Medicinal chemistry (Shāriqah (United Arab Emirates))

Publisher: Bentham Science Publishers

Journal description

Current impact factor: 1.39

Impact Factor Rankings

2015 Impact Factor Available summer 2015
2013 / 2014 Impact Factor 1.387
2012 Impact Factor 1.373
2011 Impact Factor 1.496
2010 Impact Factor 1.603
2009 Impact Factor 1.642

Impact factor over time

Impact factor
Year

Additional details

5-year impact 0.00
Cited half-life 3.20
Immediacy index 0.27
Eigenfactor 0.00
Article influence 0.00
ISSN 1875-6638

Publisher details

Bentham Science Publishers

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    • 12 months embargo
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    • Author's pre-print on author's personal website, institutional repository and open access repository
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    • Non-Commercial
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    • Publisher's version/PDF cannot be used
  • Classification
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Publications in this journal

  • Nikita V Shtyrlin, Sergey V Sapozhnikov, Sergey A Koshkin, Alfiya G Iksanova, Arthur H Sabirov, Airat R Kayumov, Aliya A Nureeva, Marina I Zeldi, Yurii G Shtyrlin
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    ABSTRACT: A series of 26 quaternary ammonium pyridoxine derivatives were synthesized and their cytotoxicity and antibacterial activity against clinically relevant bacterial strains were tested in vitro. The antibacterial activity of mono-ammonium salts increased with the rise of the lipophilicity and compound 3,3,5-trimethyl-8,8-dioctyl-1,7,8,9-tetrahydro-[1,3]dioxino[5,4-d]pyrrolo[3,4-b]pyridin-8-ium chloride (2d) reaches a maximum of that among them. Bis-ammonium salt of pyridoxine 4 with two dimethyloctylamine groups also demonstrated high antibacterial activity despite of lower lipophilicity. The results of MTT assay indicated that HEK 293 cells were more sensitive than HSF to quaternary ammonium pyridoxine derivatives. Compounds 2d and 4 did not induce the damage of the DNA and might be of interest in the development of new antimicrobials.
    Medicinal chemistry (Shāriqah (United Arab Emirates)) 05/2015;
  • X U Gang, L U Hua, Jiang Zhitao, Shuying Zhang, Shaohua Gou
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    ABSTRACT: A series of palladium complexes with 2,2'-bipyridine and 1-(substituted benzyl) azetidine-3, 3-dicarboxylates as ligands were synthesized and characterized by IR, 1H-NMR, ESI-MS spectra and elemental analysis. The in vitro cytotoxicity assays were carried out against A549, HCT-116, HepG-2 and SGC7901 cancer cell lines. The result showed that most of the complexes possessed moderate antiproliferative activity against HCT-116, HepG-2 and SGC7901 cell lines. Complex 12 (with 2,2'-bipyridine and 1-(3-methoxylbenzyl)azetidine-3,3-dicarboxylate as ligand) was the most potent antitumor agent among all thirteen complexes, which showed comparable or better cytotoxicity against all four tested cancer cell lines than carboplatin. The interaction between complex 12 and pET22b plasmid DNA was investigated by agarose gel electrophoresis, and the result of the study showed that complex 12 had no obvious interaction with the plasmid DNA.
    Medicinal chemistry (Shāriqah (United Arab Emirates)) 05/2015;
  • Caroline Descôteaux, Kevin Brasseur, Valérie Leblanc, Eric Asselin, Gervais Bérubé
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    ABSTRACT: The search for new specific chemotherapeutic drugs designed to minimize the toxic side effects resulting from chemotherapy is still a subject of intense research. The objective of the current study was to design a non-steroidal-platinum(II) derivative that would target the estrogen receptor alpha (ERa) without triggering estrogenic cell proliferation. For this purpose, the amino acid L-tyrosine was modified and attached to a cisplatin analog. Hence, the L-tyrosine portion of the molecule could possibly act as a transporter to target the ERa protein and, by doing so concentrate the cytotoxic moiety to hormone-dependent breast cancer cells. Herein, we describe three different alternative methodologies that were used to make these new anticancer molecules. The L-tyrosine-Pt(II) hybrid 5b was made in four steps with 36% overall yield by the first method, in six steps with 11% overall yield by the second method and, in four steps with 23% overall yield by the third method. Preliminary biological activity on breast cancer cell lines indicated that the final hybrids (5a and 5b) were unfortunately inactive but their platinum(II) precursors (14a and 14b) showed activity similar to that of cisplatin.
    Medicinal chemistry (Shāriqah (United Arab Emirates)) 05/2015;
  • Feng Wang, D I Fan, Jun Qian, Zhe Zhang, Jianhua Zhu, Jian Chen
