61018-80-2Relevant academic research and scientific papers
Synthesis and α-glucosidase inhibition activity of 2-[3-(Benzoyl/4-bromobenzoyl)-4-hydroxy-1,1-dioxido-2h-benzo[e][1,2]thiazin-2-yl]-n-arylacetamides: An in silico and biochemical approach
Ahmad, Matloob,Ashfaq, Usman Ali,Aslam, Sana,Hussain, Muzammil,Lee, Dae Sung,Muddassar, Muhammad,Saddique, Furqan Ahmad,Sultan, Sadia,Taj, Saman,Zaki, Magdi E. A.
, (2021/06/08)
Diabetes mellitus (DM) is a chronic disorder and has affected a large number of people worldwide. Insufficient insulin production causes an increase in blood glucose level that results in DM. To lower the blood glucose level, various drugs are employed th
Discovery of cyclic sulfonamide derivatives as potent inhibitors of SARS-CoV-2
Shin, Young Sup,Lee, Jun Young,Noh, Soojin,Kwak, Yoonna,Jeon, Sangeun,Kwon, Sunoh,Jin, Young-hee,Jang, Min Seong,Kim, Seungtaek,Song, Jong Hwan,Kim, Hyoung Rae,Park, Chul Min
, (2020/11/13)
Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2) continues to spread worldwide, with 25 million confirmed cases and 800 thousand deaths. Effective treatments to target SARS-CoV-2 are urgently needed. In the present study, we have identified a
Synthesis and biological evaluation as well as in silico studies of arylpiperazine-1,2-benzothiazine derivatives as novel anti-inflammatory agents
Szcz??niak-Si?ga, Berenika M.,Wiatrak, Benita,Czy?nikowska, ?aneta,Janczak, Jan,Wiglusz, Rafal J.,Maniewska, Jadwiga
, (2020/12/02)
Novel arylpiperazine-1,2-benzothiazine derivatives have been designed and synthesized as potential anti-inflammatory agents. Their structure and properties have been studied using spectroscopic techniques (1H NMR, 13C NMR, FT-IR), MS
Synthesis of new tricyclic 1,2-thiazine derivatives with anti-inflammatory activity
Czy?nikowska, ?aneta,Maniewska, Jadwiga,Szcz??niak-Si?ga, Berenika M.,Wiatrak, Benita
, (2021/07/25)
New, tricyclic compounds containing a sulfonyl moiety in their structure, as potential safer COX inhibitors, were designed and synthesized. New derivatives have three conjugated rings and a sulfonyl group. A third ring, i.e., an oxazine, oxazepine or oxaz
Synthesis and pharmacological evaluation of novel arylpiperazine oxicams derivatives as potent analgesics without ulcerogenicity
Szcz??niak-Si?ga, Berenika M.,Mogilski, Szczepan,Wiglusz, Rafa? J.,Janczak, Jan,Maniewska, Jadwiga,Malinka, Wies?aw,Filipek, Barbara
, p. 1619 - 1628 (2019/03/08)
Gastrotoxicity continues to be a major issue in therapy with nonsteroidal anti-inflammatory drugs (NSAIDs). Medicine is yet to develop absolutely safe analgesics. Numerous strategies are employed to discover new, safer NSAIDs, for example selective inhibi
Stereopure Functionalized Benzosultams via Ruthenium(II)-Catalyzed Dynamic Kinetic Resolution-Asymmetric Transfer Hydrogenation
Jeran, Marko,Cotman, Andrej Emanuel,Stephan, Michel,Mohar, Barbara
, p. 2042 - 2045 (2017/04/28)
A highly diastereo- and enantioselective Ru(II)-catalyzed dynamic kinetic resolution-asymmetric transfer hydrogenation (DKR-ATH) of α-(N-sulfonylimino) and α-(N-sulfonylamino) aryl ketones to 4-hydroxy-benzo-δ- and 3-(α-hydroxy-arylmethyl)-benzo-γ-sultams is presented. By employing enantiopure ansa-Ru[PipSO2DPEN(CH2)4Ph] cat. II with S/C = 10 000 in a HCO2H/Et3N binary mix, up to >99.9% ee and dr >99:1 are obtained with 100% conversion under mild conditions. Application to access the stereopure "structurally simplified TsDPEN" N,N-ligand syn-3-(α-aminobenzyl)-benzo-γ-sultam ("syn-ULTAM") and its structural isomer trans-4-amino-3-phenyl-benzo-δ-sultam (trans-4) is demonstrated.
