42292-00-2Relevant academic research and scientific papers
Microwave-assisted synthesis and anti-bacterial activity of some 2-Amino-6-aryl-4-(2-thienyl)pyrimidines
Chandrasekaran,Nagarajan
, p. 279 - 282 (2005)
Some novel 2-amino-6-aryl-4-(2-thienyl)pyrimidines were synthesized from 3-aryl-1-thien-2ylprop-2-en-1-ones and guanidine hydrochloride in presence of alkali by conventional heating in alcoholic medium and microwave heating in solvent-free conditions. The compounds were evaluated for in vitro anti-bacterial activity. The anti-bacterial data revealed that compounds 5a-e had better activity against tested Gram-positive organisms than the reference ciprofloxacin and norfloxacin. However, the compounds were nearly inactive against Gram-negative bacteria. Compounds 5c and e were the most active compounds against Gram-positive bacteria.
Synthesis, molecular modeling, and biological evaluation of 4-[5-aryl-3-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl] benzenesulfonamides toward acetylcholinesterase, carbonic anhydrase I and II enzymes
Yamali, Cem,Gul, Halise Inci,Ece, Abdulilah,Taslimi, Parham,Gulcin, Ilhami
, p. 854 - 866 (2017/12/13)
In this study, 4-[5-aryl-3-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl] benzenesulfonamides were synthesized, and inhibition effects on AChE, hCA I, and hCA II were evaluated. Ki values of the compounds toward hCA I were in the range of 24.2?±?4.6-49.8?±?12.8?nm, while they were in the range of 37.3?±?9.0-65.3?±?16.7?nm toward hCA II. Ki values of the acetazolamide were 282.1?±?19.7?nm and 103.60?±?27.6?nm toward both isoenzymes, respectively. The compounds inhibited AChE with Ki in the range of 22.7?±?10.3-109.1?±?27.0?nm, whereas the tacrine had Ki value of 66.5?±?13.8?nm. Electronic structure calculations at M06-L/6-31?+?G(d,p)//AM1 level and molecular docking studies were also performed to enlighten inhibition mechanism and to support experimental findings. Results obtained from calculations of molecular properties showed that the compounds obey drug-likeness properties. The experimental and computational findings obtained in this study might be useful in the design of novel inhibitors against hCA I, hCA II, and AChE.
Facile one pot multicomponent synthesis of novel 4-(benzofuran-2-yl)-2-(3-(aryl/heteryl)-5-(aryl/heteryl)-4,5-dihydro-1H-pyrazol-1yl)thiazole derivatives
Arandkar, Varun,Vaarla, Krishnaiah,Vedula, Rajeswar Rao
, p. 1285 - 1290 (2018/05/30)
An efficient base catalyzed one pot multicomponent reaction of aryl/hetryl chalcones, thiosemicarbazide and 1-(benzofuran-2-yl)-2-bromoethan-1-one was developed to synthesize the novel 4-(benzofuran-2-yl)-2-(3-(aryl/heteryl)-5-(aryl/heteryl)-4,5-dihydro-1H-pyrazol-1yl)thiazole derivatives.