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    ABSTRACT: Diagnosis of tumour hypoxia is an important part aspect in determining the course of tumour therapy. In this study, we developed a novel imaging agent, 99mTc-ethylenedicysteine-bis-misonidazole (99mTc-EC-MISO), for diagnosing tumour hypoxia. We used 2-nitroimidazole as a reactant to synthesize the amino derivative of misonidazole (MISO) in the first step and then conjugated the di-amino derivative of MISO to the chelating agent ethylenedicysteine (EC) for labelling 99mTc in the second step. 99mTc-pertechnetate (99mTcO4-) was reduced by tin chloride (SnCl2) for radiolabeling. The radiochemical purity was up to 94%. Tissue biodistribution and SPECT/CT imaging studies were conducted on subcutaneous gliomal tumour-bearing mice. The tumour-to-muscle ratio in the 99mTc-EC-MISO group increased with time, up to 4.6%ID/g at 4 h after injection. SPECT/CT imaging confirmed that the tumours could be visualized clearly with 99mTc-EC-MISO at 2 h. By introducing a second 2-nitroimidazole redox centre, an apparent hypoxic accumulation of this novel 99mTc-labeled imaging agent in the tumour was observed.
    Medicinal chemistry (Shāriqah (United Arab Emirates)) 05/2015;
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    ABSTRACT: The reaction of various substituted 2, 4-dichloroquinolines with ethyl 4-(3-hydroxyphenyl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate has been carried out in presence of K2CO3 as a mild and efficient base at controlled temperature leading to novel 2-chloroquinoline based polyhydroquinoline with high regioselectivity. All the synthesized compounds were characterized using IR, NMR, Mass spectral data and then subjected to the in-silico analysis against P. falciparum lactate dehydrogenase.
    Medicinal chemistry (Shāriqah (United Arab Emirates)) 04/2015;
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    ABSTRACT: The diisopentenyloxy quinolobactin derivative 3-methylbut-2-enyl-4-methoxy-8-[(3-methylbut-2-enyl)oxy]quinoline-2-carboxylate, also named as Ppc-1, has been initially isolated from the fruiting bodies of the cellular slime mold Polysphondylium pseudo-candidum. Given that few data are available in the literature concerning the biological properties of this compound, this study was undertaken to evaluate its antibacterial and anti-inflammatory properties. Ppc-1 exerted antibacterial activity on the Gram negative periodontopathogen Porphyromonas gingivalis, while it had no such effect on the other bacterial species tested. The antibacterial activity of Ppc-1 appeared to result from its ability to permeate the cell membrane. Using the U937-3xκB-LUC human monocytic cell line, Ppc-1 was found to dose-dependently inhibit the lipopolysaccharide-induced NF-κB activation, a signalling pathway that has been associated with inflammatory mediator secretion. In conclusion, Ppc-1, by exhibiting a dual mode of action including antibacterial and anti-inflammatory activities, may represent a promising targeted therapeutic agent for periodontal diseases.
    Medicinal chemistry (Shāriqah (United Arab Emirates)) 04/2015;
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    ABSTRACT: Every year, cancer takes the life of millions of people. Conventional treatments have produced unsatisfactory results for some types of cancer, and the side effects are extensive, leading to a shift in the focus of treatment towards alternative medicines. Indeed, medicinal plants have long been investigated by scientists for their anti-cancer properties. Some phytochemicals that are important active constituents of plants, including catechins, ursolic acid, silymarin, glycyrrhizin, ellagic acid, gallic acid and various types of flavonoids, have shown promise in future cancer management. The current review covers various aspects of cancer treatment based on medicinal plants at molecular level and sheds light on their structures and modes of action.
    Medicinal chemistry (Shāriqah (United Arab Emirates)) 04/2015;
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    ABSTRACT: Psychotic disorders are complex and caused by interplay of genetic and environmental factors. Influenza is a common infectious disease in humans, and it has been suggested that maternal influenza is an estimated risk factor for psychotic disorders, especially for schizophrenia. In view of conflicting results of this association in literature, we performed the strict meta-analysis to examine whether maternal influenza is a risk factor for psychosis in the children. Four ecological studies and three birth cohort studies were included in our meta-analysis. It has been observed that the Risk Ratio (RR) of maternal influenza on psychosis is 1.062 (95% Confidence Interval (CI) = 1.004-1.123) for the analysis of ecological studies and the RR is 1.564(95%CI=1.051-2.324) for the analysis of birth cohort studies. Furthermore, a survey of pregnant women and fetus' health in Nanjing of China indicated that only 1.5% of women received the influenza vaccine before pregnancy, 0.4% received it during pregnancy, and 5.1% were willing to receive the influenza vaccine if necessary. These results showed that gestational influenza could increase mental disorders risks in adult offspring besides its established harms for gravidas. Results suggest it might be effective to increase attention to gravidas to protect them from influenza infection through encouragement of vaccinations.
