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anti-HIV Activity (anti-hiv + activity)

Distribution by Scientific Domains

Chemistry	63%
Polymers and Materials Science	22%
Medical Sciences	13%

Selected Abstracts

Amino Acid Derivatives, Part 4: Synthesis and Anti-HIV Activity of New Naphthalene Derivatives

ARCHIV DER PHARMAZIE, Issue 7 2010
Nawar S. Hamad
Abstract A new series of 2-(naphthalen-2-yloxy)- N -[(aryl-5-thioxo-4,5-dihydro-1H -1,2,4-triazol-3-yl)methyl] acetamides 5a,f was synthesized from naphthalene-derived glycine derivative 2 via the hydrazinoacetamide analogs 4a,f. Alternatively, treatment of 4a with H2SO4 afforded 2-(naphthalen-2-yloxy)- N -((5-(phenylamino)-1,3,4-thiadiazol-2-yl)methyl) acetamide 6a. Alkylation or sulphonylation of 5a afforded the S-alkylated derivatives 7 and 8, respectively. Interestingly, treatment of 3 with methoxide ion gave the triazine derivative 9. The synthesized compounds have been screened for their inhibitory activity against HIV-1 and HIV-2 in MT-4 cells. However, 7 was found to be the potent inhibitor in vitro for the replication of HIV-1 (EC50 = 0.20 ,g/mL), suggesting a new lead in the development of an antiviral agent. [source]

Dendritic Catanionic Assemblies: In vitro Anti-HIV Activity of Phosphorus-Containing Dendrimers Bearing Gal,1cer Analogues

CHEMBIOCHEM, Issue 12 2005
Muriel Blanzat Dr.
Abstract Two series of water-soluble dendritic catanionic assemblies, acting as multisite analogues of galactosylceramide (Gal,1cer), have been prepared with the goal of blocking HIV infection prior to the entry of the virus into human cells. Trifunctional and hexafunctional cinnamic acid-terminated dendrimers have been synthesized from phosphorus-containing dendrimers bearing aldehyde end groups. A classical acid,base reaction performed in water between acid-terminated dendrimers and stoichiometric amounts of N -hexadecylamino-1-deoxylactitol (3) provided the expected catanionic assemblies. Antiviral assays on these supramolecular entities confirmed the crucial roles both of multivalency effects and of lipophilicity on the biological activity of Gal,1cer analogues. Moreover, correlation between in vitro tests and molecular modeling highlights the specific influence of the assembly shape on the anti-HIV efficiency, with the tri- and hexafunctional cored dendrimers, both decorated with 12 sugar moieties, exhibiting IC50 values of 1.1 and 0.12 ,M, respectively. [source]

ChemInform Abstract: Anti-HIV Activity of Novel Phosphonate Derivatives of AZT, d4T, and ddA

CHEMINFORM, Issue 48 2001
A. G. Pokrovsky
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]

Synthesis and anti-HIV activity of sulfated astragalus polysaccharide

POLYMERS FOR ADVANCED TECHNOLOGIES, Issue 7 2003
Guo-Guang Liu
Abstract Sulfated astragalus polysaccharide (sulfated astragalan, SA) was prepared by chemical modification of astragalus polysaccharide abstracted from an astragalus menbranceus used as a Mongolia herbal medicine. Anti-HIV activity of SA was assayed in vitro and the results indicated that the SA showing high anti-HIV activity and lower cytotoxity. Sulfation of astragalan was carried out by using sulfur trioxide-pyridine complex in a mixture of dimethylsulfoxide (DMSO) to give sulfated astragalan with degree of substitution (DS) of 1.14,1.20 and a number average molecular weight (Mn) of 1.27,1.46,×,104. Copyright © 2003 John Wiley & Sons, Ltd. [source]

ORIGINAL ARTICLE: CCL20/MIP3, is a Novel Anti-HIV-1 Molecule of the Human Female Reproductive Tract

AMERICAN JOURNAL OF REPRODUCTIVE IMMUNOLOGY, Issue 1 2009
Mimi Ghosh
Problem, CCL20/MIP3, is a chemokine for immature dendritic cells as well as an antibacterial against gram-positive and gram-negative bacteria. The role of CCL20/MIP3, as an antiviral is unknown. In this study, we have examined the production of CCL20/MIP3, by epithelial cells from the upper female reproductive tract as well as its activity as an antiviral molecule. Method of study, Primary uterine and Fallopian tube epithelial cells were treated with Poly(I:C) and CCL20/MIP3, mRNA and protein was measured by Realtime RT-PCR and ELISA assays. Anti-HIV activity was determined using an indicator cell line TZM-bl and quantified by using a luminometer. Results, Primary uterine and Fallopian tube epithelial cells produce CCL20/MIP3, constitutively and the production is enhanced following stimulation with viral double-stranded RNA mimic Poly(I:C). Recombinant CCL20/MIP3, was able to inhibit both T-cell-tropic X4/IIIB and macrophage-tropic R5/BaL HIV-1 when virus was directly incubated with CCL20/MIP3, but not when CCL20/MIP3, was added to cells either prior to infection or post-infection. This suggests that the mechanism of inhibition is likely to be a direct interaction between HIV-1 and CCL20/MIP3,. Conclusion, This study demonstrates that CCL20/MIP3, is an important endogenous anti-HIV-1 microbicide of the female reproductive tract. [source]

