Journal ArticleDOI
Synthesis and Anti-HIV-1 Activity of Novel 2,3-Dihydro-7H-thiazolo[3,2-a]pyrimidin-7-ones
Reads0
Chats0
TLDR
Appropriately substituted 2,3-dihydro-7H-thiazolo[3,2-a]pyrimidin-7-ones 9-12 and 18 were considered as annulated analogues of HEPT (1-[(2-hydroxyethoxyethoxy)methyl]-6-(phenylthio)-thymine), and some of these compounds were also found active against HIV-1.Abstract:
Appropriately substituted 2,3-dihydro-7H-thiazolo[3,2-a]pyrimidin-7-ones 9−12 and 18 were considered as annulated analogues of HEPT (1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine), and some of these compounds were also found active against HIV-1, the most active one being 2,3-dihydro-5-[(3,5-dimethylphenyl)methyl]-3-ethoxy-6-ethyl-7H-thiazolo[3,2-a]pyrimidin-7-one (10b). S-Alkylation of 5-alkyl-6-(arylmethyl)-2-thiouracils 1−4 was performed with 2-bromoacetaldehyde acetals to furnish the S-[bis(alkoxy)ethyl] derivatives 5−8 and with allyl bromide to furnish S-allyl derivatives 17. The target compounds 9−12 were obtained by an N1 regioselective intramolecular cyclization reaction of silylated 5−8 using trimethylsilyl trifluoromethanesulfonate (TMS triflate) as the catalyst. Treatment of the S-allyl derivatives 17 with bromine in dry methylene chloride afforded the 3-(bromomethyl) derivatives 18.read more
Citations
More filters
Journal ArticleDOI
Non-nucleoside reverse transcriptase inhibitors: the NNRTI boom.
Ole S. Pedersen,Erik B. Pedersen +1 more
TL;DR: This review discusses the properties of the FDA-approved NNRTI drugs and focuses on the recent efforts being made to produce second generation inhibitors that circumvent this resistance problem.
Journal ArticleDOI
Analgesic, anticonvulsant and anti-inflammatory activities of some synthesized benzodiazipine, triazolopyrimidine and bis-imide derivatives.
TL;DR: A series of diazipine, pyrimidine, fused triazolopyrimidine and imide derivatives were newly synthesized using 4-phenyl-but-3-en-2-one 1 as a starting material and compounds 2 and 9 are intermediates.
Journal ArticleDOI
One pot efficient diversity oriented synthesis of polyfunctional styryl thiazolopyrimidines and their bio-evaluation as antimalarial and anti-HIV agents.
Seerat Fatima,Anindra Sharma,Reshu Saxena,R.P. Tripathi,Sanjeev K. Shukla,Swaroop Kumar Pandey,Renu Tripathi,Rama P. Tripathi +7 more
TL;DR: An efficient one pot synthesis of a series of pluripotent (E)-1-(3-methyl-5-aryl-7-styryl-5H-thiazolo[3,2-a]pyrimidin-6-yl)-3-arylprop-2-en-1-ones is reported, which displayed potent antimalarial activity with IC(50)<2 μg/mL.
Journal ArticleDOI
Novel Thiourea Compounds as Dual-Function Microbicides
TL;DR: It is concluded that as potent anti-HIV agents with SIA and reduced cytotoxicity when compared with N-9, the phenyl-substituted and cyclohexenyl-based thiourea derivatives show unique clinical potential to become the active ingredients of a vaginal contraceptive for women who are at high risk for acquiring HIV by heterosexual vaginal transmission.
Journal ArticleDOI
Synthesis, characterization and biological evaluation of novel 6-ferrocenyl-4-aryl-2-substituted pyrimidine derivatives.
TL;DR: A new series of 6-ferrocenyl-4-aryl-2-substituted pyrimidines were synthesized and evaluated for in vitro antiamoebic activity against HM1:IMSS strain of Entamoeba histolytica and showed that all compounds were non-toxic.
References
More filters
Journal ArticleDOI
Rapid colorimetric assay for cellular growth and survival: Application to proliferation and cytotoxicity assays
TL;DR: A tetrazolium salt has been used to develop a quantitative colorimetric assay for mammalian cell survival and proliferation and is used to measure proliferative lymphokines, mitogen stimulations and complement-mediated lysis.
Journal ArticleDOI
Frequent detection and isolation of cytopathic retroviruses (HTLV-III) from patients with AIDS and at risk for AIDS
Robert C. Gallo,Syed Zaki Salahuddin,Mikulas Popovic,Gene M. Shearer,Mark H. Kaplan,Barton F. Haynes,Thomas J. Palker,Robert R. Redfield,James M. Oleske,Bijan Safai,Gilbert C. White,Paul Foster,Phillip D. Markham +12 more
TL;DR: Peripheral blood lymphocytes from patients with the acquired immunodeficiency syndrome (AIDS) or with signs or symptoms that frequently precede AIDS (pre-AIDS) were grown in vitro with added T-cell growth factor and assayed for the expression and release of human T-lymphotropic retroviruses (HTLV).
Journal ArticleDOI
Detection, Isolation, and Continuous Production of Cytopathic Retroviruses (HTLV-III) from Patients with AIDS and Pre-AIDS
TL;DR: A cell system was developed for the reproducible detection of human T-lymphotropic retroviruses (HTLV family) from patients with the acquired immunodeficiency syndrome (AIDS) or with signs or symptoms that frequently precede AIDS (pre-AIDS), and it provides large amounts of virus for detailed molecular and immunological analyses.
Journal ArticleDOI
Infection of HTLV-III/LAV in HTLV-I-carrying cells MT-2 and MT-4 and application in a plaque assay
TL;DR: Activities of HTLV-III were neutralized by the human antibodies against the virus when immunofluorescence and plaque assays were used, and the same results were obtained with the lymphadenopathy-associated virus (LAV1).
Journal ArticleDOI
Molecular targets for AIDS therapy
TL;DR: In the future, non-nucleoside-type drugs will likely become more important in the experimental therapy of AIDS, and antiretroviral therapy will exert major effects against the morbidity and mortality caused by HIV.