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Novel Series (novel + series)
Selected AbstractsSynthesis and Antibacterial Activity of a Novel Series of 2,3-Diaryl-substituted-imidazo(2,1- b)-benzothiazole DerivativesARCHIV DER PHARMAZIE, Issue 6 2010Mahesh Palkar Abstract Benzothiazole and imidazole compounds are extensively studied heterocyclics due to their wide spectrum of bioactivities. Among them, the imidazo(2,1- b)-benzothiazole derivatives are pharmacologically important because of their immunostimulant, anti-inflammatory, antifungal, antimicrobial, antitumor, and other activities. In the present research work, a novel series of 2,3-diaryl-substituted imidazo(2,1- b)-benzothiazoles 13a,o have been synthesized by reaction of substituted 2-aminobenzothiazoles 1,8 and an appropriately substituted ,-bromo-1-(4,,-substituted)-phenyl-2-(4,-substituted)-phenyl-1-ethanones 9,12 in the presence of anhydrous acetonitrile. They were characterized by physicochemical, elemental, and spectral (IR, 1H-NMR, and Mass) data. All the synthesized compounds were screened for their in-vitro antibacterial activity against Gram-positive, Gram-negative bacteria. The investigation of antibacterial screening data revealed that most of the compounds tested have demonstrated congruent activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa as compared with the standard ampicillin. Among the series, compounds 13d, 13h, and 13m exhibited excellent an antibacterial activity profile as compared with the standard. In summary, preliminary results indicate that some of the newly synthesized title compounds exhibited promising antibacterial activities and they warrant more consideration as prospective antimicrobials. [source] Synthesis and Antimycobacterial Activity of a Novel Series of Isonicotinylhydrazide DerivativesARCHIV DER PHARMAZIE, Issue 12 2009Sandip Jaju Abstract A novel series of 14 new isonicotinyl hydrazide derivatives 2a,g, 3a,g containing a 4-thiazolidinone / 2-azetidinone nucleus were synthesized by reacting N,-substituted arylidene / heteroarylidene isonicotinyl hydrazide 1a,g with thioglycollic acid in the presence of dry benzene and with chloroacetyl chloride in the presence of triethylamine, respectively. Structures of all newly synthesized compounds were characterized on the basis of elemental analyses and spectral data (IR and 1H-NMR). All the title compounds were tested for their in-vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv using Alamar-Blue susceptibility test, and the activity is expressed as the minimum inhibitory concentration (MIC) in ,g/mL. Among the series, compounds 2b, 2g, 3b, and 3g displayed an encouraging antimycobacterial activity profile as compared to that of the reference drugs isoniazid / rifampicin. [source] ChemInform Abstract: Synthesis and Spectral Characterization of a Novel Series of Methylcinnamate Derivatives of 15-Crown-5.CHEMINFORM, Issue 41 2009Cihan Guenduez 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] A Novel Series of Arylsulfonylthiophene-2-carboxamidine Inhibitors of the Complement Component C1s.CHEMINFORM, Issue 30 2006Nalin L. Subasinghe 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] 1-Phenyl-8-azabicyclo[3.2.1]octane Ethers: A Novel Series of Neurokinin (NK1) Antagonists.CHEMINFORM, Issue 27 2006Ian T. Huscroft 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] N-Arylpiperazine-1-carboxamide Derivatives: A Novel Series of Orally Active Nonsteroidal Androgen Receptor Antagonists.CHEMINFORM, Issue 38 2005Isao Kinoyama Abstract For Abstract see ChemInform Abstract in Full Text. [source] Thiazoles and Thiopyridines: Novel Series of High Affinity h5HT7 Ligands.CHEMINFORM, Issue 23 2004Christopher G. Thomson Abstract For Abstract see ChemInform Abstract in Full Text. [source] Novel Series of 8H-Quinazolino[4,3-b]quinazolin-8-ones via Two Niementowski Condensations.CHEMINFORM, Issue 25 2003Francois-Rene Alexandre Abstract