共查询到20条相似文献,搜索用时 46 毫秒
1.
Y. Rajendra Prasad G. V. Suresh Kumar S. M. Chandrashekar 《Medicinal chemistry research》2013,22(5):2061-2078
A focused library of 4,5-dihydropyrazole dervivatives (4, 5, 6, 7a–h, 8, 9a–g, and 10a–g) were synthesized from novel 5-(2,6-difluorophenyl)-3-phenyl-4,5-dihydropyrazole-1-carbothioamide 4. The synthesized compounds were characterized using elemental analysis and spectral data (IR, mass spectra, 1H and 13C NMR) and evaluated for antimicrobial activity by broth dilution method and in vitro anticancer activity. Among the synthesized compounds 7a, 9c, 9g, and 10d exhibit broad spectrum antimicrobial activity against tested microbial strains. The in vitro cancer results ascertain 7a, 9c, and 10d are most potent molecules in comparison to reference standard cisplatin. 相似文献
2.
New series of [1,3,4]thiadiazolo[3,2-a]pyrimidines, [1,3,4]thiadiazolo[2,3-b]quinazolines, and pyrimido[2,1-b][1,3]benzothiazoles have been synthesized and characterized by analytical and spectrometrical methods (IR, MS, 1H, and 13C NMR). Sixteen of the synthesized compounds; namely, 3a, b, 5a–f, 8a, b, 10, 11a–c, and 13a, b were screened for antibacterial activity against Escherichia coli, Staphylococcus aureus, and Bacillus cereus. They were found to be either moderately active, slightly active or inactive against the selected microorganisms. The antifungal activity of these compounds were also tested against Candida albicans, Aspergillus fumigatus 293, and Aspergillus flavus 3375. Compound 11a showed potent antifungal activity against the three selected fungi; the rest of the tested compounds displayed either weaker activity or were completely inactive. The same compounds were examined for antiquorum-sensing activity against Chromobacterium violaceum ATCC 12472, where compounds 3a, 10, 11a, and 13a, b exhibited promising activity. The in vitro cytotoxic activity of these compounds was also studied by brine shrimp lethality bioassay, and results indicated that compounds 3a, 11a, and 13a have the highest cytotoxic activity. 相似文献
3.
Jianwen Yao Jing Chen Zuopeng He Wei Sun Hao Fang Wenfang Xu 《Medicinal chemistry research》2013,22(8):3959-3968
A series of novel sorafenib derivatives containing diaryl thiourea and thioether, 9a–u, was designed and synthesized, and their antiproliferative activities against HCT116 and MDA-MB-231 cell lines were also evaluated and described. Most compounds exhibited potent antiproliferative activity against HCT116 cells with IC50 = 1.8–80.4 μM. Compounds 9p, 9r, and 9s demonstrated competitive antiproliferative activities to sorafenib, against all two cancer cell lines. The structures of all the newly synthesized compounds were determined by 1H NMR, 13C NMR, and HRMS, and compound 9n was characterized by single-crystal X-ray diffraction. Primary structure–activity relationships (SAR) have also been established. 相似文献
4.
Pawan K. Sharma Satish Kumar Pawan Kumar Pawan Kaushik Chetan Sharma Dhirender Kaushik Kamal R. Aneja 《Medicinal chemistry research》2012,21(10):2945-2954
A new series of 1-(4-aminosulfonylphenyl)-3,5-diaryl pyrazolines (5) was synthesized by the reaction of appropriate chalcones 3 with 4-hydrazinobenzenesulfonamide hydrochloride (4) in ethanol in the presence of catalytic amount of acetic acid. All newly synthesized compounds were in vivo evaluated for their antiinflammatory activity using carrageenan-induced rat paw edema assay. Five of the newly synthesized compounds, 5d, 5g, 5h, 5i, and 5m displayed significant antiinflammatory activity, greater than 55% inhibition 3?h after the carrageenan injection. All the newly synthesized compounds were evaluated for their in vitro antimicrobial activity against two Gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis); two Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa), and two yeast (Candida albicans and Saccharomyces cerevisiae). Some of the newly synthesized compounds 5a, 5f, 5g, 5h, 5j, and 5k showed excellent antifungal activity, greater than the reference drug amphotericin B, against Saccharomyces cerevisiae. 相似文献
5.