ChemInform Abstract: Synthesis and anti-HIV Activity of S-Dihydro(alkyloxy)benzyloxypyrimidine Derivatives.

CHEMINFORM, Issue 44 2008
Zhi-Kun Rao
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]

Synthesis and anti-HIV Activity of Substituted 1,2,4-Triazolo-thiophene Derivatives.

CHEMINFORM, Issue 38 2007
Yaseen A. Al-Soud
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source]

Microwave-Assisted Synthesis and anti-HIV Activity of New Benzenesulfonamides Bearing 2,5-Disubstituted-1,3,4-oxadiazole Moiety.

CHEMINFORM, Issue 36 2007
Muhammad Zareef
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source]

Synthesis and anti-HIV Activity of 2,3-Diaryl-1,3-thiazolidin-4-ones.

CHEMINFORM, Issue 22 2003
Angela Rao
Abstract For Abstract see ChemInform Abstract in Full Text. [source]

Molecular surface electrostatic potentials in relation to noncovalent interactions in biological systems

INTERNATIONAL JOURNAL OF QUANTUM CHEMISTRY, Issue 6 2001
Peter Politzer
Abstract Noncovalent interactions are predominantly electrostatic in nature. It follows that an effective tool for their investigation and elucidation is the electrostatic potential on the molecular surface. We have shown that a variety of condensed phase macroscopic properties can be expressed quantitatively in terms of certain site-specific and global statistical quantities that characterize the overall pattern of the surface potential. We are now extending this approach to interactions in biological systems. Several applications will be discussed, including initial qualitative studies of dioxins, a series of anticonvulsants and some tetracyclines, the nucleotide bases, and a recent quantitative treatment of the anti-HIV activities of three groups of reverse transcriptase inhibitors. © 2001 John Wiley & Sons, Inc. Int J Quantum Chem, 2001 [source]

Syntheses of cyclodextrin,3,-azido-3,-deoxythymidine conjugates and their sulfates with improved anti-HIV activities

JOURNAL OF POLYMER SCIENCE (IN TWO SECTIONS), Issue 1 2006
Ildoo Chung
Abstract New anti-HIV agents, cyclodextrin,3,-azido-3,-deoxythymidine (CD,AZT) conjugates, were synthesized and characterized. A succinate diester spacer was used to covalently couple 3,-azido-3,-deoxythymidine (AZT) onto cyclodextrin. In addition, their sulfates were prepared by the reaction of CD,AZT conjugates and a sulfur trioxide/pyridine complex at 80 °C. The degree of AZT substitution of the synthesized conjugates and the sulfur contents of their sulfates were calculated from elemental analysis and ranged from 1.3 to 4.7 and from 8.4 to 12.1, respectively. These resulting sulfated conjugates were expected to have a synergistic effect against HIV because of the two anti-HIV active agents (sulfate group and AZT) by the inhibition of virus attachment to cells and that of reverse transcriptase. The in vitro antiviral activity of these conjugates was determined and used to evaluate the potential applications in anti-AIDS drugs. The in vitro anti-HIV activities indicated that the synthesized conjugates and their sulfates against HIV-1 and HIV-2 strains were much better inhibitors than AZT. © 2005 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 44: 295,303, 2006 [source]

Microwave-assisted synthesis and anti-HIV activity of new benzenesulfonamides bearing 2,5-disubstituted-1,3,4-oxadiazole moiety

HETEROATOM CHEMISTRY, Issue 4 2007
Muhammad Zareef
New benzenesulfonamides, most of which are chiral, incorporating 1,3,4-oxadiazole, and selected amino acid entities have been synthesized, using the microwave irradiation method. Most of the synthesized compounds were tested against HIV activity. © 2007 Wiley Periodicals, Inc. Heteroatom Chem 18:425,431, 2007; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/hc.20316 [source]

Synthesis and anti-HIV activity of new chiral 1,2,4-triazoles and 1,3,4-thiadiazoles