2,3,5 TRISUBSTITUTED PYRROLE DERIVATIVES AS TOPOISOMERASE INHIBITORS AND THERAPEUTIC USES THEREOF
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Page/Page column 25; 34, (2017/03/14)
The compounds of Formula (1) having topoisomerase inhibitory effect includes [Formula should be inserted here] wherein, R1 is selected from a group consisting of H, OR5, optionally substituted C1-C12 alkyl, haloalkyl, C2-C12alkenyl, C2-C12alkynyl, C1-C12alkyloxy, C1-C12haloalkyloxy, C2-C10 heteroalkyl, C3- C12 cycloalkyl, C3-C12cycloalkenyl, C2- C12heterocycloalkyl, C2-C2 heterocycloalkenyl, C6-C18aryl, and C1-C18heteroaryl; R2, R3 and R4 are independently selected from a group consisting of H, halogen, CN, - NO2, SH, CF3, OH, CO2H, CONH2, OCF3, optionally substituted C1-C12alkyl, optionally substituted C1-C12haloalkyl optionally substituted C2-C12alkenyl, optionally substituted C2- C12alkynyl, optionally substituted C1-C12alkyloxy, optionally substituted C1- C12haloalkyloxy, optionally substituted C2-C12heteroalkyl, optionally substituted C3- C12cycloalkyl, optionally substituted C3-C12 cycloalkenyl, optionally substituted C2-C12 heterocycloalkyl, optionally substituted C2-C12 heterocycloalkenyl, optionally substituted C6- C18aryl, and optionally substituted C1-C18heteroaryl; R5 is selected H, optionally substituted C1-C12alkyl, optionally substituted C2- C12alkenyl, optionally substituted optionally substituted C1-C12 haloalkyl, optionally substituted C3-C12cycloalkyl, optionally substituted C6- C18aryl, and optionally substituted C1- Ci18heteroaryl; or a pharmaceutically acceptable salt, N-oxide, or prodrug thereof.
Design, synthesis and biological evaluation of pyrazoline nucleus based homoleptic Ru(III) compounds
Mehta, Jugal V.,Gajera, Sanjay B.,Patel, Mohan N.
, p. 1367 - 1380 (2016/07/21)
A series of tri-substituted pyrazoline nucleus based homoleptic Ru(iii) complexes of type [Ru(L1-7)2]·(PF6)3 (L1-7= heterocyclic pyrazoline derivatives) were synthesized and characterized by elemental
Critical assessment of two classical synthetic methods for preparation of thiophene-substituted isoxazoles
Roman, Gheorghe
, p. 2039 - 2057 (2014/05/06)
Formation of thiophene-substituted isoxazoles by reaction of chalcone dibromides and 1,3-diketones with hydroxylamine hydrochloride has been examined under different conditions. Use of KOH as base in the reaction of dibromide chalcone analogs with hydroxy
Synthesis of 1-acetyl-3-(2-thienyl)-5-aryl-2-pyrazoline derivatives and evaluation of their anticancer activity
Oezdemir, Ahmet,Altintop, Mehlika Dilek,Kaplancikli, Zafer Asim,Turan-Zitouni, Guelhan,Ciftci, Guelsen Akalin,Yildirim, Safak Ulusoylar
, p. 1221 - 1227 (2013/12/04)
In the present study, 1-acetyl-3-(2-thienyl)-5-aryl-2-pyrazoline derivatives (1-6) were synthesized via the ring closure reaction of 1-(2-thienyl)-3-aryl-2-propen-1-ones with hydrazine hydrate in acetic acid. The chemical structures of the compounds were
Antimicrobial activity of new 4, 6-disubstituted pyrimidine, pyrazoline, and pyran derivatives
Ramiz, Mahmoud M. M.,El-Sayed, Wael A.,El-Tantawy, Asmaa I.,Abdel-Rahman, Adel A. -H.
experimental part, p. 647 - 654 (2011/11/14)
A number of new 2, 6-didisubstituted pyrimidine, pyrazoline, and pyran derivatives were synthesized starting from their chalcone derivative. The synthesized compounds displayed different degrees of antimicrobial activity against Bscillus subtilis (Gram-positive), Pseudomonas aeruginosa (Gram-negative), and Streptomyces species (Actinomycetes).
Identification of compounds with anti-West Nile virus activity
Goodell, John R.,Puig-Basagoiti, Francesc,Forshey, Brett M.,Shi, Pei-Yong,Ferguson, David M.
, p. 2127 - 2137 (2007/10/03)
The lack of antiviral compounds targeting flaviviruses represents a significant problem in the development of strategies for treating West Nile Virus (WNV), Dengue, and Yellow Fever infections. Using WNV high-throughput screening techniques developed in o
