oxadiazole

5-(5-methyl-1H-1,2,4-triazol-3-yl)-3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazole 可用于合成杂环化合物抑制 HIF 通路活性。

2-Methylbiphenyl-oxadiazole-NH-Ph-CHO 是 AUTACPD-L1degrader-3 的 PD-L1 配体，可用于 AUTAC 合成。

2-Methylbiphenyl-oxadiazole-NH-Ph-NH-PEG3-C2-NH-Boc 是 AUTACPD-L1degrader-3 的 PD-L1 配体-连接子聚合物，并可用于 AUTAC 合成。

2,5-Di(pyridin-4-yl)-1,3,4-oxadiazole 是一种有用的有机化合物，可用于生命科学领域的相关研究。其产品编号为 T67321，CAS号为 15420-02-7。

1,3,4-Oxadiazoles 是一种合成化合物，具有广泛的应用潜力，涵盖了抗惊厥、抗抑郁、镇痛、抗炎、抗过敏、抗精神病、抗微生物、抗结核、抗肿瘤及抗病毒等生物活性。该化合物的衍生物仍有待进一步研发以充分发掘其医疗潜力。

Tioxazafen 是一种二取代的恶二唑，是一种广谱种子处理杀线虫剂，对玉米，大豆和棉花中的线虫有效。

Antileishmanial agent-2 是一种基于 3-Br-isoxazoline 的疟原虫抑制剂恶性疟原虫（D10 和 W2 菌株）和利什曼原虫属。 (L. infantum 和 L.tropica) 前鞭毛体，IC50 为 0.035、0.058、3.5 和 7.5 μM。

HC-056456 (3,4-Bis(2-thienoyl)-1,2,5-oxadiazole-N-oxide) 是一种有效但不完全选择性的 CatSper 通道阻断剂。它能够减慢 [Na+]i 上升(IC50:3 µM)。

Nitrobenzoxadiazolealanine is a fluorescent dinitrophenyl analog.

(S)-BI 665915 is an orally active inhibitor of oxadiazole-containing 5-lipoxygenase-activating protein (FLAP)(IC50 of 1.7 nM for FLAP binding)..

NLRP3-IN-68 (Compound 2d) 是一种活性显著的1,3,4-恶二唑衍生物。它具备抗炎和抗氧化的特性，可以抑制炎性细胞因子的分泌、iNOS的表达以及NLRP3炎性小体的激活。NLRP3-IN-68 适用于抗炎药物的研究。

Way 120744 is a new naphthyl 3h -1,2,3,5-oxadiazole 2-oxide.

MBD, a novel fluorescent probe (7-(p-Methoxybenzylamino)-4-nitrobenz-2,1,3-oxadiazole), is utilized to study the conformation of protein and nucleoprotein. Its application is extended to bacterial ribosomes, as well as bovine trypsinogen and trypsin. MBD exhibits significant fluorescence when it binds to the hydrophobic region of macromolecules [1][2].

CAY10742 is an orally bioavailable oxadiazole antibiotic.1It is active against the Gram-positive bacteriaS. aureus,S. epidermidis,S. haemolyticus,B. cereus,B. licheniformis,E. faecalis, andE. faecium(MICs = 1-4 μg/ml), including laboratory strains and clinical isolates with varying degrees of resistance to methicillin, vancomycin, linezolid, and other antibiotics. CAY10742 (40 mg/kg) reduces the number of bacteria in mouse neutropenic thigh models of linezolid-sensitive or -resistant methicillin-resistantS. aureus(MRSA) infection. 1.Boudreau, M.A., Ding, D., Meisel, J.E., et al.Structure-activity relationship for the oxadiazole class of antibacterialsMed. Chem. Lett.11(3)322-326(2019)