Piyush P. Savaliya Vikunjana K. Akbari Jigisha A. Modi Keshav C. Patel 《Medicinal chemistry research》2013,22(12):5789-5797
The title compounds (5a–j), (6a–j), and (7a–j) were prepared via a four-step procedure using starting material 4-methoxyaniline (1). The structure of all synthesized compounds was confirmed by FT-IR, 1H NMR, 13C NMR, and CHN analysis. The synthesized compounds were tested for their antibacterial and antifungal activity (MIC) in vitro against organisms viz. B. subtilis, S. aureus, E. coli, P. aeruginosa, and C. albicans taking ciprofloxacin, ampicillin, streptomycin, penicillin-G, fluconazole, and nystatin as the standard drugs. Some of the compounds have shown significant activities. 相似文献
6.
Amlipur Santhoshi Partha Sarathi Sadhu Rekulapally Sriram Chebolu Naga Sesha Sai Pavan Kumar Budde Mahendar Manda Sarangapani Vaidya Jayathirtha Rao 《Medicinal chemistry research》2013,22(7):3329-3340
A facile route for the synthesis of 20 new 1,4-disubstituted tetrazolone derivatives from allyl bromides of Baylis–Hillman adducts and various 1-substituted tetrazolones is described. All the synthesized compounds were screened for in vitro antibacterial and antifungal activity. Out of 20 newly synthesized compounds 16 compounds showed very good activity against the Gram-positive bacteria Bacillus subtilis compare to the standard drug ciprofloxacin. The compounds 7b, 7n and 7o showed remarkable activity against both the Gram-positive bacteria B. subtilis and Staphylococcus aureus. Two compounds 7l and 7o showed very good activity against the Gram-negative bacteria Escherichia coli. The compounds, when tested for antifungal activity four compounds— 7b, 7l, 7o and 7s— showed very good activity against the strain Aspergillus niger, whereas seven compounds— 7e, 7g, 7h, 7l, 7o and 7s— display good activity against Candida albicans. Compounds 7b, 7e, 7g, 7l and 7o exhibited very good-to-high activity towards all the strains tested. 相似文献
7.
Synthesis, characterization, and antimicrobial evaluation of novel naphthalene-based 1,2,4-triazoles
N. C. Desai P. N. Shihora K. M. Rajpara V. V. Joshi H. V. Vaghani H. M. Satodiya A. M. Dodiya 《Medicinal chemistry research》2012,21(10):2981-2989
In order to search for new bioactive molecules with significant antimicrobial action, a series of 1,2,4-triazole and naphthalene analogs bearing structurally diverse substituents, N-(3-mercapto-5-(naphthalen-1-yl)-4H-1,2,4-triazol-4-yl)(aryl)amides 3a–l were synthesized in good yield by a multi-step synthetic procedure. Their antimicrobial activity was screened against various Gram-positive and Gram-negative bacteria and fungi. Compounds 3a, 3f, 3g, 3j, and 3k exerted strong inhibition of the investigated bacterial and fungal strains compared to control antibiotic ampicillin and antifungal griseofulvin. On the basis of statistical analysis, it is observed that the compounds give significant co-relation. All the synthesized compounds have been characterized by IR, 1H NMR, 13C NMR, and mass spectral data. 相似文献
8.
Aletti S. Praveen Hemmige S. Yathirajan Badiadka Narayana Balladka K. Sarojini 《Medicinal chemistry research》2014,23(1):259-268
A series of novel N-[4-(substituted)-1,3-thiazol-2-yl]-2-(substituted)acetamide (9a–m) and methyl 2-(2-(2-(substituted)acetamido)thiazol-4-yl)acetate (9n–o) derivatives have been synthesized and compounds were characterised by spectral and analytical studies. All compounds were screened for their in vitro antibacterial activity against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumonia by disc diffusion method and for antifungal activity against Penicillium marneffei, Trichophyton mentagrophytes, Aspergillus flavus and Aspergillus fumigatus by serial plate dilution method. Compounds 9b, 9e, 9m and 9o exhibited growth inhibition against all the tested bacterial strains, with MIC values varying from 12.5 to 6.25 μg/ml. Among the compounds tested for antifungal activity, 9a, 9b, 9d, 9j, 9k, 9p and 9n showed wide range of activity against all the tested strains. Most of the newly synthesized compounds were effective against fungal strains rather than bacterial strains. However, some of the compounds like 9a, 9e, 9j, 9k and 9i showed selective sensitivity against some of the bacterial strains whereas they were unable to sustain the growth of other strains. 相似文献
9.