For Abstract see ChemInform Abstract in Full Text. [source] Discovery of a Novel Series of 6-Azauracil-Based Thyroid Hormone Receptor Ligands: Potent, TR, Subtype-Selective Thyromimetics.CHEMINFORM, Issue 23 2003Robert L. Dow Abstract For Abstract see ChemInform Abstract in Full Text. [source] Photo-Oxygenation of Geraniol: Synthesis of a Novel Series of Hydroxy-Functionalized anti-Malarial 1,2,4-Trioxanes.CHEMINFORM, Issue 44 2002Chandan Singh Abstract For Abstract see ChemInform Abstract in Full Text. [source] ChemInform Abstract: Synthesis and Structure,Activity Relationships of a Novel Series of HIV-1 Protease Inhibitors Encompassing ABT-378 (Lopinavir).CHEMINFORM, Issue 33 2002Hing L. Sham 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] ChemInform Abstract: Initial Structure,Activity Relationship Studies of a Novel Series of Pyrrolo[1,2-a]pyrimid-7-ones as GnRH Receptor Antagonists.CHEMINFORM, Issue 24 2002Yun-Fei Zhu 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] ChemInform Abstract: A Novel Series of Hybrid Compounds Derived by Combining 2-Aminotetralin and Piperazine Fragments: Binding Activity at D2 and D3 ReceptorsCHEMINFORM, Issue 23 2002Aloke K. Dutta 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] ChemInform Abstract: Synthesis and Structure,Activity Relationship of 2-(Aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine Derivatives: A Novel Series of 5-HT2A/2C Receptor Antagonists.CHEMINFORM, Issue 20 2002Part 1. 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] ChemInform Abstract: A Novel Series of Thromboxane A2 Synthetase Inhibitors with Free Radical Scavenging and Antiperoxidative Activities.CHEMINFORM, Issue 46 2001Shoji Kamiya 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] ChemInform Abstract: Synthesis and Biological Evaluation of 2,5-Dihydropyrazolo[4,3-c]quinolin-3-ones, a Novel Series of PDE 4 Inhibitors with Low Emetic Potential and Antiasthmatic Properties.CHEMINFORM, Issue 14 2001Maria I. Crespo 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] Chalcones as potent antiplatelet agents and calcium channel blockersDRUG DEVELOPMENT RESEARCH, Issue 1 2001Chun-Nan Lin Abstract In an effort to continually develop potent antiplatelet agents with vasorelaxing and antiinflammatory actions, a novel series of antiinflammatory chalcones was continually screened to evaluate their antiplatelet and vasorelaxing effects. Their structure,activity relationships and mode of action were discussed and characterized. A novel series of antiinflammatory chalcones was studied on antiplatelet effect in rabbit washed platelets and human platelet-rich plasma (PRP) and vasorelaxing effect in rat thoracic aorta. Arachidonic acid-induced platelet aggregation was potently inhibited by almost all the chalcone derivatives and 13,15 also had a potent inhibitory effect on cyclooxygenase. The selective chalcones 12,16 tested in human PRP significantly inhibited secondary aggregation induced by adrenaline. In rat thoracic aorta, most of chalcones at high concentration significantly depressed the contractions induced by Ca2+ (1.9 mM) in high K+ (80 mM) medium and the phasic and tonic contractions caused by norepinephrine (3 ,M). In the rat thoracic aorta, the phenylephrine- and high K+ -induced 45Ca2+ influx were both inhibited by a selective chalcone derivative, 14. These results indicate that the antiplatelet actions of chalcones are mainly mediated through the suppression of cyclooxygenase activity and reduced thromboxane formation and their inhibitory effects on the contractile response caused by high K+ and norepinephrine in rat thoracic aorta are mainly due to inhibition of Ca2+ influx through both voltage-dependent and receptor-operated Ca2+ channels. Drug Dev. Res. 53:9,14, 2001. © 2001 Wiley-Liss, Inc. [source] Functionalized 3,3,,5,5,-Tetraaryl-1,1,-Biphenyls: Novel Platforms for Molecular ReceptorsHELVETICA CHIMICA ACTA, Issue 3 2003Roger Welti This