A number of new 5-[(naphthalen-5-yloxy)methyl]-1,3,4-oxadiazole derivatives, 2-5 and 8-11, were synthesized. The 2-{5-[(naphthalen-5-yloxy)methyl]-1,3,4-oxadiazol-2-ylthio}acetohydrazones 6a 6b synthesized by the reaction hydrazide 4 with corresponding monosaccharides. Cyclization sugar hydrazones acetic anhydride afforded substituted oxadiazoline derivatives 7a 7b. compounds evaluated for their antiviral activity against, human immunodeficiency virus (HIV-1) some these showed moderate to...

Certain pyridothienopyrimidine derivatives exhibit antiatheroscleorotic, antibacterial, antiviral, antidepressant, antidiabetic, antihypertensive, anticancer, antihistaminic, antiallergic, anti-inflammatory, spasmolytic, analgesic, and neurotropic activities. 4-Hydrazino-7,9-dimethylpyrido[3',2':4,5]thieno[3,2-d]pyrimidine (1) is a reported derivative. In the current study, has been reacted with different reagents to obtain 12 new derivatives. The newly synthesized five-membered heterocyclic...

We report the facile generation of chroman-4-one-derived thiosulfines 10 under mild conditions by our well-established nucleophilic “unzipping” corresponding acetyl α-chloroalkyl disulfides 9 which in turn can be prepared from α-chloro sulfenyl chlorides 8. Spontaneous partial loss sulfur 10, most probably disproportionation to 11 and 12, generates expectedly reactive β-oxo thioketones partly dimerize a precedented Diels−Alder fashion, give 1,3,4-oxadithiins 13, cycloadd form...

Six new examples of intercalating nucleic acids were synthesized in order to evaluate the dependence length linker between oligo and intercalator on thermal stability their corresponding duplexes triplexes.

A number of 1,3,4-oxadiazole, 3 - 9, and 1,2,4-triazole derivatives, 13 15, were synthesized starting form the acid hydrazide 1. The 1,3,4-thiadiazole derivative 12 was prepared from substituted phenylthiosemicarbazide 11 by treatment with sulfuric acid. aryl hydrazone derivatives 10a c reaction 1 corresponding ketones. thioalkyl 16a e akylation thiol different alkylating agents. newly compounds tested for their anti-HBV activity some these showed high antiviral

Synthesis of some 1,3,4-thia-, oxa-diazol and 1,2,4 triazole incorporated the biologically active pyrazolopyri-dine derivative. Molecular modeling docking compounds into AKR1C3 complexed with its bound inhibitor indomethacin using Molsoft ICM 3.4-8C program were performed in order to predict affinity orientation synthesized at site.

In this paper, we report on the design and synthesis of a novel series quinazoline-2,4(1H,3H)-dione derivatives as fluoroquinolone-like inhibitors bacterial gyrase DNA topoisomerase IV to identify develop antimicrobial agents prevent resistance problems. Their structures were confirmed using spectroscopic analyses (IR, NMR, EI-MS). The evaluated for their activities against Gram-positive Gram-negative strains Agar well diffusion method study compared them with standard drugs. Most compounds...

8,10-Dimethyl-3-(unsubstituted, methyl, ethyl, n-butyl, phenyl)-4-hydroxypyrido[2′,3′:3,4]pyrazolo[1,5-a]pyrimidin-2(1H)-ones and 3-(2-hydroxyethyl)-2,8,10-trimethylpyrido[2′,3′:3,4]pyrazolo[1,5-a]pyrimidin-4-ol were synthesized by cyclocondensation of 3-amine-4,6-dimethyl-1H-pyrazolo[3,4-b]pyridine with ethyl malonates α-acetyl-γ-butyrlolactone. Dichloro- diazido- derivatives obtained from the reaction pyridopyrazlopyrimidine POCl3 followed NaN3. The tetrahetrocyclic systems formed...

A series of 2‐oxo‐2,5‐dihydro‐1 H ‐chromeno[4,3‐ b ]pyridine derivatives were obtained by using a one‐pot three component reaction 2,2‐disubstituted chroman‐4‐one with aromatic aldehydes and 2‐cyanoacetamide in the presence sodium hydroxide under solvent‐free conditions. Heating chromenopyridine phosphoryl chloride gave corresponding chloro derivatives. The hydrazine hydrate afforded dihydrochromeno[4,3‐ ]pyrazolo[4,3‐ e ]pyridines Condensation dimethyl derivative compound...

This study reports the design, synthesis, and antibacterial evaluation of a library novel polyheterocyclic derivatives featuring unique fused pyrimidopyridopyrazole moiety. A cyclocondensation reaction between an amino-pyrazolopyridopyrimidine precursor malonates afforded series pyrimidopyridopyrazolopyrimidine derivatives. Further diversification was achieved through nucleophilic cyclocondensation, yielding collection complex systems encompassing various ring structures. All synthesized...

Abstract 6‐(2‐Phenylethyl) and 6‐cyclohexyl 5‐cyanouracils ( 1a,b ) were synthesized reacted with chloromethyl ethyl ether, benzyl methyl sulfide (2‐acetoxyethoxy)methyl bromide. New uracil analogues of S )‐DHPA by reaction compounds (( )‐2,2‐dimethyl‐1,3‐dioxolane‐4‐yl) alkyl p ‐toluenesulfonate.

A series of substituted 1,3,4‐oxadiazole, 1,2,4‐triazole, and 1,3,4‐thiadiazole derivatives the 3‐carboethoxy‐1,4‐dihydro‐4‐oxoquinoline have been synthesized through reaction key intermediate thiosemicarbazide with different reagents. N ′‐Arylidene‐4‐oxo‐1,4‐dihydroquinoline‐3‐carbohydrazides were also condensation corresponding hydrazides appropriate aldehydes. Antimicrobial activity some compounds was evaluated.

Abstract magnified image A series of isolated and fused tetracyclic compounds, containing pyrido[2′,3′:3,4]pyrazolo[1,5‐ a ]pyrimidine linked with 1,3,4‐oxa‐, thiadiazole, 1,2,4‐tetrazole, pyrazole derivatives were prepared by the reaction 1,8,10‐trimethyl‐4‐oxo‐1,4‐dihydropyrido[2′,3′:3,4]pyrazolo[1,5‐ ]pyrimidine‐3‐carboxylate some common reagents to provide product in satisfactory yields. J. Heterocyclic Chem., (2010).

Abstract This paper presents the synthesis of some novel acyclonucleosides containing 2‐pyridinones and 2‐hydroxyethoxymethyl, 2,3‐dihydroxy‐propyl side chain. The tosylate these nucleosides analogues could be modified to azido derivatives. Also, with 1‐ethoxymethyl, 1‐benzyloxymethyl, 1‐methylthiomethy 1 2‐hydroxyethyl chains have been investigated. O ‐alkylated pyridine derivatives were obtained during most reactions.

Nucleoside analogs of pyridothienopyramidines were prepared by condensing the sodium salt 2a,b with an acyclic side chain in form acetylated haloalkoxyalcohol, and subsequent removal protecting acetyl group ammonia/methanol afforded 4a,b. The O-tosyl derivative 4a could then be modified to azido- amino derivatives. Reaction 2b halo-ether, benzyl halo-ether and/or halo-thioether gave N- S-alkylated products, 8 9, respectively. Coupling 10 corresponding dioxolane derivatives 11, 13, 14, which...