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Rajesh Kumar Pradeep Kumar Mahesh Kumar Balasubramanian Narasimhan 《Medicinal chemistry research》2012,21(12):4301-4310
A series of 4-amino-3-hydroxy-naphthalene-1-sulfonic acid derivatives (1–18) was synthesized and tested in vitro for its anti-microbial potential. The results of anti-microbial studies indicated that derivatives having 3,4,5 trimethoxy (6) and 2,4 dichloro (17) groups on benzylidene amino portion were found to be most effective ones. The mt-QSAR model for anti-microbial activity revealed the importance of topological parameter, valence zero-order molecular connectivity index (0χv) in describing the anti-microbial activity of synthesized 4-amino-3-hydroxy-naphthalene-1-sulfonic acid derivatives. 相似文献
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Triazoles with different substituent groups are found to possess diverse applications in the field of medicine and industry. A series of 4-(substituted ethanoyl)amino-3-mercapto-5-(4-nitro)phenyl-1,2,4-triazoles (NU-1 to NU-15) were synthesized as novel antimicrobial agents starting from 4-nitrobenzoic acid. The chemical structures of these newly synthesized compounds were elucidated by IR, 1H NMR, 13C NMR, FAB+ -MS spectral data and elemental analysis. Their antimicrobial activities against Staphylococcus aureus (ATCC-25923), Pseudomonas aeruginosa (ATCC-27853), Escherichia coli (ATCC-8739), Bacillus substilis (ATCC-6633), Candida albicans (MTCC-227), Aspergillus niger (MTCC-3323) and Fusarium oxysporum (MTCC-2087) were investigated. 相似文献
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The ergolines are an important class of dopamine receptor agonists1), and the identification of their dopaminergic pharmacophore has been sought as a means of developing “purer” agonists related to these structures2). Ergolines combine a phenethylamine and a pyrroleethylamine moiety, both of which have been proposed as the dopaminergic pharmacophores of the molecules3,4). Support for these postulates is the fact that certain simplified partial ergoline structures5,6) show potent dopamine agonist activities. The simple 3-(2-aminoethyl)pyrrole was also synthesized6) but it was found inert as a dopamine receptor agonist. This inactivity was rationalized on the basis that this primary amino compound is rapidly destroyed in vivo by monoamine oxidases6). 相似文献
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Rajesh H. Tale Atish H. Rodge Girish D. Hatnapure Ashish P. Keche Kalpana M. Patil Rajendra P. Pawar 《Medicinal chemistry research》2013,22(3):1450-1455
A new series of 4-(3-arylureido)phenyl-1,4-dihydropyridine urea derivatives were synthesized using simple three component condensation, reduction, and nucleophilic addition sequence in moderate to good yields. All the synthesized compounds 6a–j were evaluated for their anti-inflammatory [against the pro-inflammatory cytokines (tumor necrosis factor-alpha, TNF-α and interleukin-6, IL-6)] and anti-microbial activity (anti-bacterial and anti-fungal). Among all the compound screened, the compound 6b, 6f, and 6j were found to have promising anti-inflammatory activity, 74–83 % TNF-α and 91–96 % IL-6 inhibitory activity, respectively as compared to the standard dexamethasone (71 and 86 % inhibition) but at the MIC of 10 μM/ml. The compounds 6d–e and 6h exhibited relatively lower TNF-α and IL-6 inhibitory activity and found to be moderately potent anti-inflammatory agents. The compounds 6c–e, 6g, and 6i were found to be promising anti-bacterial and anti-fungal agents and remarkably some of the new compounds, viz. 6d and 6i were found be more potent than the standard ciprofloxacin or miconazole. It is to be noted that this is the first report on the anti-inflammatory activity evaluation of novel 1,4-dihydropyridine urea derivatives against the important molecular target, TNF-α, and IL-6. 相似文献
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Agarwal HK Chhikara BS Hanley MJ Ye G Doncel GF Parang K 《Journal of medicinal chemistry》2012,55(10):4861-4871
A number of fatty acyl derivatives of (-)-2',3'-dideoxy-3'-thiacytidine (lamivudine, 3TC, 1) were synthesized and evaluated for their anti-HIV activity. The monosubstituted 5'-O-fatty acyl derivatives of 3TC (EC(50) = 0.2-2.3 μM) were more potent than the corresponding monosubstituted N(4)-fatty acyl (EC(50) = 0.4-29.4 μM) and 5'-O-N(4)-disubstituted (EC(50) = 72.6 to >154.0 μM) derivatives of the nucleoside. 5'-O-Myristoyl (16) and 5'-O-12-azidododecanoyl derivatives (17) were found to be the most potent compounds (EC(50) = 0.2-0.9 μM) exhibiting at least 16-36-fold higher anti-HIV activity against cell-free virus than 1 (EC(50) = 11.4-32.7 μM). The EC(90) values for 16 against B-subtype and C-subtype clinical isolates were several folds lower than those of 1. The cellular uptake studies confirmed that compound 16 accumulated intracellularly after 1 h of incubation with CCRF-CEM cells and underwent intracellular hydrolysis. 5'-O-Fatty acyl derivatives of 1 showed significantly higher anti-HIV activity than the corresponding physical mixtures against the B-subtype virus. 相似文献