paper describes the development of novel aromatic platforms for supramolecular construction. By the Suzuki cross-coupling protocol, a variety of functionalized m- terphenyl derivatives were prepared (Schemes,1,4). Macrolactamization of bis(ammonium salt) (S,S)- 6 with bis(acyl halide) 7 afforded the macrocyclic receptor (S,S)- 2 (Scheme,1), which was shown by 1H-NMR titration studies to form ,nesting' complexes of moderate stability (Ka between 130 and 290,M,1, 300,K) with octyl glucosides 13,15 (Fig.,2) in the noncompetitive solvent CDCl3. Suzuki cross-coupling starting from 3,3,,5,5,-tetrabromo-1,1,-biphenyl provided access to a novel series of extended aromatic platforms (Scheme,5) for cleft-type (Fig.,1) and macrotricyclic receptors such as (S,S,S,S)- 1. Although mass-spectral evidence for the formation of (S,S,S,S)- 1 by macrolactamization between the two functionalized 3,3,,5,5,-tetraaryl-1,1,-biphenyl derivatives (S,S)- 33 and 36 was obtained, the 1H- and 13C-NMR spectra of purified material remained rather inconclusive with respect to both purity and constitution. The versatile access to the novel, differentially functionalized 3,3,,5,5,-tetrabromo-1,1,-biphenyl platforms should ensure their wide use in future supramolecular construction. [source] Application of 3-methylthiopyrido[4,3- e]-1,4,2-dithiazine 1,1-dioxide to the synthesis of novel series of 4H -pyrido[4,3- e]-1,2,4-thiadiazine derivatives with potential biological activityJOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 6 2009Zdzis, aw Brzozowski Two series of 4H -pyrido[4,3- e]-1,2,4-thiadiazine derivatives 3,5 and 7,12 were synthesized by the reactions of 3-methylthiopyrido[4,3- e]-1,4,2-dithiazine 1,1-dioxide 1 with 2-or 6-hydrazinoazines and 2-aminophenols or 2-aminothiophenol, respectively. Aminolysis of 8 (R = Me, Y = O) afforded the corresponding 3-(R-amino)-4-(2-hydroxy-5-methylphenyl)-4H -pyrido[4,3- e]-1,2,4-thiadiazine 1,1-dioxides 13,18. The structures of these compounds were confirmed on the basis of elemental analysis, spectral data, and X-ray crystallography. Compounds 3,5, 7,10, 12,15, and 17,18 were screened in vitro for antibacterial activity. Moreover, preliminary in vitro anticancer assay was performed for compounds 3, 7, 10, 11,13, and 17,18 at the National Cancer Institute (Bethesda, MD) at a single dose (10 ,M) in the full NCI 60 cell panel. J. Heterocyclic Chem., (2009). [source] Ethyl {4-[2-(saccharin-2-yl)acetylsulfamoyl]phenylazo}cyanoacetate in the synthesis of polyfunctionally heteroaromatic derivativesJOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 5 2009A. A. Aly An efficient and direct one-pot reaction of ethyl saccharinylcyanoacetate derivative 3 with a variety of active methylene reagents and nitrogen nucleophiles afforded novel series of polyfunctionally substituted heteroaromatic derivatives 5,13, respectively. The pyrazole derivative 13 was seemed to be the excellent precursors for the synthesis of pyrazolo[1,5-a]pyrimidine derivatives 14,24. The antimicrobial screening of some synthesized products was evaluated against some selected bacteria and fungi. The structures of the synthesized derivatives were established by elemental and spectral data. J. Heterocyclic Chem., (2009). [source] One-pot synthesis of N2 -aminoprotected 6-substituted and cycloalka[d] 4-trifluoromethyl-2-acetylaminopyrimidinesJOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 2 2008Helio G. Bonacorso The one-pot synthesis of a novel series of amino-protected 6-alkyl-, 6-aryl-, 6-heteroaryl- and 5,6-fused-cycloalkane 4-trifluoromethyl-2-acetylaminopyrimidines, where alkyl = Me; aryl = Ph, 4-CH3Ph, 4-FPh, 4-ClPh, 4-BrPh, 4-OCH3Ph, 4-NO2Ph, 4,4,-biphenyl, 1-naphthyl; heteroaryl = 2-thienyl, 2-furyl and cycloalkyl = c -C6H4, c -C7H5 from the reaction of substituted 4-methoxy-1,1,1-trifluoroalk-3-en-2-ones with 1-acetylguanidine in acetonitrile or propan-2-ol as solvent, is reported. The acetylamino