Discovery of (2-benzoylethen-1-ol)-containing 1,2-benzothiazine derivatives as novel 4-hydroxyphenylpyruvate dioxygenase (HPPD) inhibiting-based herbicide lead compounds
Lei, Kang,Hua, Xue-Wen,Tao, Yuan-Yuan,Liu, Yang,Liu, Na,Ma, Yi,Li, Yong-Hong,Xu, Xiao-Hua,Kong, Chui-Hua
, p. 92 - 103 (2015/12/31)
A series of (2-benzoylethen-1-ol)-containing benzothiazine derivatives was synthesized, and their herbicidal activities were first evaluated. The bioassay results indicated that some of 3-benzoyl-4-hydroxy-2-methyl-2H-1,2-benzothiazine-1,1-dioxide derivatives displayed good herbicidal activity in greenhouse testing, especially, compound 4w had good pre-emergent herbicidal activities against Brassica campestris, Amaranthus retroflexus and Echinochloa crusgalli even at a dosage of 187.5 g ha-1. More importantly, compound 4w displayed significant inhibitory activity against Arabidopsis thaliana HPPD and was identified as the most potent candidate with IC50 value of 0.48 μM, which is better than the commercial herbicide sulctrione (IC50 = 0.53 μM) and comparable with the commercial herbicide mesotrione (IC50 = 0.25 μM). The structure-activity relationships was studied and provided some useful information for improving herbicidal activity. The present work indicated that (2-benzoylethen-1-ol)-containing 1,2-benzothiazine motif could be a potential lead structure for further development of novel HPPD inhibiting-based herbicides.
Novel structural hybrids of pyrazolobenzothiazines with benzimidazoles as cholinesterase inhibitors
Aslam, Sana,Zaib, Sumera,Ahmad, Matloob,Gardiner, John M.,Ahmad, Aqeel,Hameed, Abdul,Furtmann, Norbert,Gütschow, Michael,Bajorath, Jürgen,Iqbal, Jamshed
, p. 106 - 117 (2014/04/17)
Two series of novel pyrazolobenzothiazine-based hybrid compounds were efficiently synthesized starting from saccharin sodium salt. Pyrazolo[4,3-c][1,2]benzothiazine scaffolds were N-arylated by using p-fluorobenzaldehyde, followed by the incorporation of
Synthesis of novel pyrazolobenzothiazine 5,5-dioxide derivatives as potent anti-HIV-1 agents
Ahmad, Matloob,Aslam, Sana,Bukhari, Mujahid Hussain,Montero, Catherine,Detorio, Mervi,Parvez, Masood,Schinazi, Raymond F.
, p. 1309 - 1319 (2014/03/21)
A new series of pyrazolobenzothiazine-based carbohydrazides was prepared in a facile way, starting with commercially available sodium saccharine. The final products were sufficiently characterized by spectroscopic techniques. In addition, compound 5k was
Synthesis, molecular docking and antiviral screening of novel N'-substitutedbenzylidene-2-(4-methyl-5,5-dioxido-3-phenylbenzo[e]pyrazolo[4, 3-c][1,2]thiazin-1(4H)-yl)acetohydrazides
Aslam, Sana,Ahmad, Matloob,Athar, Muhammad Makshoof,Ashfaq, Usman Ali,Gardiner, John M.,Montero, Catherine,Detorio, Mervi,Parvez, Masood,Schinazi, Raymond F.
, p. 2930 - 2946 (2014/05/06)
N'-Substitutedbenzylidene-2-(4-methyl-5,5-dioxido-3-phenylbenzo[e] pyrazolo[4,3-c][1,2]thiazin-1(4H)-yl)acetohydrazides (7a-u) were synthesized through a multistep reaction. The final compounds were screened for anti-HIV-1 and cytotoxic activities. Among