CAY10761 is an inhibitor of ectonucleotide pyrophosphatase phosphodiesterase 1 (ENPP1; IC50s = 467 and 429 μM for the human and snake venom enzymes, respectively).1,2 It also inhibits mushroom tyrosinase (Ki = 1.9 μM) and urease from jack bean, P. mirabilis, and B. pasteurii (IC50s = 0.093, <0.125, and 0.089 mM, respectively, at pH 8.2).3,4 |1. Khan, K.M., Fatima, N., Rasheed, M., et al. 1,3,4-Oxadiazole-2(3H)-thione and its analogues: A new class of non-competitive nucleotide pyrophosphatases phosphodiesterases 1 inhibitors. Bioorg. Med. Chem. 17(22), 7816-7822 (2009).|2. Onyedibe, K.I., Wang, M., and Sintim, H.O. ENPP1, an old enzyme with new functions, and small molecule inhibitors - A STING in the tale of ENPP1. Molecules 24(22), E4192 (2019).|3. Ghani, U., and Ullah, N. New potent inhibitors of tyrosinase: Novel clues to binding of 1,3,4-thiadiazole-2(3H)-thiones, 1,3,4-oxadiazole-2(3H)-thiones, 4-amino-1,2,4-triazole-5(4H)-thiones, and substituted hydrazides to the dicopper active site. Bioorg. Med. Chem. 18(11), 4042-4048 (2010).|4. Amtul, Z., Rasheed, M., Choudhary, M.I., et al. Kinetics of novel competitive inhibitors of urease enzymes by a focused library of oxadiazoles thiadiazoles and triazoles. Biochem. Biophys. Res. Commun. 319(3), 1053-1063 (2004).

DDO-7263 是一种 1,2,4-Oxadiazole 衍生物， 通过与 Rpn6 结合上调 Nrf2，从而阻断 26S 蛋白酶体的组装和随后Nrf2 的泛素化降解。DDO-7263 是一种有效的Nrf2激活剂，能够激活 Nrf2-ARE 信号通路并发挥抗炎活性。

Antibacterial agent 66 (Compound 6q) 是一种三氟甲基吡啶 1,3,4-恶二唑衍生物，对 Xanthomonas oryzae pv. oryzae (Xoo) 具有活性 (EC50: 7.2 μg mL）。

Pifexole is the 1,2,4-oxadiazole derivative. It has a similar profile of muscle-relaxant activity in animals to that of chlorzoxazone. In rats, pifexole is reported to be seven times more potent than chlorzoxazone in inhibition of strychnine-induced convulsions.

P-gp BCRP-IN-2（化合物15）为恶二唑衍生物，作为ABC转运蛋白P-glycoprotein（IC50：1.6 nM）及BCRP（IC50：600 nM）的双重抑制剂。该化合物增强了Doxorubicin针对耐药型人腺癌结肠癌细胞系HT29 DX及MDCK-MDR1细胞的抗增殖效果。

Tuberculosis inhibitor 12（compound 12）作为恶二唑衍生物，表现出对结核分枝杆菌的显著抑制作用。在7H9-Tw-OADC介质中，Tuberculosis inhibitor 12（20 μM）展现了82%的抑制率，而在相同条件下抑制率为78%。

Phidianidine B，一种海洋来源的1,2,4-恶二唑代谢物，具有显著的细胞毒性。该化合物作为天然产物，可以从海洋软体动物中分离得到。

ITF5924 (compound 1) 是一种高效且极具选择性的HDAC6抑制剂，IC50为7.7 nM，对其他HDAC亚型的选择性超过104倍。ITF5924 含有二氟甲基-1,3,4-恶二唑 (DFMO) 结构，作为HDAC6缓慢结合的底物类似物，通过酶催化开环反应形成紧密且持久的酶抑制剂复合物。

SE-7552, 一种2-(difluoromethyl)-1,3,4-oxadiazole (DFMO) 衍生物，具备口服活性，是一个高选择性非异羟肟酸HDAC6抑制剂，IC50为33 nM。此化合物对所有其他已知HDAC同工酶的选择性高出850倍。SE-7552有效抑制体内多发性骨髓瘤的生长，并在饮食诱导的肥胖小鼠中起到抗肥胖作用。

MicroRNA modulator-1 (TABLE4 compound 1) 可抑制恶二唑类miR-21，AC50=14.64 μM。