group of 2-acetylaminopyrimidines was hydrolyzed under three different conditions to afford the corresponding free 2-aminopyrimidines. [source] Synthesis, X-ray crystal structure and biological activities of ,-phenoxyl-1,2,3-thiadiazoleacetamideJOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 5 2003Wei Guang Zhao The annelation of 1,2,3-thiadiazole rings was accomplished by the reaction of N -acylhydrazone 2a bearing an adjacent ,-methyl with thionyl chloride to give ,-chloro- N -methyl-1,2,3-thiadiazole-4-acetamide 4 and was demonstrated by the X-ray crystal structure of its derivative 5a. A novel series of ,-substituted phenoxy- N -methyl-1,2,3-thiadiazole-4-acetamide 5 were synthesized through the reaction of the compound 4 and phenols. The results of bioassays show that the title compounds exhibit good anti-HBV activities. The crystal of compound 5a, N -methyl-,-2-bromophenyl-1,2,3-thiadiazole-4-acetamide, has been prepared and determined by X-ray diffraction. [source] Semibatch RAFT polymerization for producing ST/BA copolymers with controlled gradient composition profilesAICHE JOURNAL, Issue 4 2008Xiaoying Sun Abstract With controlled/living radical copolymerization, the composition profile along polymer chains becomes a tunable parameter in preparing copolymer products for novel materials properties. In this work, a novel series of styrene/butyl acrylate (St/BA) copolymers with precisely designed composition profiles (uniform, linear gradient, tanh gradient, and triblock with a linear gradient mid-block) were produced using a semibatch reversible addition-fragmentation chain transfer copolymerization mediated by benzyl dithioisobutyrate. The comonomer feeding rate was programmed based on a kinetic model with the targeted composition profile as an objective functions. The experimental composition and molecular weight profiles agreed very well with the model predictions. The polymer molecular weight distributions were narrow with polydispersity index values about 1.3. The amount of dead chains was controlled below 10%. The glass transition behaviors of the St/BA copolymers were evaluated and their Tg values were found to be in an order of uniform < linear gradient < tanh gradient < triblock with 10°C for uniform and 140°C for triblock copolymers. © 2008 American Institute of Chemical Engineers AIChE J 2008 [source] Phenothiazine- S,S -dioxide- and fluorene-based light-emitting polymers: Introduction of e, -deficient S,S -dioxide into e, -rich phenothiazineJOURNAL OF POLYMER SCIENCE (IN TWO SECTIONS), Issue 7 2007Jonghee Lee Abstract A novel series of poly(10-hexyl-phenothiazine- S,S -dioxide-3,7-diyl) and poly(9,9,-dioctyl-fluorene-2,7-diyl- alt -10-hexyl-3,7-phenothiazine- S,S -dioxide) (PFPTZ-SS) compounds were synthesized through Ni(0)-mediated Yamamoto polymerization and Pd(II)-catalyzed Suzuki polymerization. The synthesized polymers were characterized by 1H NMR spectroscopy and elemental analysis and showed higher glass transition temperatures than that of pristine polyfluorene. In terms of photoluminescence (PL), the PFPTZ-SS compounds were highly fluorescent with bright blue emissions in the solid state. Light-emitting devices were fabricated with these polymers in an indium tin oxide/poly(3,4-ethylene dioxythiophene):poly(styrene sulfonate)/polymer/Ca/Al configuration. The electroluminescence (EL) of the copolymers differed from the PL characteristics: the EL device exhibited a redshifted greenish-blue emission in contrast to the blue emission observed in the PL. Additionally, this unique phenothiazine- S,S -dioxide property, triggered by the introduction of an electron-deficient SO2 unit into the electron-rich phenothiazine, gave rise to improvements in the brightness, maximum luminescence intensity, and quantum efficiency of the EL devices fabricated with PFPTZ-SS. © 2007 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 45: 1236,1246, 2007 [source] Novel organosoluble