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A series of heterocyclic derivatives including 1,2,4-triazole-3(4H)-one (3a,b), 1H-pyrazol-5(4H)-one (4,5), 1H-pyrazol-4-carbonitrile (7), pyridine-3-carbonitrile (8, 9a,b), pyrimidine-5-carbonitrile (10a,b), methylpyrimidin-2(1H)-one or thione (11a,b), pyrimidine-5-carboxylate (12a,b), quinazolin-5(6H)-one (13a,b) and indeno [1,2-d] pyrimidin-5-one (14a,b) moieties conjugated with 1,3-disubstituted pyrazole moiety were synthesized on reaction with semicarbazide, thiosemicarbazide, 3-amino-5-oxo-2-pyrazoline, cyanoacetohydrazide, 2-acetyl thiophene, p-chloroacetophenone, urea, thiourea and 1,3-dicarbonyl compounds, respectively, by using 1-(3-chlorophenyl)-3-(4-methoxyphenyl)-1H-pyrazole-4-carboxaldehyde (2) as starting material. The structures of all the newly synthesized products have been established on the basis of analytical and spectral data. The anti-inflammatory screening showed that most of the obtained compounds were found to have significant anti-inflammatory activities with prostaglandin inhibition at a dose level of 2.5 and 5 mg/kg comparable to celecoxib as a reference control. The ulcer indices of all compounds are mainly in the safe level (UI = 2.10-4.27) except for compounds 9a and 14a, which were highly ulcerogenic. 相似文献
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A. Parthiban J. Muthukumaran A. Moushumi Priya S. Jayachandran R. Krishna H. Surya Prakash Rao 《Medicinal chemistry research》2014,23(2):642-659
A series of N-methyl-3-nitro-4-(nitromethyl)-4H-chromen-2-amine derivatives 8 were synthesized from 2-((E)-2-nitrovinyl)phenol 7 and ((E)-N-methyl)-1-(methylthio)-2-nitroethenamine 5. The cytotoxic activity of these molecules was tested against two cancer cell lines namely HeLa (cervical cancer) and HEp-2 (epidermoid laryngeal carcinoma). Among them, two molecules (4H-chromenes 8h and 8i) displayed potent anti-proliferative activity with IC50 values of 115.04 and 18.96 μM for HeLa and 86.94 and 25.08 μM for Hep-2 cell lines, respectively. Morphological evaluation of the cell lines revealed that both 8h and 8i induce the apoptotic process. Molecular docking studies of all the 4H-chromenes 8 with anti-apoptotic Bcl-2, Bcl-w, and Bcl-xL proteins revealed that the 4H-chromenes 8h and 8i have good docking score and thus corroborated in vitro studies. Furthermore, evaluation of Lipinski and ADMET properties revealed their drug-like pharmacokinetic profiles. Thus, 4H-chromenes 8h and 8i exhibit promising anti-cancer properties and can be used as lead compounds for further development. 相似文献
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Ahmad F. Eweas S. A. Swelam O. A. Fathalla N. M. Fawzy Sh. I. Abdel-Moez 《Medicinal chemistry research》2012,21(11):3848-3857
Synthesis of some new pyrazolo[3,4-d]pyrimidine derivatives using readily available starting materials are described. A one-pot multi component cyclocondensation reaction was used to prepare the novel 3-methyl-4-aryl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidine-6-thiol which served as a new starting material for all new compounds in this research. The anti-microbial activities of the selective synthesized compounds have been evaluated. Some of the newly prepared compounds were found to have moderate to strong anti-microbial activity, e.g., compound 4a, 6a, and 8, in comparison to the reference drugs. Molecular modeling of the most three biologically active new compounds 4a, 6a, and 8 compared to the reference drugs tobramycin and fluconazole was carried out using Fieldalign 2.0 software. 相似文献
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The synthesis of 2,4-dione derivatives of 1,5-benzodithiepine, 1,5-benzodiazepine and 1,5-benzothiazepine and the anti-microbial activity in vitro of these derivatives and of analogous of 1,5-benzodioxepine, 1,5-benzoxathiepine and 1,5-benzoxazepine, previously prepared, are reported. Some of these compounds showed a good activity against some Gram positive microorganisms and blastomycetes. 相似文献
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Alaa A. El-Tombary Yasser S. Abdel-Ghany Ahmad S. F. Belal Shams A. Shams El-Dine Farid S. G. Soliman 《Medicinal chemistry research》2011,20(7):865-876
In search for novel anti-cancer and anti-microbial agents with promising pharmacotoxicological profile, the synthesis of some
substituted 4-halofuran-2(5H)-ones (8a–l, 9, 11) and derived halogenated quinoxalin-2(1H)-ones (12a–d) is described. Some of the halogenated furanones were readily oxidized to the corresponding 2-bromo-2-propenoic acids (13a–c) with hydrogen peroxide in alkaline medium. Twenty-two compounds were preliminary tested for their in vitro activity against
three bacteria and one fungus and revealed encouraging activity. On the other hand, three compounds were screened as anti-cancer
