-100
New benzo[b][1,4]thiazin-3(4H)-one derivatives (compounds 12a–p) were synthesized via Smiles rearrangement and assayed in vitro for their antimicrobial activity against Gram-positive, Gram-negative
bacteria and fungi. The antimicrobial activity of the benzo[b][1,4]thiazin-3(4H)-ones showed, on the whole, potent toward all tested Gram-positive and Gram-negative microorganism (minimal inhibitory concentration
ranging from 16 to 64 μg/ml), whereas weak effectiveness was exhibited against fungi. Data obtained suggested that 12g, 12i, and 12o exerted the best antibacterial activity against Gram-positive bacteria and compound 12b demonstrated the best inhibition of Gram-negative bacteria. These observations provide some predictions to design further
antimicrobial active compounds prior to their synthesis following with molecular modeling studies. 相似文献
11.
Heterocycles via Mannich Bases, VII: Synthesis of Pyrazolo[1,5-a]pyrido[2,3-d]pyrimidin-9(4H)-ones The title compounds 4 are synthesised from 5-amino-3-methylpyrazolo[1,5-a]pyrimidin-7(4H)-one (2) and ketone Mannich bases or dehydro Mannich bases. 相似文献
12.
Foroumadi A Firoozpour L Emami S Mansouri S Ebrahimabadi AH Asadipour A Amini M Saeid-Adeli N Shafiee A 《Archives of pharmacal research》2007,30(2):138-145
A series ofN-[5-(chlorobenzylthio)-1,3,4-thiadiazol-2-yl] piperazinyl quinolone derivatives (4a-1) have been synthesized by reaction of piperazinyl quinolones with 5-chloro-2-(chloroben-zylthio)-1,3,4-thiadiazoles. Their
structures were confirmed by elemental analysis, IR and NMR spectra. The antibacterial activities of4a-1 against a variety of Gram-positive and Gram-negative bacteria were determined. Several compounds showed a good antibacterial
activity against Gram-positive bacteria among which, compound 4e with a 2-chlorobenzylthio moiety in ciprofloxacin derivative,
exhibited high activities againstStaphylococcus aureus andStaphylococcus epidermidis (MIC=0.06 μg/mL). The structure-activity relationship (SAR) study revealed that the position of chlorine atom on benzyl moiety
would dramatically affect the antibacterial activities of the synthesized compounds. 相似文献
13.
Mulabagal Vanisree Ch. Bheemasankara Rao 《Journal of Asian natural products research》2013,15(1):23-29
Abstract A new ceramide, (2S,3R,4E)-1,3-dihydroxy-2-[(hexadecanoyl)amino]-nonadeca-4-ene (1), cholest-5-en-3β,7β,19-triol (2), identified as its, peracetyl derivative (3), and batyl alcohol (4) were isolated from Pseudopterogorgia species. 1 exhibited antibacterial activity against Gram-positive and Gram-negative bacteria. 相似文献
14.
Angela Hayes N. Yi Mok Manjuan Liu Ching Thai Alan T. Henley Butrus Atrash 《Xenobiotica; the fate of foreign compounds in biological systems》2017,47(9):771-777
1.?We have previously described C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-one derivatives as cell permeable inhibitors of the KDM4 and KDM5 subfamilies of JmjC histone lysine demethylases.2.?Although exemplar compound 1 exhibited moderate clearance in mouse liver microsomes, it was highly cleared in vivo due to metabolism by aldehyde oxidase (AO). Similar human and mouse AO-mediated metabolism was observed with the pyrido[3,4-d]pyrimidin-4(3H)-one scaffold and other C8-substituted derivatives.3.?We identified the C2-position as the oxidation site by LC-MS and 1H-NMR and showed that C2-substituted derivatives are no longer AO substrates.4.?In addition to the experimental data, these observations are supported by molecular modelling studies in the human AO protein crystal structure. 相似文献
15.