    Medicinal chemistry (Shāriqah (United Arab Emirates)) 04/2015;
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    ABSTRACT: A facile and atom-economical boric acid catalyzed direct amidation without any coupling agents for the preparation of Suberoylanilide Hydroxamic Acid (SAHA) and SAHA-based inhibitors targeting anti-proliferation of cancer cells is described. It is applicable to the preparation of SAHA-based inhibitors having an unprotected hydroxyl group in the phenyl ring without the need of the protection. The in-vitro assays data indicate that the nature and the position of the substituents (activating and/or deactivating) in the capping group (phenyl ring) of SAHA-based inhibitors synthesized in this study have a vital impact on the potency of anti-proliferative activity against cancer cells. With low toxicity toward the normal cells, a number of synthesized SAHA-based inhibitors with two substituents in the phenyl ring possess higher anti-proliferative activity than SAHA and Cisplatin toward six studied cancer cell lines: A375 human skin cancer cells, A549 human lung cancer cells, MGC80-3 human gastric cancer cells, H460 human lung cancer cells, H1299 human lung cancer cells, and HepG2 human liver cancer cells. Cisplatin is a common chemotherapeutic drug with high cytotoxicity for a variety of cancer treatments. The inhibitors provided in this study might signify future therapeutic drugs for cancer treatment.
    Medicinal chemistry (Shāriqah (United Arab Emirates)) 04/2015;
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    ABSTRACT: Oxime K203 seems to be the most promising oxime in case of reactivation of tabun-inhibited acetylcholinesterase (AChE). Although it was originally developed for treatment of tabun intoxications, it is able to reactivate cholinesterases inhibited by other nerve agents. This study is aimed at the evaluation of its potency in vitro against other nerve agents. For this purpose, sarin, tabun, cyclosarin, soman, VX, Russian VX and DFP were selected as members of the nerve agent family to check its universality. At high concentrations (10-3 M), oxime K203 reached promising reactivation activity. At low concentrations, relevant for human use (10-5 M), promising reactivation potency was obtained only with tabun. In conclusion, oxime K203 reactivates other nerve agents-inhibited cholinesterases, however its broad-spectrum reactivation is limited at high, for human not attainable, concentrations only.
    Medicinal chemistry (Shāriqah (United Arab Emirates)) 04/2015;
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    ABSTRACT: Acid hydrazides are vital chemical entities due to their biological activities. On complexation to certain metal ions their biological activity is known to be positively enhanced. The present work describes the synthesis of Cr(III)-hydrazide complexes, their structural, spectroscopic and antioxidant properties to reveal the biochemistry and chemistry of Cr(III)-hydrazide complexes. Physical (magnetic moment, conductivity measurements), analytical (C, H, N and Cr analysis) and spectral (EI-Mass, FT-IR) techniques are used for characterization of synthetic compounds. All Cr(III)-hydrazide complexes showing octahedral geometry with general formula [Cr(L)2(H2O)2]Cl3. In Cr(III) complexes, the hydrazide ligands are coordinated in bidentate fashion exhibiting carbonyl oxygen and terminal amino nitrogen as donor atom. All Cr(III)-hydrazide complexes were further screened for in vitro diphenyl dipicryl hydrazine (DPPH), superoxide dismutase and nitric oxide radical scavenging activities. This study has revealed that most of the Cr(III)-hydrazide complexes were more potent scavengers than their parent hydrazides. This study demonstrates an interesting structure-activity relationship (SAR) which is presented in this paper.
    Medicinal chemistry (Shāriqah (United Arab Emirates)) 03/2015;
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    ABSTRACT: Mitochondrial enzymes monoamine oxidases were thought to be an emerging and useful therapeutic target for neurodegenerative disorders. Monoamine oxidases have two isoforms, A and B. MAO-A is related with metabolism of amine neurotransmitters in the brain whereas MAO-B is concerned with aging related neurodegenerative disorders. Therefore the identification, characterization and discovery of potent MAO-A and B inhibitors is very crucial in research. A series of quinolyl-thienyl chalcones were tested against MAO-A and B. Among the screened compounds, most of them revealed potent MAO-A and B inhibition. Compound 5i presented most potent MAO-A inhibition having IC50 values 0.047 µM, while 4l showed excellent inhibitory potency against MAO-B among all the tested compound having IC50 values 0.063 µM. Molecular modelling studies were performed against human MAO-A and MAO-B for the explanation of binding site interactions.