agents using cell line panel protocol and 22 compounds were subjected to cycline-dependent kinases (CDKs) inhibition screening
program but were inactive. 相似文献
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J P Yevich J S New D W Smith W G Lobeck J D Catt J L Minielli M S Eison D P Taylor L A Riblet D L Temple 《Journal of medicinal chemistry》1986,29(3):359-369
Members of the series of title compounds were tested for potential antipsychotic activity in relevant receptor binding assays and behavioral screens. Structure-activity relationships within the series are discussed. Compound 24 (BMY 13859-1), a (1,2-benzisothiazol-3-yl)piperazine derivative, was selected for further study because of its potent and selective profile in primary CNS tests. It was active in the Sidman avoidance paradigm and blocked amphetamine-induced stereotyped behavior in dogs for up to 7 h. The compound's lack of typical neuroleptic-like effects in the rat catalepsy test and its failure to produce dopamine receptor supersensitivity following chronic administration indicate that it should not cause the movement disorders commonly associated with antipsychotic therapy. Although 24 has potent affinity for dopaminergic binding sites, its even greater affinity for serotonin receptors suggests that a serotonergic component may be relevant to its atypical profile. Compound 24 is currently undergoing clinical evaluation in schizophrenic patients. 相似文献
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Beadle JR Wan WB Ciesla SL Keith KA Hartline C Kern ER Hostetler KY 《Journal of medicinal chemistry》2006,49(6):2010-2015
9-(S)-(3-Hydroxy-2-phosphonomethoxypropyl)adenine [(S)-HPMPA] was one of the first acyclic nucleoside phosphonates described and has been reported to have good antiviral activity against most double-stranded DNA viruses, including the herpes group viruses and the orthopoxviruses. However, (S)-HPMPA is not orally bioavailable and has not been developed for clinical use. We have prepared orally bioavailable lipid esters of (S)-HPMPA and report their synthesis and antiviral evaluation against cytomegalovirus and orthopoxviruses. These esters were evaluated in vitro in cells infected with human cytomegalovirus (HCMV), murine cytomegalovirus (MCMV), vaccinia (VV), and cowpox viruses (CV). The most active compound, oleyloxyethyl-(S)-HPMPA, was found to have EC50 value of 0.003 microM against HCMV vs 1.4 microM for unmodified HPMPA. In cells infected with VV and CV, octadecyloxyethyl-(S)-HPMPA had EC50 values of 0.01-0.02 microM versus 2.7-4.0 microM for unmodified HPMPA. When compared with the alkoxyalkyl esters of cidofovir, the corresponding alkoxyalkyl esters of (S)-HPMPA were equally active against HCMV and MCMV but were 15-20-fold more active against VV and CV in vitro. The alkoxyalkyl esters of (S)-HPMPA are promising new compounds worthy of further investigation for treatment of infections caused by herpes viruses and orthopoxviruses. 相似文献
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Neeraj Upmanyu Sanjay Kumar Pawan Porwal Kamal Shah Pradeep Mishra 《Medicinal chemistry research》2012,21(8):1967-1976
Triazoles and its derivatives are found to possess diverse applications in the field of medicine and industry. A series of novel 1,2,4-triazole derivatives have been synthesized as novel antimicrobial agents starting from different 4-substituted benzoic acids. The chemical structures of these newly synthesized compounds were elucidated by Fourier transform infrared spectroscopy (FTIR), 1H NMR, 13C NMR, FAB+-MS spectral data, and elemental analysis. Their antimicrobial activities were investigated against four bacterial strains S. aureus (ATCC-25923), P. aeruginosa (ATCC-27853), E. coli (ATCC-8739), B. subtilis (ATCC-6633) and three fungal strains C. albicans (MTCC-227), A. niger (MTCC-3323), and F. oxysporum (MTCC-2087). Preliminary results indicate that some of them exhibit promising activities and deserve further consideration. 相似文献
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Xu L Kulkarni SS Izenwasser S Katz JL Kopajtic T Lomenzo SA Newman AH Trudell ML 《Journal of medicinal chemistry》2004,47(7):1676-1682
3 beta-Aryltropane analogues wherein the 2-position was substituted with various diarylmethoxyalkyl groups were synthesized and evaluated for binding at the dopamine transporter (DAT), serotonin transporter (SERT), norepinephrine transporter (NET), and muscarinic (M(1)) receptors. The 2 beta-analogues 9a-i generally demonstrated high to moderate binding affinities (K(i) = 34-112 nM) at the DAT with good selectivity over SERT, NET, and M(1) receptors. Alternatively, the 2 alpha-isomers 10a-i were 10-fold less potent at the DAT with poor selectivity over SERT. These SAR studies provide further evidence for the varied binding requirements of structurally diverse tropane-based ligands and support future studies to elucidate DAT binding requirements in relation to cocaine-like behavioral endpoints. 相似文献