Burcu Çalışkan Akın Yılmaz İlker Evren Sevda Menevşe Orhan Uludag Erden Banoglu 《Medicinal chemistry research》2013,22(2):782-793
In this article, we synthesized a series of novel 1-benzyl-5(3)-p-tolyl-1H-pyrazole-3(5)-carboxylic acid derivatives and characterized by IR, 1H NMR, and mass spectroscopy. Compounds were evaluated for their in vivo analgesic and anti-inflammatory activity using the p-benzoquinone-induced writhing test and the carrageenan-induced paw edema model, respectively. Out of 14 compounds tested, 7a, 7c, 7e, 7f, 7i, 8a–b, and 8f–g exhibited potent analgesic and/or anti-inflammatory activity as compared to reference drugs aspirin and indomethacin. Anticancer activity of these compounds was assessed against five cancer cell lines with the MTT assay (HL-60, human promyelocytic leukemia cells; HeLa, human cervical cancer cells; Raji, human B lymphocyte cell line; MCF7, human breast adenocarcinoma cell line; MDA-MB-231, estrogen-independent human breast cancer cell line). Compounds 7a, 8a, and 8b with high anti-inflammatory activity, and also 7d and 7j with mild anti-inflammatory activity exhibited promising anticancer activity against some selected cell lines. 相似文献
10.
G. Govinda Rajulu Halehatty S. Bhojya Naik G. Charan Kumar S. Ramaraj Ganesh Sambasivam Kesavan Poonimangadu Koppolu 《Medicinal chemistry research》2014,23(6):2856-2868
A series of nine new N-(substituted azetidine-3-carbonyl)-N-methyl-hydrazino derivatives at C-7 position of fluoroquinolones were designed and synthesized through multistep synthesis. The synthesized compounds were characterized by 1H NMR, 13C NMR, ESI–MS and IR. The new compounds were tested for their in vitro antimicrobial and anti-proliferative activity. Out of the nine derivatives, compound 6i exhibited good antibacterial activity by inhibiting the growth of Methicillin-sensitive Staphylococcus aureus, Methicillin-resistant S. aureus and ATCC 35218 Escherichia coli (MIC: 0.25–16.00 μg/mL). Compounds 6c, 6g–h are displayed good growth inhibition against MCF-7 Breast carcinoma, HCT-116 Colon carcinoma and A549 Lung adenocarcinoma cell lines. Compound 6h is the most active against MCF-7 cell line with superior growth inhibition compared to ciprofloxacin and reference anticancer drug SAHA. 相似文献
11.
Maryam Mohebbi Peyman Salehi Morteza Bararjanian Atousa Aliahmadi Reihaneh Safavi-Sohi Jahan B. Ghasemi 《Medicinal chemistry research》2014,23(10):4531-4541
New derivatives of 1,2,3-triazolyl 7-carboxamidodesacetoxy cephalosporanic acid were synthesized using alkyne-azide 1,3-dipolar cycloaddition. The synthesized compounds were evaluated for their antibacterial activity against a collection of Gram-positive and Gram-negative bacteria and also in synergy with cefixime and cephalexin. Some compounds inhibited vancomycin-resistant strain of Enterococcus faecium (MIC = 8 µg/mL) and in the synergy experiments compounds 13a, 13f, and 13g decreased the level of MIC against an ESBL strain of Klebsiella pneumonia. A comparative molecular field analysis has been carried out, and the effect of substituents on the antibacterial activities of the synthesized compounds was explained. 相似文献
12.
3-(Aryl)-2-(2-chlorophenyl)-6-{2-[2-(2-chlorophenyl)-4-oxo(3-hydroquinazolin-3yl)]ethyl}-3-hydroquinazolin-4-ones had been selected as target bio-active molecules. Several quinazoline derivatives were prepared by using anthranilic acid, acid chloride, 2-amino-ethanol, and different amines. Newly synthesized compounds were screened for their antibacterial and antifungal activities on Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Staphylococcus pyogenes, Candida albicans, Aspergillus niger, and Aspergillus clavatus. The compounds 5e, 5g, and 5h are shown to have excellent activity, while 5c, 5d, 5i, 5k, 5l are shown to have very good activity against several strains of bacteria. The structures of the synthesized compounds were firmly established by well-defined spectral analysis techniques like IR, 1H-NMR, 13C-NMR, and Mass spectra. 相似文献
13.
