resistant strain

Lersivirine (UK-453061) 是非核苷逆转录的抑制剂 (NNRTI)，有效抑制 NNRTI 耐药病毒。它对野生型人类免疫缺陷病毒和临床相关 NNRTI 耐药菌株显示出强大的抗逆转录病毒活性。

GNF179 Metabolite, the derivative of GNF179—an optimized 8,8-dimethyl IP analog—demonstrates significant potency (4.8 nM against the multidrug-resistant W2 strain) alongside in vitro metabolic stability and in vivo oral bioavailability.

LtaS-IN-1 是多药耐药粪肠球菌中脂磷壁酸合成的有效抑制剂，可改变细胞壁形态。 LtaS-IN-1 对抗肠球菌属 28 菌株，MIC 值从 0.5 μg/mL 到 64 μg/mL 不等。 LtaS-IN-1 抑制菌株 E1630 和 E1590，MIC 值为 0.5 μg/mL。

GNF179 是8,8-二甲基 IP 类似物。 它表现出对多药耐药菌株 W2 的效力，具有良好的体外代谢稳定性和体内口服生物相容性。

HDAC-IN-76 (compound 6i) 作为一种组蛋白去乙酰化酶 (HDAC) 抑制剂，对Pf3D7 (chloroquine 药敏品系) 和 PfDd2 (chloroquine 耐药品系) 的抗疟活性表现出色，IC50分别为30 nM 和 98 nM。该化合物在无性血期疟原虫中具有高效的抗疟作用，能选择性地抑制寄生虫生长。此外, HDAC-IN-76 对人类HDAC1和HDAC6的抑制作用强，IC50分别为7 nM 和 9 nM，且能同时抑制PfHDAC1。

Villalstonine，一种具抗癌、抗疟以及抗阿米巴原虫效果的双吲哚生物碱，对抗多药耐药性恶性疟原虫K1株表现出显著效能，其IC50为0.27 μM。

抗菌剂-38 (compound 10) 是对甲氧西林耐药金黄色葡萄球菌 (S. aureus) ATCC 700699 和非耐药菌株 ATCC 29213 的有效抑制剂，最低抑菌浓度 (MIC) 分别为 32 mg/L 和 64 mg/L。

RMM23 是一种靶向PfBDP1的抑制剂，其Kd值为 1.24 μM。RMM23 在体外血液阶段对野生型菌株3D7、NF54以及多重耐药菌株K1的EC50值分别为18 μM、14 μM和20 μM。

Mer-NF5003F (Stachybotrydial; F 1839M) 是一种从葡萄穗霉中提取的倍半萜化合物，能抑制禽类髓母细胞瘤病毒 (AMV) 蛋白酶 (IC50=7.8 μM)。它还可抑制唾液酸转移酶 6N (ST6N)、ST3O 和 ST3N（IC50=0.61、6.7 和 10 μg/mL），以及岩藻糖基转移酶 (IC50=11.3 μg/mL)。此外，Mer-NF5003F 在体外实验中显示出对单纯疱疹病毒HSV-1 (IC50=4.32 μg/mL) 和多重耐药性恶性疟原虫 K1 株 (IC50=0.85 μg/mL) 的抑制作用。

Anti-MRSA agent 11 在对氟喹诺酮敏感的菌株 USA500 和耐药 MRSA 菌株 Mu50 上展示出优良的活性，其 MIC 值为 0.39 μg/mL。Anti-MRSA agent 11 还具有良好的体内半衰期和安全性。

6-Prenylindole is a bacterial metabolite that has been found in Streptomyces and has antifungal and antimalarial properties.1 It is active against A. brassicicola strain TP-F0423 and F. oxysporum f. sp. tulipae TU-4-2 (15 and 30 μg/disc in the paper disc assay), and also drug-resistant P. falciparum strain K1 (IC50 = 21 μg/ml).2 |1. Sasaki, T., Igarashi, Y., Ogawa, M., et al. Identification of 6-prenylindole as an antifungal metabolite of Streptomyces sp. TP-A0595 and synthesis and bioactivity of 6-substituted indoles. J. Antibiot. (Tokyo) 55(11), 1009-1012 (2002).|2. Nkunya, M.H., Makangara, J.J., and Jonker, S.A. Prenylindoles from Tanzanian Monodora and Isolona species. Nat. Prod. Res. 18(3), 253-258 (2004).

