Synthesis and antimicrobial evaluation of substituted fluoroquinolones under conventional and microwave irradiation conditions

A series of new fluoroquinolones analogs (3a-i) were prepared under conventional and microwave irradiation technique. Ethyl 1-cyclopropyl-6,7-difluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylate (1) on reaction with boric acid and acetic anhydride in the presence of catalytic amount of zinc chloride under reflux, resulted in an unstable borate complex. Which was instantaneously treated with morpholine, piperidine, thiomorpholine, 2,6-dimethylmorpholine, 4,5,6,7-tetrahydrothieno[3,2-c]pyridine hydrochloride, 5,6,7,7a-tetrahydrothieno[3,2-c]pyridin-2(4H)-one hydrochloride, 2,3-dichlorophenylpiperazine hydrochloride, 3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride and 5,6,7,8-tetrahydro-[1,2,4] triazolo[4,3-a]pyrazine, in the presence of triethylamine to yield compounds 3a-i. The same compounds on the other hand synthesized using a microwave irradiation technique in the presence of triethylamine and adsorbed neutral alumina. The structures of the synthesized compounds were established on the basis of spectral and analytical data. The antimicrobial activity of newly synthesized compounds were evaluated against different microorganisms and found the compounds exhibited significant activity

Influence of substrate temperature on the physical properties of reactive evaporated indium oxide films

395-398<span style="font-size: 15.0pt;mso-bidi-font-size:8.0pt;font-family:" times="" new="" roman","serif""="">Indium oxide thin films were deposited on glass substrates at 373-673 K by reactive evaporation of indium in an oxygen partial pressure of 2× 10-4 mbar. The films formed at 373 K were mixed phase of indium and indium oxide where as those formed at temperatures <span style="font-size:13.5pt;mso-bidi-font-size: 6.5pt;font-family:" times="" new="" roman","serif";mso-fareast-font-family:hiddenhorzocr"="">≥<span style="font-size:13.5pt;mso-bidi-font-size:6.5pt;font-family:HiddenHorzOCR; mso-hansi-font-family:" times="" new="" roman";mso-bidi-font-family:hiddenhorzocr"=""> 473 K were single phase of indium oxide. The electrical resistivity of the films formed at 373 K was high (3.7× 10-1 <span style="font-size:14.0pt;mso-bidi-font-size:7.0pt;font-family: " times="" new="" roman","serif""="">Ω <span style="font-size:15.0pt;mso-bidi-font-size: 8.0pt;font-family:" times="" new="" roman","serif""="">cm) due to their amorphous nature. When the substrate temperature was increased to 673 K. electrical resistivity dec reased to 4.2× 10-<span style="font-size:13.0pt; mso-bidi-font-size:6.0pt;font-family:" times="" new="" roman","serif""="">3 Ω cm due to improvement in the degree of crystallinity of the films. The Hall mobility of these films increased from 2 cm<span style="font-size:13.0pt; mso-bidi-font-size:6.0pt;font-family:" times="" new="" roman","serif""="">2/V sec to 10 cm<span style="font-size:13.0pt;mso-bidi-font-size:6.0pt; font-family:" times="" new="" roman","serif""="">2<span style="font-size: 15.0pt;mso-bidi-font-size:8.0pt;font-family:" times="" new="" roman","serif""="">/V sec with the increase of substrate temperature (423-673 K). The temperature dependence of Hall mobility indicated that the grain boundary scattering of the charge carriers was predominant electrical transport in these films. The optical band gap of the films increased from 3.65 eV to 3.76 eV with the increase of substrate temperature from 473 K to 673 K, respectively. </span

4-Aminoquinolone Piperidine Amides: Noncovalent Inhibitors of DprE1 with Long Residence Time and Potent Antimycobacterial Activity

4-Aminoquinolone piperidine amides (AQs) were identified as a novel scaffold starting from a whole cell screen, with potent cidality on Mycobacterium tuberculosis (Mtb). Evaluation of the minimum inhibitory concentrations, followed by whole genome sequencing of mutants raised against AQs, identified decaprenylphosphoryl-beta-D-ribose 2'-epimerase (DprE1) as the primary target responsible for the antitubercular activity. Mass spectrometry and enzyme kinetic studies indicated that AQs are noncovalent, reversible inhibitors of DprE1 with slow on rates and long residence times of similar to 100 min on the enzyme. In general, AQs have excellent leadlike properties and good in vitro secondary pharmacology profile. Although the scaffold started off as a single active compound with moderate potency from the whole cell screen, structure-activity relationship optimization of the scaffold led to compounds with potent DprE1 inhibition (IC50 < 10 nM) along with potent cellular activity (MIC = 60 nM) against Mtb