Sheelavanth Shankerrao Yadav D. Bodke Sundar S. Mety 《Medicinal chemistry research》2013,22(3):1163-1171
A new series of phenolic esters 2(a–j) and amides 3(a–c) of 2-(1-benzofuran-2-yl) quinoline-4-carboxylic acid were synthesized by the reaction of 2-(1-benzofuran-2-yl)-quinoline-4-carboxylic acid (1) with various substituted phenols and secondary amines using ethyl-(N′,N′-dimethylamino)propyl carbodiimide hydrochloride (EDC.HCl) as a coupling agent. The newly synthesized compounds were evaluated for in vitro antioxidant and antibacterial activity. Among all tested compounds 2a, 2c, 2e, and 2h showed good chelating ability with Fe+2 ions, whereas compounds 2g and 2j exhibited good scavenging activity with DPPH free radicals. Concerning antibacterial activities compounds 2a, 2b, 2c, and 2h were found to be equipotent to ampicillin against Enterococcus sp and Staphylococcus aureus, while compound 2e is found to be as potent as ampicillin against Pantoea Dispersa and Ochrobactrum sp. amide derivatives 3(a–c) were found to be less potent when compared to standard. 相似文献
14.
Rohit Singh Gurubasavaraj V. Pujar Madhusudan N. Purohit V. M. Chandrashekar 《Medicinal chemistry research》2013,22(5):2163-2173
A series of asymmetric bis-1,2,4-triazoles (4a–l) were synthesized from respective 1,2,4-triazole-3-thiocarbohydrazides (2a, b) via base catalyzed dehydrative cyclization of thiosemicarbazide intermediates (3a–l). The synthesized compounds were characterized by IR, 1H-NMR, 13C-NMR, and Mass spectral studies. The asymmetric bis-1,2,4-triazole derivatives (4a–l) were evaluated for in vitro antioxidant activity by DPPH radical scavenging assay method. The compounds with significant antioxidant potential were evaluated for in vitro cytotoxicity by MTT assay method against HT29 (Human adenocarcinoma) and MDA-231 (Human breast cancer) cancer cell lines. All the synthesized compounds were evaluated for in vitro antibacterial activity against Bacillus subtilus (ATCC 6633), Staphylococcus aureus (ATCC-25923), Escherichia coli (ATCC-25922), and Pseudomonas aeruginosa (ATCC-27853). 相似文献
15.
Om Prakash Deepak K. Aneja Poonam Lohan Khalid Hussain Sanjiv Arora Chetan Sharma Kamal R. Aneja 《Medicinal chemistry research》2012,21(10):2961-2968
A series of 5-((3-aryl-1-phenyl-1H-pyrazol-4-yl)methylene)thiazolidine-2,4-diones was synthesized by Knoevenagel condensation of various 3-aryl-1-phenyl-1H-pyrazole-4-carbaldehydes (1a–h) with thiazolidine-2,4-dione (2) in ethanol in the presence of piperidine. All compounds were screened for their in vitro antibacterial (Staphylococcus aureus, Bacillus subtilis, Pseudomonas aeruginosa and Escherichia coli) activity and compared with the commercially available antibiotic, ciprofloxacin. All compounds showed good activity against gram-positive bacteria, however, none of the compounds were found to be effective against gram-negative bacteria. Compound 3g was found to be most potent member among all the compounds showing MIC of 16?μg/ml against S. aureus and 32?μg/ml against B. subtilis. All the synthesized compounds were also tested for their in vitro antifungal (Aspergillus niger and A. flavus) activity and compared with commercially available fluconazole. They showed excellent antifungal activity. Compounds 3b, 3e, 3f and 3g were active against both fungi showing more than 60% inhibition. Compound 3e was found to be superior to the reference drug. 相似文献
16.
C. P. Kaushik Kashmiri Lal Ashwani Kumar Sunil Kumar 《Medicinal chemistry research》2014,23(6):2995-3004
A small library of amino acid-linked 1,4-disubstituted 1,2,3-bistriazole conjugates has been synthesized from the N-protected l-amino acids propargyl esters through one-pot click reaction. All the newly synthesized compounds were tested in vitro for antimicrobial activity against Gram-positive (Staphylococcus aureus, Bacillus subtilis), Gram-negative (Escherichia coli) bacteria and fungi (Candida albicans, Aspergillus niger). The antibacterial evaluation data indicated that compounds 3c, 3h, 5a, 5b, 5c, 5d, 5e, 5g, and 5h exhibited comparable activity to standard ciprofloxacin. However, the bistriazoles 3b, 3c, 3e, 3f, and 3g showed good antifungal activity than others against both fungi. Further, docking simulation of the two most active compounds 5c against S. aureus tyrosyl tRNA synthetase and 5h into E. coli topoisomerase II DNA Gyrase B, respectively, was also performed. 相似文献
17.