Violacein is a bacterial metabolite originally isolated from C. violaceum that has antibacterial and antiprotozoal activities.[1] [2] It is produced by C. violaceum as a purple pigment in response to N-hexanoyl homoserine lactone , a property that has been modified to create a strain of C. violaceum used in detecting quorum-sensing molecules.[3] Violacein is active against Gram-positive bacteria, including B. subtilis and S. aureus (MICs = 0.8 and 1.6 µM, respectively). It is also active against P. falciparum, including chloroquine-susceptible and -resistant strains (IC50s = 0.85 and 0.63 µM, respectively).[2] It reduces parasitemia in a mouse model of nonlethal P. chabaudi chabaudi infection when administered at a dose of 7.5 mg/kg and increases survival in a mouse model of lethal P. chabaudi chabaudi infection. Violacein permeabilizes the cytoplasmic membrane of bacterial cells but does not affect the cell wall.[1]

Milbemycin A4 oxime is a derivative of milbemycin A4 and a component of milbemycin oxime , compounds that both have insecticidal and nematocidal activity. Milbemycin A4 oxime (0.05 mg/kg) reduces the number of microfilariae of the heartworm D. immitis in naturally infested dogs. It inhibits the growth of clinical isolates of C. glabrata with MIC80 values ranging from 16 to greater than 32 μg/ml. Milbemycin A4 oxime (2.5 μg/ml) blocks efflux of fluconazole from a clinical isolate of C. glabrata, but not from a strain lacking the efflux pumps CgCDR1 and PDH1, and reduces the MICs of fluconazole and 4-nitroquinoline 1-oxide in wild-type C. glabrata. It enhances adriamycin-induced inhibition of cell growth, as well as increases the intracellular accumulation of adriamycin and the P-glycoprotein substrate rhodamine 123 , in adriamycin-resistant, but not -sensitive, MCF-7 breast cancer cells in a concentration-dependent manner.

Neospiramycin I is a macrolide antibiotic and derivative of spiramycin I.1It is active against the macrolide-sensitive KB210, but not the macrolide-resistant KB224, strain ofS. aureus(MICs = 3.12 and >100 μg/ml, respectively), as well asB. cereus,B. subtilis,M. luteus,E. coli, andK. pneumoniae(MICs = 1.56, 3.12, 3.12, 0.2, 50, and 12.5 μg/ml, respectively). Neospiramycin I binds toE. coliribosomes with an IC50value of 1.2 μM. It protects against mortality in a mouse model ofS. pneumoniaetype III infection (ED50= 399.8 mg/kg).2

N-Acetyltyramine 是一种群体感应抑制剂，由溶藻弧菌 M3-10 产生。N-Acetyltyramine 可以抑制C. violaceumATCC 12472 的群体感应。它可以逆转阿霉素耐药白血病 P388 细胞的耐药性。

Licoricone exhibits anti-helicobacter pylori activity against the CLAR and AMOX-resistant strain as well as four CLAR (AMOX)-sensitive strains.

4,4'-Dicyanostilbene (化合物 43) 是一种有效的抗疟药，可抗 Dd2 菌株，EC50值为 27 nM。4,4'-Dicyanostilbene 对耐甲氧西林金黄色葡萄球菌具有体内功效。

RYL-552S 是一种可杀死恶性疟原虫 Plasmodium falciparum 的耐药菌株，其可在体外有效杀灭无性血内阶段的寄生虫。

Antimycobacterial agent-3 是一种抗分枝杆菌 (antimycobacterial) 剂，细胞毒性较低。Antimycobacterial agent-3 能够有效作用于药敏的 MTB 菌株 H37Rv 和耐药的临床分离株 (MIC< 0.029-0.110 μM)。

Anti-IAV agent 1-1a) 是一种口服抗甲型流感病毒(IAV)剂，对IAV H1N1及Oseltamivir抗性IAV H1N1的IC50值分别是0.03μM与0.06μM。

Wychimicin C为源自罕见放线菌Actinocrispum wychmicini菌株MI503-AF4的螺旋藻酸聚酮类化合物。此化合物展现出卓越的抗菌效果，尤其对耐甲氧西林的Staphylococcus. aureus（IC50=0.125-0.5 μg/mL）和Enterococcus. Faecalis/faecium（IC50=0.125-0.25 μg/mL）展现显著的抑制活性。

Wychimicin A 是一种螺旋藻酸聚酮，可从罕见的放线菌 Actinocrispum wychmicini 菌株 MI503-AF4 中分离得到。Wychimicin A 具有强抗菌活性，显著抑制耐甲氧西林的金黄色葡萄球菌Staphylococcus. aureus(IC50=0.125-0.5 μg/mL) 和 肠球菌Enterococcus. Faecalis/faecium(IC50=0.25 μg/mL)。

HIV-1inhibitor-58（Compound 10c）是一款抗逆转录病毒活性的广谱非核苷逆转录酶抑制剂，有效抑制MT-4细胞中的HIV-1 WT株IIIB以及NNRTI耐药菌株，如K103N和E138K（EC50 < 50 nM）。此外，HIV-1inhibitor-58对CYP2C9与CYP2C19也表现出抑制作用（IC50分别为2.06 μM与1.91 μM），适用于HIV感染研究。

Antimycobacterial agent-6 (compound 25) 是抗结核药物，针对野生型及氟喹诺酮耐药的结核分枝杆菌 (Mtb) 株有效。此化合物对 Mtb DprE1-C387S 突变具有抑制作用，其最小抑菌浓度（MIC90）对 H37Rv 和 MoxR 株均为 0.9 μM，对 DprE1-P116S 株为 0.5 μM。