    Medicinal chemistry (Shāriqah (United Arab Emirates)) 01/2015; DOI:10.2174/1573406410666141226131252
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    ABSTRACT: A series of piperidyl-thienyl & 2-pyrazoline derivatives of quinolyl-thienyl chalcones were tested to observe the structural characteristics for the monoamine oxidase inhibitory (MAO) activity. In both these series, a diverse range of substituted thiophenes are used which enable us the structure activity relationship and these compounds showed enhanced inhibition against MAO-A & B as compared to reference compounds. Compound 1c presented most potent MAO-A inhibition having IC50 values 0.062 µM, while 1j showed excellent inhibitory potency against MAO-B among all the tested compound having IC50 values 0.088 µM. The present investigation demonstrated that among piperidyl-thienyl chalcones, almost all the compounds exhibit significant MAO-A inhibition, thus may have antidepressant activity. Whereas among the 2-pyrazoline derivatives of chalcones, many compounds revealed MAO-B inhibition and hence can be applied in the control of senile dementia. Molecular docking studies were carried out against human MAO-A and MAO-B to rationalize important binding site interactions.
    Medicinal chemistry (Shāriqah (United Arab Emirates)) 01/2015; DOI:10.2174/1573406410666141229101130
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    ABSTRACT: Alzheimer’s disease (AD) is a type of neurodegenerative disorder which is responsible for many cognitive dysfunctions. According to a most accepted cholinergic hypothesis, cholinesterases (AChE and BChE) have a major role in AD symptoms. The use of small molecules as inhibitors is one of the most striking strategy to control AD. In the present work, a series of N-phenylthiazol-2-amine derivatives was screened against acetylcholinesterase (AChE) from Electrophorus electricus and butyrylcholinesterase (BChE) from horse serum by using Ellman’s method, taking neostigmine and donepezil as reference drugs. Some of the assayed compounds proved to be potent inhibitors for AChE and BChE activity. N-(2,3-dimethylphenyl)thiazol-2-amine 3j was found to be the most active inhibitor among the series with IC50 value of 0.009±0.002μM and 0.646±0.012 against AChE and BChE respectively. Molecular docking studies were carried out in order to better understand the ligand binding site interactions
    Medicinal chemistry (Shāriqah (United Arab Emirates)) 01/2015; DOI:10.2174/1573406411666141230104536
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    ABSTRACT: A series of 36 novel substituted quinazolinone derivatives were synthesized and evaluated for their antiinflammatory activity by carrageenan induced paw inflammation model. The ability of these compounds to inhibit cyclooxygenase (COX-1 and 2) enzyme has been determined in-vitro; the results indicated that quinazolinone derivatives were selective towards COX-2 rather than COX-1. Among the quinazolinone derivatives tested, compound 32 showed better inhibition against COX-2 when compared with Celecoxib. Pharmacophore modeling and 3D QSAR studies were performed in order to elucidate structural insights for the anti-inflammatory activity.
    Medicinal chemistry (Shāriqah (United Arab Emirates)) 10/2014; 10(7):711-723. DOI:10.2174/1573406409666131128142843
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    ABSTRACT: Ever growing resistance by the pathogenic bacteria against the prevalent antibiotics has forced the researchers to look for new methods and techniques to design effective antimicrobial agents. In the present study a new tetracycline-based antimicrobial polymer (AMP) was synthesized via acryloylation method using lipase-catalyzed esterification of tetracycline with methacrylic acid (MAAc). The aforesaid polymer was transformed into nanoparticles by an emulsion method. These polymers were characterized by various techniques, i.e., FTIR, NMR, XRD, SEM, and EDAX. The antibacterial activity of the AMPs was studied against two bacteria P. aeruginosa [resistant (-)] and S. aureus [susceptible (+)]. The synthesized AMP was observed to be more potent and efficient antimicrobial agent than the precursor tetracycline.
    Medicinal chemistry (Shāriqah (United Arab Emirates)) 05/2014; DOI:10.2174/1573406410666140507094435