Pawan Kumar Sharma Prabal Bandyopadhyay Pratibha Sharma Ashok Kumar 《Medicinal chemistry research》2014,23(7):3569-3584
A series of 7-hydroxy-2-aryl-6-aryldiazenyl-4H-chromen-4-one derivatives (6a–m) was synthesized in quantitative yields and their structures were corroborated on the basis of FT-IR, 1H, 13C NMR, ESI–MS, and elemental analysis data. The synthesized compounds were screened for in vitro antibacterial activities against a representative panel of Gram-positive and Gram-negative bacteria, as well as to evaluate their antioxidant potential using DPPH assay method. Bio-evaluation studies revealed that compounds 6c, 6d, 6e, 6j, and 6l exhibited moderate to good antibacterial activity against all the tested bacterial strains. Furthermore, from the antioxidant screening results, it has been observed that compounds 6c, 6e, and 6g manifested profound antioxidant potential (IC50 <7.68 μM) in comparison to the standard antioxidant ascorbic acid. 相似文献
18.
J. John Francis Xavier R. Venkateswaramoorthi A. Kamaraj K. Krishnasamy 《Medicinal chemistry research》2013,22(11):5105-5111
Substituted 2-(benzothiazol-2-yl)-1-(alkyl-2,6-diarylpiperidin-4-ylidine)hydrazines 10–17 were synthesized by the condensation of different 2r,6c-diarylpiperidin-4-ones 1–8 with 2-hydrazinobenzothiazole 9. All the synthesized compounds were investigated in solution and in the solid state by IR, 1H, 13C and 2D NMR spectral techniques. The structure–activity relationships were studied by the screening of the antimicrobial activity over a representative panel of bacterial and fungal strains using two-fold serial dilution method. 相似文献
19.
N. C. Desai D. D. Pandya K. A. Bhatt G. M. Kotadiya Priyanka Desai 《Medicinal chemistry research》2014,23(8):3823-3835
A series of 6-(1H-benzo[d]imidazol-2-yl)-2-(2-(3-nitrophenyl)-4-oxothiazolidin-yl)-4-(aryl)nicotinonitriles 5a–l were synthesized and characterized by IR, 1H NMR, 13C NMR, and mass spectrometry techniques. These novel compounds 5a–l were screened for their in vitro antimicrobial activity against different bacterial and fungal strains and in vitro cytotoxicity study (HeLa cell line) using MTT colorimetric assay. The results demonstrated that compounds 5c, 5e, and 5i–k exhibited excellent antibacterial activity, while compounds 5d, 5i, and 5k were found to be the most potent antifungal agents. From the standpoint of SAR studies, it was observed that the presence of electron donating groups remarkably enhanced the antimicrobial activity of newly synthesized compounds. Further, the results of preliminary MTT cytotoxicity studies on HeLa cells suggested that potent antimicrobial activity of 5c–e and 5i–k was accompanied by low cytotoxicity. 相似文献
20.
Navin B. Patel Hemant R. Patel Faiyazalam M. Shaikh Dhanji Rajani 《Medicinal chemistry research》2014,23(3):1360-1370
New thiazolidinones 5a–o were prepared from Schiff base 4a–o and thioglycolic acid in the presence of ZnCl2 from 4-[2-(5-ethylpyridin-2-yl)ethoxy]benzaldehyde. The structures of the synthesized compounds were assigned on the basis of elemental analysis, IR, 1H NMR 13C NMR, and mass spectral data. All the compounds were screened against different strains of bacteria and fungi. Compounds 4e, 4n, 4m, 4o, 5e, 5f, 5j, and 5m possessed very good activity against bacterial and fungal species. These active compounds impelled us to study their antitubercular activity. Schiff base 4n and 4e showed M. tuberculosis MIC value 25 and 62.5 μg/ml, respectively. Thiazolidinone 5m displayed M. tuberculosis MIC at 25 μg/ml, which is better antitubercular activity compared with rifampicin. 相似文献