HETEROATOM CHEMISTRY, Issue 3 2007
Tashfeen Akhtar
5-substituted 4-(4-chlorophenyl)-4H-1,2,4-triazol-3-thiones 3 and 2-substituted 5-(4-chlorophenylamino)-1,3,4-thiadiazoles 4 were prepared from the intermediate thiosemicarbazides 2 under basic and acidic conditions, respectively. The thiosemicarbazides, in turn, were prepared by the reaction of hydrazides 1 with 4-chlorophenylisothiocyanate in MeOH. Some of the new synthesized compounds were assayed against HIV-1 and HIV-2 in MT-4 cells. All the compounds were inactive except 3f, which showed an EC50 value of 23.9 ,g/mL and 9.9 ,g/mL against HIV-1 and HIV-2 with a therapeutic index of 3 and 7, respectively. It means that compound 3f was cytotoxic to MT-4 cells at CC50 of 72.7 ,g/mL in both strains. © 2007 Wiley Periodicals, Inc. Heteroatom Chem 18:316,322, 2007; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/hc.20282 [source]

Computational modeling of tetrahydroimidazo-[4,5,1-jk][1,4]-benzodiazepinone derivatives: An atomistic drug design approach using Kier-Hall electrotopological state (E-state) indices

JOURNAL OF COMPUTATIONAL CHEMISTRY, Issue 11 2008
Nitin S. Sapre
Abstract Quantitative structure-activity relationships (QSAR), based on E-state indices have been developed for a series of tetrahydroimidazo-[4,5,1-jk]-benzodiazepinone derivatives against HIV-1 reverse transcriptase (HIV-1 RT). Statistical modeling using multiple linear regression technique in predicting the anti-HIV activity yielded a good correlation for the training set (R2 = 0.913, R = 0.897, Q2 = 0.849, MSE = 0.190, F -ratio = 59.97, PRESS = 18.05, SSE = 0.926, and p value = 0.00). Leave-one-out cross-validation also reaffirmed the predictions (R2 = 0.850, R = 0.824, Q2 = 0.849, MSE = 0.328, and PRESS = 18.05). The predictive ability of the training set was also cross-validated by a test set (R2 = 0.812, R = 0.799, Q2 = 0.765, MSE = 0.347, F -ratio = 64.69, PRESS = 7.37, SSE = 0.975, and p value = 0.00), which ascertained a satisfactory quality of fit. The results reflect the substitution pattern and suggest that the presence of a bulky and electropositive group in the five-member ring and electron withdrawing groups in the seven-member ring will have a positive impact on the antiviral activity of the derivatives. Bulky groups in the six-member ring do not show an activity-enhancing impact. Outlier analysis too reconfirms our findings. The E-state descriptors indicate their importance in quantifying the electronic characteristics of a molecule and thus can be used in chemical interpretation of electronic and steric factors affecting the biological activity of compounds. © 2008 Wiley Periodicals, Inc. J Comput Chem, 2008 [source]

Peptide T revisited: conformational mimicry of epitopes of anti-HIV proteins

JOURNAL OF PEPTIDE SCIENCE, Issue 4 2001
Delia Picone
Abstract Peptide T (ASTTTNYT), a fragment corresponding to residues 185,192 of gp120, the coat protein of HIV, is endowed with several biological properties in vitro, notably inhibition of the binding of both isolated gp120 and HIV-1 to the CD4 receptor, and chemotactic activity. Based on previous nuclear magnetic resonance (NMR) studies performed in our laboratory, which were consistent with a regular conformation of the C -terminal pentapeptide, and SAR studies showing that the C -terminal pentapeptide retains most of the biological properties, we designed eight hexapeptides containing in the central part either the TNYT or the TTNY sequence, and charged residues (D/E/R) at the two ends. Conformational analysis based on NMR and torsion angle dynamics showed that all peptides assume folded conformations, albeit with different geometries and stabilities. In particular, peptides carrying an acidic residue at the N -terminus and a basic residue at the C -terminus are characterized by stable helical structures and retain full chemotactic activity. The solution conformation of peptide ETNYTR displays strong structural similarity to the region 19,26 of both bovine pancreatic and bovine seminal ribonuclease, which are endowed with anti-HIV activity. Moreover, the frequent occurrence, in many viral proteins, of TNYT and TTNY, the two core sequences employed in the design of the hexapeptides studied in the present work, hints that the sequence of the C -terminal pentapeptide TTNYT is probably representative of a widespread viral recognition motif. Copyright © 2001 European Peptide Society and John Wiley & Sons, Ltd. [source]