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    ABSTRACT: A series of twelve analogs carrying fluoro, chloro, bromo and iodo halogens on the ortho, meta and para positions of a benzoyloxytropane skeleton were synthesized by a simple acylation of 8-methyl-8-aza-bicyclo[3.2.1]octan-3α-ol by halogenobenzoyl chlorides. The compounds were evaluated in vitro against Plasmodium falciparum (P. f.), Trypanosoma brucei brucei (T. b. b.), Trypanosoma cruzi (T. c.) and Leishmania infantum (L. i.). This study shows that the presence of a halogenated atom and its position on the aromatic ring are important for in vitro activity. Compounds 4 (IC50 = 3.6 µM), 8 (IC50 = 6.7 µM), 5 (IC50 = 8.1 µM) and 7 (IC50 = 9.5 µM) were found the most active against P. f., whereas compounds 12 (IC50 = 5.1 µM), 11 (IC50 = 5.6 µM) and 9 (IC50 = 5.8 µM) exhibited the most pronounced activity against T. b. b. This series of compounds can be considered as non-toxic to the human cell line MRC-5.
    Medicinal chemistry (Shāriqah (United Arab Emirates)) 05/2014;
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    ABSTRACT: Valproic acid (VPA) is considered first-line treatment for primarily generalized idiopathic seizures such as absence, generalized tonic-clonic and myoclonic seizures. Among major antiepileptic drugs, VPA is also considered effective in childhood epilepsies and infantile spasms. Due to its broad activity, it acts as a mood stabilizer in bipolar disorder and it is useful in migraine prophylaxis. Despite its long-standing usage, severe reactions to VPA, such as liver toxicity and teratogenicity, are reported. To circumvent side effects due to structural characteristics of VPA, a new VPA-aminoacid conjugate, the N-valproyl-L-Phenylalanine, has been synthesized in good yield and characterized by FT-IR, MS, 13C and 1H- NMR analyses. The Log DpH7.4 (0.19) indicate that this new molecule potentially is able to cross biological membranes. The resistence to chemical and enzymatic hydrolysis of N-valproyl-L-Phenylalanine were also assessed. All trials suggested that the compound at the pH conditions of the entire gastro-intestinal tract remained unmodified. Moreover, the novel compound did not undergo enzymatic cleavage both in plasma and in cerebral medium up to 24 h. Toxicity assay on primary cultures of astrocytes indicated that synthetized conjugate is less toxic than both free VPA and L-Phenylalanine. In this paper, the anticonvulsant activity of the new compound against epileptic burst discharges evoked in vitro in rat hippocampal slices was also evaluated. These preliminary results underlines that N-valproyl-L-Phenylalanine could represent a good candidate to further investigation as new potential antiepileptic agent.
    Medicinal chemistry (Shāriqah (United Arab Emirates)) 05/2014; DOI:10.2174/1573406410666140507094954
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    ABSTRACT: Background: Cholesterol is essential for the growth and maintenance of mammalian cells. However, elevated level of serum cholesterol is among the associated risk factors for the coronary heart disease. Cholesterol is derived from two different sources of endogenous synthesis and diet. Statins can reduce endogenous sterol synthesis by inhibit HMG-CoA reductase, whereas cholesterol absorption inhibitors, such as ezetimibe, can block cholesterol uptake from dietary sources by block Niemann-Pick C1-like 1 (NPC1L1). Objective: The present review focus on the main research progress of cholesterol absorption inhibitors, the structure of NPC1L1 and discovery of novel chemical entities by virtual screening. Conclusion: Studies on the structure-activity relationship reveal that azetidinone is important to keep activity in azetidinone derivatives and the novel heterocyclic compounds with replacement of β-lactam scaffold by oxazolidinone also shows similar activity as ezetimibe. Virtual screening in data bases as computer-aided molecular design tools to propose novel cholesterol absorption inhibitors are kind of complement to design and synthesize structurally novel compounds.
    Medicinal chemistry (Shāriqah (United Arab Emirates)) 04/2014; DOI:10.2174/1573406410666140428152436
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    ABSTRACT: Estrogen receptors (ERs) are members of a superfamily of ligand-modulated nuclear receptors, which have been associated with an increased risk of cardiovascular diseases and breast cancer. Based on molecular docking studies, 1,4-dihydrothieno[3',2':5,6]thiopyrano[4,3-c]pyrazole-3-carboxamide derivatives as estrogen receptor inhibitors with a new scaffold , have been synthesized and tested for the antitumor activity on the ER expressing (ER dependent) human MCF-7 breast cancer cell line. According to the biological activity evaluation, compound 6a demonstrated the most potent antiproliferative activity (relative inhibitory rate: 100%). Several of these compounds exhibited moderate antitumor activity and worthy of further modification to obtain more potent anticancer candidate drugs.
    Medicinal chemistry (Shāriqah (United Arab Emirates)) 04/2014;