Synthesis and biological screening of 2′-aryl/benzyl-2-aryl-4-methyl-4′,5-bithiazolyls as possible anti-tubercular and antimicrobial agents

Abhale, Yogita K.; Sasane, Amit V.; Chavan, Abhijit P.; Deshmukh, Keshav K.; Kotapalli, Sudha Sravanti; Ummanni, Ramesh; Sayyad, Sadikali F.; Mhaske, Pravin C.

doi:10.1016/j.ejmech.2015.03.016

Cited by 32 publications

(14 citation statements)

References 41 publications

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“…Abhale et al [108] synthesized a series of 4 ,5-bisthiazole derivatives and tested their antimicrobial activity against four bacterial strains (Bacillus subtilis, Staphylococcus aureus, Escherichia coli, and Proteus vulgaris) and one mycobacterial strain (Mycobacterium smegmatis). Amoxicillin, ciprofloxacin, rifampicin, and isoniazid were used as reference substances for antimicrobial activity assays.…”

Section: Biological Activity Of Bisthiazole Derivatives 61 Antimicrobial Activitymentioning

confidence: 99%

An Overview of the Synthesis and Antimicrobial, Antiprotozoal, and Antitumor Activity of Thiazole and Bisthiazole Derivatives

et al. 2021

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Thiazole, a five-membered heteroaromatic ring, is an important scaffold of a large number of synthetic compounds. Its diverse pharmacological activity is reflected in many clinically approved thiazole-containing molecules, with an extensive range of biological activities, such as antibacterial, antifungal, antiviral, antihelmintic, antitumor, and anti-inflammatory effects. Due to its significance in the field of medicinal chemistry, numerous biologically active thiazole and bisthiazole derivatives have been reported in the scientific literature. The current review provides an overview of different methods for the synthesis of thiazole and bisthiazole derivatives and describes various compounds bearing a thiazole and bisthiazole moiety possessing antibacterial, antifungal, antiprotozoal, and antitumor activity, encouraging further research on the discovery of thiazole-containing drugs.

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Section: Biological Activity Of Bisthiazole Derivatives 61 Antimicrobial Activitymentioning

confidence: 99%

An Overview of the Synthesis and Antimicrobial, Antiprotozoal, and Antitumor Activity of Thiazole and Bisthiazole Derivatives

et al. 2021

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“…The syntheses of compounds 1a – d to 7a – d are reported in our previous papers. Ethyl 2‐arylthiazole‐4‐carboxylate, 1a – d on reduction of carboethoxy group followed by selective oxidation using iodoxy benzoic acid furnished 2‐arylthiazole‐4‐carbaldehyde 2a – d . Aldehyde 2a – d on reaction with iodine and ammonia in tetrahydrofuran gave 2‐arylthiazole‐4‐carbonitrile 3a – d .…”

Section: Resultsmentioning

confidence: 99%

“…In our previous communication, 4,5′‐bisthiazole, 2,5′‐bisthiazole, thiazole substituted thiosemicarbazideand thiazolyl‐oxazole derivatives were shown as potent antitubercular and antibacterial agents . Encouraged by the observed biological activities of the various thiazole derivatives and as part of our ongoing search for compounds as potential antimicrobial agents, employing molecular simplification, the synthesis and antimicrobial screening of uncommon 4″‐methyl‐2,2″‐diphenyl‐4,2′:4′,5″‐terthiazole derivatives is reported.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization, and Antimicrobial Screening of 4″‐methyl‐2,2″‐diaryl‐4,2′:4′,5″‐terthiazole Derivatives

Nalawade

Mhaske

Shinde

et al. 2018

Journal of Heterocyclic Chem

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A series of novel 4″‐methyl‐2,2″‐diaryl‐4,2′:4′,5″‐terthiazole (8a‐p) derivatives has been synthesized and screened for antibacterial activity against four pathogenic bacteria, Escherichia coli, Pseudomonas flurescence, Staphylococcus aureus, and Bacillus subtilis. Among them, compounds 8a and 8j exhibited excellent antibacterial activity with minimum inhibitory concentration range of 1.0 to 5.3 μg/mL and compounds 8m and 8p exhibited moderate to good antibacterial activity with minimum inhibitory concentration range of 16.9 to 29.7 μg/mL against all tested strains. All the synthesized compounds were screened for their in vitro antifungal activity against Cocinida candida. Most of the compounds reported moderate antifungal activity. This study provides valuable directions to our ongoing endeavor of rationally designing more potent antimicrobial agent.

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“…Abhale et al. synthesized a series of bithiazolyl compounds and observed that compound 276 displayed activity (MIC = 30.38 μM) higher than standard drug isoniazid (MIC = 36.46 μM) . Balas et al.…”

Section: Thiazolesmentioning

confidence: 99%

New structural classes of antituberculosis agents

Kumar

Patel

Jain

2017

Medicinal Research Reviews

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Tuberculosis (TB), one of the deadliest diseases is shattering the health and socioeconomic status of the society. The emergence of multidrug resistant (MDR) and extremely drug resistant (XDR) strains has provided unprecedented lethal character to TB. The development of MDR and XDR strains of TB results in more deaths, longer duration of therapy, and appearance of the disease in the immunocompromised patients. Because of the development of rapid resistance by Mycobacterium tuberculosis, researchers are confronted with serious challenges in combating TB. For instance, the need for potency and specificity in therapeutic agents approaching clinics, and the increasing demand of low toxicity due to long duration of treatment. Recently, it is proposed that such challenges could be addressed by a shift from contemporary or known classes of drugs to new scaffold-containing or entirely new structural classes of drugs that possibly act on the previously unknown targets, resulting in possibly less instances of resistance development. The exploitation of advances made in the biology of TB in the last and present decades have created opportunities to discover a large number of new structural classes that specifically targets TB by molecular mechanism of action(s) unknown earlier. We have earlier reviewed new structural classes of anti-TB agents up to year 2005. This review covers literature reports of the subsequent 10 years on the discovery of new structural classes of synthetic anti-TB agents. Due to the availability of large number of research reports, we have divided new compounds in 38 structural classes, 368 structures, and 307 references.

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Synthesis and biological screening of 2′-aryl/benzyl-2-aryl-4-methyl-4′,5-bithiazolyls as possible anti-tubercular and antimicrobial agents

Cited by 32 publications

References 41 publications

An Overview of the Synthesis and Antimicrobial, Antiprotozoal, and Antitumor Activity of Thiazole and Bisthiazole Derivatives

An Overview of the Synthesis and Antimicrobial, Antiprotozoal, and Antitumor Activity of Thiazole and Bisthiazole Derivatives

Synthesis, Characterization, and Antimicrobial Screening of 4″‐methyl‐2,2″‐diaryl‐4,2′:4′,5″‐terthiazole Derivatives

New structural classes of antituberculosis agents

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