Anna Bielenica Jerzy Kossakowski Marta Struga Izabela Dyba?a Paolo La Colla Elena Tamburini Roberta Loddo 《Medicinal chemistry research》2011,20(8):1411-1420
The preparation of twelve aminoalkanol derivatives of 2,3-dihydro-5H-[1,4]dithiino[2,3-c]pyrrole-5,7(6H)-dione was described. Newly obtained compounds, as well as their propyl and butyl analogues, were evaluated in vitro against
selected viruses. Selected derivatives were tested for their antibacterial and antifungal activity. Compounds 3h, 3j, 4b and 5a–d showed moderate to significant protections against CVB-2, HSV-1 and YFV viruses. The molecular structures of 4a, 5c and 5g were determined by an X-ray analysis. 相似文献
16.
Diuretics, III: 4-Aminopyrazolo[3,4-d]pyrimidines with Carbocyclic or Heterocyclic Substituents at N-1 As analogues of the diuretically active 4,6-diamino-1-(2-pyridyl)-1H-pyrazolo[3,4-d]pyrimidine, the 4-aminopyrazolo[3,4-d]pyrimidines 3a–g were prepared by condensation of the 5-amino-4-cyanopyrazoles 1a–g with formamide (2) . 相似文献
17.
Aamer Saeed Hummera Rafique Zaman Ashraf 《Journal of Asian natural products research》2013,15(2):130-135
Synthesis of the 6-hydroxy-7-methyl analog of typharin (8-dihydroxy-3-styryl-3,4-dihydroisocoumarin) isolated from the rhizomes of Typha capensis has been described. Direct condensation of 3,5-dimethoxy-4-methylhomophthalic acid (1) with cinnamoyl chloride at elevated temperature under inert conditions afforded 6,8-dihydroxy-7-methyl-3-styrylisocoumarin (2). Hydrolysis of isocoumarin to keto acid (3) followed by reduction and cyclodehydration of hydroxy acid analog (4) afforded ( ± )-6,8-dimethoxy-3-(4-methoxyphenyl)-3,4-dihydroisocoumarin (5). Demethylation of the latter using anhydrous aluminum chloride/ethane thiol furnished the title isocoumarin (6). Compounds (1–6) were screened for in vitro antibacterial activity against a representative panel of Gram-positive and Gram-negative bacteria using levofloxacin as the reference drug. 相似文献
18.
New aminopyrazolo[1,5-a]pyrimidines, pyrazolo[3,4-d]pyrimidines and imidazo[1,2-b]pyrazoles were synthesised from ethyl 3,5-diaminopyrazole-4-carboxylate (1) . 相似文献
19.
A new series of substituted 1-(2-ethylphenyl)-2-oxo-1,2-dihydropyridine-3-carbonitriles have been synthesized. Moreover, substituted
bicyclic derivatives e.g. thieno[3,4-c]pyridone, pyrido[3,4-c]pyridone, benzo[c]pyridone, and tricyclic derivatives, chromeno[3,4-c]pyridones have been prepared and evaluated for their antifibrotic activity. Among the tested compounds, compounds 4d and 5a exhibited potent antifibrotic activity without harmful side effects on liver and kidney functions. Detailed synthesis, spectroscopic
and biological data are reported. 相似文献
20.
Fa-Sheng Li Liang Xu Xiao-Feng Chi Ting-Guo Kang Hai-Xue Kuang 《Journal of Asian natural products research》2013,15(7):639-642
Two new phenolic glycosides were isolated from the seeds of Cucurbita moschata. Their structures were elucidated as (2-hydroxy)phenylcarbinyl 5-O-benzoyl-β-d-apiofuranosyl(1 → 2)-β-d-glucopyranoside (1) and 4-β-d-(glucopyranosyl hydroxymethyl)phenyl 5-O-benzoyl-β-d-apiofuranosyl(1 → 2)-β-d-glucopyranoside (2) on the basis of spectroscopic analysis and chemical evidence. 相似文献