and colorless poly(ether imide)s based on 3,3-bis[4-(3,4-dicarboxyphenoxy)phenyl]phthalide dianhydride and aromatic bis(ether amine)s bearing pendent trifluoromethyl groupsJOURNAL OF POLYMER SCIENCE (IN TWO SECTIONS), Issue 9 2006Chin-Ping Yang Abstract A novel series of colorless and highly organosoluble poly(ether imide)s were prepared from 3,3-bis[4-(3,4-dicarboxyphenoxy)phenyl]phthalide dianhydride with various fluorinated aromatic bis(ether amine)s via a conventional two-stage process that included ring-opening polyaddition to form the poly(amic acid)s followed by cyclodehydration to produce the polymer films. The poly(ether imide)s showed excellent solubility, with most of them dissoluble at a concentration of 10 wt % in amide polar solvents, in ether-type solvents, and even in chlorinated solvents. Their films had a cutoff wavelength between 358 and 373 nm, and the yellowness index ranged from 3.1 to 9.5. The glass-transition temperatures of the poly(ether imide) series were recorded between 237 and 297 °C, the decomposition temperatures at 10% weight loss were all above 494 °C, and the residue was more than 54% at 800 °C in nitrogen. These films showed high tensile strength and also were characterized by higher solubility, lighter color, and lower dielectric constants and moisture absorption than an analogous nonfluorinated polyimide series. © 2006 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 44: 3140,3152, 2006 [source] Optically Active Methacrylic Copolymers Bearing Side-Chain Bisazoaromatic and Bulky Achiral MoietiesMACROMOLECULAR CHEMISTRY AND PHYSICS, Issue 14 2007Luigi Angiolini Abstract The synthesis of two novel series of optically active methacrylic copolymers that contain a side-chain chiral moiety linked to a photochromic bisazoaromatic chromophore has been carried out by radical copolymerization of the monomer (S)-3-methacryloyloxy-1-[4,-phenylazo-(4-azobenzene)]pyrrolidine with highly sterically hindered monomers such as tert- butyl methacrylate or triphenylmethyl methacrylate with the aim to investigate the effect on the optical activity of the resulting derivatives. The copolymeric products have been fully characterized and their spectroscopic and thermal properties compared to those of the related optically active homopolymer and the copolymers with methyl methacrylate, previously reported. The optical activity displayed by the polymers is discussed in terms of extent of chiral conformations assumed by the macromolecules as a consequence of the insertion of co-monomers capable of affecting the dipole-dipole interactions that occur in these derivatives between the side-chain bisazoaromatic chromophores disposed according to a mutual chiral arrangement. [source] Synthesis and herbicidal activity of phenyl-substituted benzoylpyrazolesPEST MANAGEMENT SCIENCE (FORMERLY: PESTICIDE SCIENCE), Issue 12 2002Thomas L Siddall Abstract A novel series of substituted 3-phenyl benzoylpyrazoles were prepared and tested as potential grass herbicides. The targeted materials were prepared by three newly developed synthetic routes, which allowed a comprehensive study of the SAR (structure,activity relationships) of this series. The best combination of grass weed activity (Avena fatua L, Setaria viridis (L) Beauv and Alopecurus myosuroides Huds) and wheat selectivity was obtained with an alkoxy group in the 4-position of the phenyl ring. Activity was further enhanced by the presence of tert -butyl on the pyrazole and a methyl group at the C-2 position of the benzoyl moiety. The alkoxy-substituted 3-phenylbenzoylpyrazoles are a novel class of herbicides with potential utility for control of important grass weeds in cereals. © 2002 Society of Chemical Industry [source] Organometallic dyes: Part 1.APPLIED ORGANOMETALLIC CHEMISTRY, Issue 11 2001Synthesis of orange to cyan dyes based on donor, acceptor chromogenes using ferrocene as the donor group, conjugated Abstract A novel