Alcohol Suppresses IL-2,Induced CC Chemokine Production by Natural Killer Cells

ALCOHOLISM, Issue 9 2005
Ting Zhang
Background: Natural killer (NK) cells are a critical component of the host innate immune system. We investigated whether alcohol impairs NK cell function, particularly production of CC chemokines induced by interleukin (IL)-2, the natural ligands for CCR5 receptor. Methods: Primary NK cells and NK cell line (YTS) were cultured with or without alcohol (10 to 80 mM) for three hours. The culture supernatants were then harvested and used to treat human peripheral blood monocyte-derived macrophages and a HeLa cell line, which expresses CD4, CCR5, and CXCR4 receptors (MAGI cells). CC chemokine expression by YTS and primary NK cells treated with or without alcohol was analyzed with the real-time RT-PCR and ELISA. Ca2+i and Western blot assays were used to determine calcium-mediated intracellular signaling pathway and NF-,B p65 expression. HIV strains (Bal and UG024) were used to infect macrophages and MAGI cells. In addition, ADA (macrophage-tropic strain) and murine leukemia virus (MLV) envelope-pseudotyped HIV infection was carried out in macrophages. HIV infectivity was determined by HIV reverse transcriptase (RT) and ,-galactosidase activity assays. Results: Alcohol inhibited IL-2,induced CC chemokine (CCL3 and CCL4) expression by NK cells. Functional tests demonstrated that this reduced expression of CC chemokines was associated with diminished anti-HIV ability of NK cells. Alcohol also reduced the ability of NK cells to response to CCL3-mediated chemotaxis. Alcohol inhibited IL-2,induced NF-,B p65 protein expression and calcium mobilization by NK cells. Conclusions: Alcohol, through the inhibition of IL-2,induced NF-,B p65 protein expression and intracellular calcium mobilization, suppressed NK cell production of CC chemokines. This suppression of CC chemokine production was associated with diminished anti-HIV activity of NK cells. Thus, by inhibiting NK cell,mediated innate immunity against HIV, alcohol consumption may have a cofactor role in the immunopathogenesis of HIV disease. [source]

Synthesis and anti-HIV activity of sulfated astragalus polysaccharide

REVIEW ARTICLE: HIV Infection in the Female Genital Tract: Discrete Influence of the Local Mucosal Microenvironment

AMERICAN JOURNAL OF REPRODUCTIVE IMMUNOLOGY, Issue 6 2010
Charu Kaushic
Citation Kaushic C, Ferreira VH, Kafka JK, Nazli A. HIV infection in the female genital tract: discrete influence of the local mucosal microenvironment. Am J Reprod Immunol 2010 Women acquire HIV infections predominantly at the genital mucosa through heterosexual transmission. Therefore, the immune milieu at female genital surfaces is a critical determinant of HIV susceptibility. In this review, we recapitulate the evidence suggesting that several distinctive innate immune mechanisms in the female genital tract (FGT) serve to significantly deter or facilitate HIV-1 infection. Epithelial cells lining the FGT play a key role in forming a primary barrier to HIV entry. These cells express Toll-like receptors and other receptors that recognize and respond directly to pathogens, including HIV-1. In addition, innate biological factors produced by epithelial and other cells in the FGT have anti-HIV activity. Female sex hormones, co-infection with other pathogens and components in semen may also exacerbate or down-modulate HIV transmission. A combination of innate and adaptive immune factors and their interactions with the local microenvironment determine the outcome of HIV transmission. Improving our understanding of the female genital microenvironment will be useful in developing treatments that augment and sustain protective immune responses in the genital mucosa, such as microbicides and vaccines, and will provide greater insight into viral pathogenesis in the FGT. [source]

Synthesis and In-vitro Activity of 4,-Modified Analogues of ddA as Potent Anti-HIV Agents

ARCHIV DER PHARMAZIE, Issue 10 2009
Joon Hee Hong
Abstract This paper reports the synthesis of novel 4,-hydrophobic pocket deoxythreosyl C-nucleosides. The key threose-like intermediates 9 and 14 were constructed from acyclic ketone derivatives, respectively. The antiviral activities of the synthesized compounds against the HIV-1, HSV-1, HSV-2, and HCMV viruses were evaluated. The 9-deaza-adenine derivatives 10 and 20 showed good anti-HIV activity without exhibiting significant cytotoxicity. [source]

Synthesis and Studies of New 2-(Coumarin-4-yloxy)-4,6-(substituted)-s-Triazine Derivatives as Potential Anti-HIV Agents

ARCHIV DER PHARMAZIE, Issue 5 2009
Dharmesh H. Mahajan
Abstract Novel 2-(coumarin-4-yloxy)-4,6-(substituted)-s-triazine derivatives i. e., diaryltriazine (DATA) are reported as novel non-nucleoside reverse transcriptase inhibitors (NNRTIs), were synthesized and their activities against human immunodeficiency virus HIV-1 (III-B), HIV-2 (ROD), and the double RT mutant HIV-1 (K103N and Y181C) were assessed. Modifications at positions 4 and 6 of the coumarinyl-triazine scaffold generated interesting derivatives displaying good to moderate anti-HIV activity against selected HIV strains as compared to nevirapine and efavirenz. The synthesized compounds were characterized by FTIR, 1H-NMR, and mass spectral data together with elemental analysis. [source]