series of organometallic donor,conjugated,acceptor dyes derived from ferrocene as the donor group have been synthesized via the Knoevenagel reaction of ferrocene carboxaldehyde and various active methylene compounds to give a range of dyes ranging from orange to blue,green in color. The most bathochromic dye is that derived from dialkyl thiobarbituric acid and the least is that derived from the tetralone. The dyes showed an unusual negative solvatochromism as the solvent polarity increased. All dyes synthesized are expected to have some non-linear optical properties, as evidenced from the pronounced solvatochromism. Copyright ©,2001 John Wiley & Sons, Ltd. [source] Synthesis and Antibacterial Activity of a Novel Series of 2,3-Diaryl-substituted-imidazo(2,1- b)-benzothiazole DerivativesARCHIV DER PHARMAZIE, Issue 6 2010Mahesh Palkar Abstract Benzothiazole and imidazole compounds are extensively studied heterocyclics due to their wide spectrum of bioactivities. Among them, the imidazo(2,1- b)-benzothiazole derivatives are pharmacologically important because of their immunostimulant, anti-inflammatory, antifungal, antimicrobial, antitumor, and other activities. In the present research work, a novel series of 2,3-diaryl-substituted imidazo(2,1- b)-benzothiazoles 13a,o have been synthesized by reaction of substituted 2-aminobenzothiazoles 1,8 and an appropriately substituted ,-bromo-1-(4,,-substituted)-phenyl-2-(4,-substituted)-phenyl-1-ethanones 9,12 in the presence of anhydrous acetonitrile. They were characterized by physicochemical, elemental, and spectral (IR, 1H-NMR, and Mass) data. All the synthesized compounds were screened for their in-vitro antibacterial activity against Gram-positive, Gram-negative bacteria. The investigation of antibacterial screening data revealed that most of the compounds tested have demonstrated congruent activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa as compared with the standard ampicillin. Among the series, compounds 13d, 13h, and 13m exhibited excellent an antibacterial activity profile as compared with the standard. In summary, preliminary results indicate that some of the newly synthesized title compounds exhibited promising antibacterial activities and they warrant more consideration as prospective antimicrobials. [source] Synthesis and Antimycobacterial Activity of Azetidine-, Quinazoline-, and Triazolo-thiadiazole-containing PyrazinesARCHIV DER PHARMAZIE, Issue 4 2010Chandrakant G. Bonde Abstract The re-emergence of tuberculosis (TB) as a global health problem over the past few decades, accompanied by the rise of drug-resistant strains of Mycobacterium tuberculosis, emphasizes the need for the discovery of new therapeutic drugs against this disease. The emerging serious problem both in terms of TB control and clinical management prompted us to synthesize a novel series of N -[2-(substituted aryl)-3-chloro-4-oxoazetidin-1-yl]-2-(pyrazin-2-yloxy)acetamide, 6-(substituted aryl)-3-[(pyrazin-2-yloxy)methyl][1,2,4]triazolo[3,4- b][1,3,4]thiadiazole, and N -[6-({2-[(pyrazin-2-yloxy)acetyl] hydrazino}sulfonyl)-2-methyl-4-oxo-1,4-dihydroquinazolin-3(2H)yl]-substituted aryl sulfonamides. The compounds were synthesized using the appropriate synthetic route. All synthesized compounds were assayed in vitro for antimycobacterial activity against the H37 Rv strain of Mycobacterium tuberculosis. The minimum inhibitory concentration (MIC) was determined for the test compounds as well as for the reference standards. The compound which exhibited good antimycobacterial activity contains the substituents fluorine and methoxy. These electron-withdrawing or -donating substituents amend the lipophilicity of the test compounds which, in turn, alter the permeability across the bacterial cell membrane. Compounds 28, 37, and 43 showed good antimycobacterial activity while compound 51 showed a promising antimycobacterial activity. [source] | |||||||||||||||||||||||||||||||